1,5-Substituted nipecotic amides: Selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability (English)
- New search for: DeNinno, Michael P.
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In:
Bioorganic & medicinal chemistry letters
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21
, 10
; 3095-3099
;
2011
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ISSN:
- Article (Journal) / Print
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Title:1,5-Substituted nipecotic amides: Selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability
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Contributors:
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Published in:Bioorganic & medicinal chemistry letters ; 21, 10 ; 3095-3099
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Publisher:
- New search for: Elsevier
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Place of publication:Amsterdam [u.a.]
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Publication date:2011
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ISSN:
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ZDBID:
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Type of media:Article (Journal)
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Type of material:Print
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Language:English
- New search for: 35.70 / 44.33 / 44.42
- Further information on Basic classification
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Keywords:
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Source:
Table of contents – Volume 21, Issue 10
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
- 2785
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Graphical contents list| 2011
- 2806
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Structure–activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP3 receptor antagonistsMorales-Ramos, Ángel I. / Li, Yue H. / Hilfiker, Mark / Mecom, John S. / Eidam, Patrick / Shi, Dongchuan / Tseng, Pei-San / Brooks, Carl / Zhang, David / Wang, Ning et al. | 2011
- 2812
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Synthesis and antibacterial activity of alaremycin derivatives for the porphobilinogen synthaseIwai, Noritaka / Nakayama, Kyosuke / Oku, Jumpei / Kitazume, Tomoya et al. | 2011
- 2816
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SAR of 2-amino and 2,4-diamino pyrimidines with in vivo efficacy against Trypanosoma bruceiPerales, Joe B. / Freeman, Jennifer / Bacchi, Cyrus J. / Bowling, Tana / Don, Robert / Gaukel, Eric / Mercer, Luke / Moore III, Joseph A. / Nare, Bakela / Nguyen, Tien M. et al. | 2011
- 2820
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MMP-13 selective a-sulfone hydroxamates: A survey of P1prime heterocyclic amide isosteresBarta, T. E. / Becker, D. P. / Bedell, L. J. / Easton, A. M. / Hockerman, S. L. / Kiefer, J. / Munie, G. E. / Mathis, K. J. / Li, M. H. / Rico, J. G. et al. | 2011
- 2820
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MMP-13 selective α-sulfone hydroxamates: A survey of P1′ heterocyclic amide isosteresBarta, Thomas E. / Becker, Daniel P. / Bedell, Louis J. / Easton, Alan M. / Hockerman, Susan L. / Kiefer, James / Munie, Grace E. / Mathis, Karl J. / Li, Madeleine H. / Rico, Joseph G. et al. | 2011
- 2823
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MMP-13 selective alpha-sulfone hydroxamates: Identification of selective P1′ amidesFobian, Yvette M. / Freskos, John N. / Barta, Thomas E. / Bedell, Louis J. / Heintz, Robert / Kassab, Darren J. / Kiefer, James R. / Mischke, Brent V. / Molyneaux, John M. / Mullins, Patrick et al. | 2011
- 2823
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MMP-13 selective alpha-sulfone hydroxamates: Identification of selective P1prime amidesFobian, Y. M. / Freskos, J. N. / Barta, T. E. / Bedell, L. J. / Heintz, R. / Kassab, D. J. / Kiefer, J. R. / Mischke, B. V. / Molyneaux, J. M. / Mullins, P. et al. | 2011
- 2826
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Synthesis and antifungal activity of functionalized 2,3-spirostane isomersUpadhyay, Sunil Kumar / Creech, Clinton C. / Bowdy, Katharine L. / Stevens, Edwin D. / Jursic, Branko S. / Neumann, Donna M. et al. | 2011
- 2832
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Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonistsGuay, Daniel / Beaulieu, Christian / Belley, Michel / Crane, Sheldon N. / DeLuca, Jeancarlo / Gareau, Yves / Hamel, Martine / Henault, Martin / Hyjazie, Huda / Kargman, Stacia et al. | 2011
- 2836
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The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14Gauthier, Jacques Yves / Belley, Michel / Deschênes, Denis / Fournier, Jean-François / Gagné, Sébastien / Gareau, Yves / Hamel, Martine / Hénault, Martin / Hyjazie, Huda / Kargman, Stacia et al. | 2011
- 2840
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New monoterpene glycosides and phenolic compounds from Distylium racemosum and their inhibitory activity against ribonuclease HKim, Jeong Ah / Yang, Seo Young / Wamiru, Anthony / McMahon, James B. / Le Grice, Stuart F.J. / Beutler, John A. / Kim, Young Ho et al. | 2011
- 2845
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Cytotoxic and PPARs transcriptional activities of sterols from the Vietnamese soft coral Lobophytum laevigatumQuang, Tran Hong / Ha, Tran Thu / Minh, Chau Van / Kiem, Phan Van / Huong, Hoang Thanh / Ngan, Nguyen Thi Thanh / Nhiem, Nguyen Xuan / Tung, Nguyen Huu / Thao, Nguyen Phuong / Thuy, Dinh Thi Thu et al. | 2011
- 2850
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Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitorsYoo, Yeong Jae / Nam, Dong Hyuk / Jung, Seo Yun / Jang, Jae Wan / Kim, Hyoung Ja / Jin, Changbae / Pae, Ae Nim / Lee, Yong Sup et al. | 2011
- 2855
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Synthesis, structure–activity relationship of novel substituted 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylates as potential anti-mycobacterial and anticancer agentsChina Raju, B. / Nageswara Rao, R. / Suman, P. / Yogeeswari, P. / Sriram, D. / Shaik, Thokhir Basha / Kalivendi, Shasi Vardhan et al. | 2011
- 2860
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Thermal solvent-free synthesis of novel pyrazolyl chalcones and pyrazolines as potential antimicrobial agentsSiddiqui, Zeba N. / Mohammed Musthafa, T.N. / Ahmad, Anis / Khan, Asad U. et al. | 2011
- 2866
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Synthesis and in vitro antitubercular activity of ferrocene-based hydrazonesMahajan, Aman / Kremer, Laurent / Louw, Stefan / Guéradel, Yann / Chibale, Kelly / Biot, Christophe et al. | 2011
- 2869
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The Synthesis and evaluation of a novel class of (E)-3-(1-cyclohexyl-1H-pyrazol-3-yl)-2-methylacrylic acid Hepatitis C virus polymerase NS5B inhibitorsMartin, Scott W. / Glunz, Peter / Beno, Brett R. / Bergstrom, Carl / Romine, Jeffrey L. / Scott Priestley, E. / Newman, Makenzie / Gao, Min / Roberts, Susan / Rigat, Karen et al. | 2011
- 2873
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Further biochemical studies on aminopyrrolnitrin oxygenase (PrnD)Tiwari, Manish Kumar / Lee, Jung-Kul / Moon, Hee-Jung / Zhao, Huimin et al. | 2011
- 2877
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A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptorBach, Peter / Boström, Jonas / Brickmann, Kay / van Giezen, J.J.J. / Hovland, Ragnar / Petersson, Annika U. / Ray, Asim / Zetterberg, Fredrik et al. | 2011
- 2882
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Antiplasmodial and antitumor activity of dihydroartemisinin analogs derived via the aza-Michael addition reactionFeng, Tzu-Shean / Guantai, Eric M. / Nell, Margo J. / van Rensburg, Constance E.J. / Hoppe, Heinrich C. / Chibale, Kelly et al. | 2011
- 2887
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Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agentsKhera, Manoj K. / Cliffe, Ian A. / Mathur, Tarun / Prakash, Om et al. | 2011
- 2890
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SAR studies of pyridazinone derivatives as novel glucan synthase inhibitorsZhou, Gang / Ting, Pauline C. / Aslanian, Robert / Cao, Jianhua / Kim, David W. / Kuang, Rongze / Lee, Joe F. / Schwerdt, John / Wu, Heping / Jason Herr, R. et al. | 2011
- 2894
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Penicisteroids A and B, antifungal and cytotoxic polyoxygenated steroids from the marine alga-derived endophytic fungus Penicillium chrysogenum QEN-24SGao, Shu-Shan / Li, Xiao-Ming / Li, Chun-Shun / Proksch, Peter / Wang, Bin-Gui et al. | 2011
- 2898
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Pharmacophore elucidation for a new series of 2-aryl-pyrazolo-triazolo-pyrimidines as potent human A3 adenosine receptor antagonistsCheong, Siew Lee / Federico, Stephanie / Venkatesan, Gopalakrishnan / Paira, Priyankar / Shao, Yi-Ming / Spalluto, Giampiero / Yap, Chun Wei / Pastorin, Giorgia et al. | 2011
- 2906
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Antifibrotic constituents of Alnus firma on hepatic stellate cellsLee, Mina / Lee, Mi Kyeong / Kim, Young Choong / Sung, Sang Hyun et al. | 2011
- 2911
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Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonistsWang, Liping / Hubert, James A. / Lee, Susan J. / Pan, Jie / Qian, Su / Reitman, Marc L. / Strack, Alison M. / Weingarth, Drew T. / MacNeil, Douglas J. / Weber, Ann E. et al. | 2011
- 2916
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Design and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agentsLiu, Xin-Hua / Ruan, Ban-Feng / Liu, Jing-Xin / Song, Bao-An / Jing, Ling-Hong / Li, Jun / Yang, Yang / Zhu, Hai-Liang / Qi, Xing-Bao et al. | 2011
- 2921
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Synthesis of 5(6)-dihydro-OSW-1 analogs bearing three kinds of disaccharides linking at 15-hydroxy and their antitumor activitiesGuan, Yuyao / Zheng, Dan / Zhou, Liang / Wang, Haixing / Yan, Zheng / Wang, Nan / Chang, Hong / She, Pingping / Lei, Pingsheng et al. | 2011
- 2925
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Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virusZheng, Xiaofan / Hudyma, Thomas W. / Martin, Scott W. / Bergstrom, Carl / Ding, Min / He, Feng / Romine, Jeffrey / Poss, Michael A. / Kadow, John F. / Chang, Chong-Hwan et al. | 2011
- 2930
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Total synthesis of solamargineWei, Guohua / Wang, Jing / Du, Yuguo et al. | 2011
- 2934
-
A chemically modified lipase preparation for catalyzing the transesterification reaction in even highly polar organic solventsSolanki, Kusum / Gupta, Munishwar Nath et al. | 2011
- 2937
-
Synthesis and transfection activity of novel galactosylated polycationic lipidMaslov, M.A. / Medvedeva, D.A. / Rapoport, D.A. / Serikov, R.N. / Morozova, N.G. / Serebrennikova, G.A. / Vlassov, V.V. / Zenkova, М.A. et al. | 2011
- 2941
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Tumor-specific hybrid polyhydroxybutyrate nanoparticle: Surface modification of nanoparticle by enzymatically synthesized functional block copolymerLee, Jin / Jung, Sung-Geun / Park, Cheon-Seok / Kim, Hae-Yeong / Batt, Carl A. / Kim, Young-Rok et al. | 2011
- 2945
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Inhibition and structural reliability of prenylated flavones from the stem bark of Morus lhou on β-secretase (BACE-1)Cho, Jung Keun / Ryu, Young Bae / Curtis-Long, Marcus J. / Kim, Ji Young / Kim, Doman / Lee, Sun / Lee, Woo Song / Park, Ki Hun et al. | 2011
- 2945
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Inhibition and structural reliability of prenylated flavones from the stem bark of Morus lhou on b-secretase (BACE-1)Cho, J. K. / Ryu, Y. B. / Curtis-Long, M. J. / Kim, J. Y. / Kim, D. / Lee, S. / Lee, W. S. / Park, K. H. et al. | 2011
- 2949
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New aromatic substituted pyrazoles as selective inhibitors of human adipocyte fatty acid-binding proteinLiu, Xiujie / Huang, Xiaoli / Lin, Wanhua / Wang, Dongye / Diao, Yanyan / Li, Honglin / Hui, Xiaoyan / Wang, Yu / Xu, Aimin / Wu, Donghai et al. | 2011
- 2953
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Identification of chemicals to inhibit the kinase activity of leucine-rich repeat kinase 2 (LRRK2), a Parkinson’s disease-associated proteinYun, HyeJin / Heo, Hye Young / Kim, Hyun Ha / DooKim, Nam / Seol, Wongi et al. | 2011
- 2958
-
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitorsWang, Tao / Ioannidis, Stephanos / Almeida, Lynsie / Block, Michael H. / Davies, Audrey M. / Lamb, Michelle L. / Scott, David A. / Su, Mei / Zhang, Hai-Jun / Alimzhanov, Marat et al. | 2011
- 2962
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Synthesis and evaluation of novel N-fluoropyridyl derivatives of tropane as potential PET imaging agents for the dopamine transporterLiu, Jingying / Zhu, Lin / Plössl, Karl / Lieberman, Brian P. / Kung, Hank F. et al. | 2011
- 2966
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2-Arylimidazo[2,1-b]benzothiazoles: A new family of amyloid binding agents with potential for PET and SPECT imaging of Alzheimer’s brainAlagille, David / DaCosta, Herve / Baldwin, Ronald M. / Tamagnan, Gilles D. et al. | 2011
- 2969
-
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitorBeria, Italo / Bossi, Roberto T. / Brasca, Maria Gabriella / Caruso, Michele / Ceccarelli, Walter / Fachin, Gabriele / Fasolini, Marina / Forte, Barbara / Fiorentini, Francesco / Pesenti, Enrico et al. | 2011
- 2975
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Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XIIRami, Marouan / Maresca, Alfonso / Smaine, Fatma-Zhora / Montero, Jean-Louis / Scozzafava, Andrea / Winum, Jean-Yves / Supuran, Claudiu T. et al. | 2011
- 2980
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Diaryl urea analogues of SB-334867 as orexin-1 receptor antagonistsPerrey, David A. / Gilmour, Brian P. / Runyon, Scott P. / Thomas, Brian F. / Zhang, Yanan et al. | 2011
- 2986
-
Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitorsZhao, Xue Zhi / Maddali, Kasthuraiah / Metifiot, Mathieu / Smith, Steven J. / Christie Vu, B. / Marchand, Christophe / Hughes, Stephen H. / Pommier, Yves / Burke, Terrence R. Jr. et al. | 2011
- 2991
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Discovery of small molecule human FPR1 receptor antagonistsUnitt, John / Fagura, Malbinder / Phillips, Tim / King, Sarah / Perry, Matthew / Morley, Andrew / MacDonald, Cathy / Weaver, Richard / Christie, Jadeen / Barber, Simon et al. | 2011
- 2998
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Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1Yamasaki, Tomoteru / Fujinaga, Masayuki / Yoshida, Yuichiro / Kumata, Katsushi / Yui, Joji / Kawamura, Kazunori / Hatori, Akiko / Fukumura, Toshimitsu / Zhang, Ming-Rong et al. | 2011
- 3002
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Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitorsKim, Sora / Jung, Jin Kyo / Lee, Hyo Seon / Kim, Youngjae / Kim, Jiyoon / Choi, Kihang / Baek, Du-Jong / Moon, Bongjin / Oh, Kwang-Seok / Lee, Byung Ho et al. | 2011
- 3007
-
Synthesis and evaluation of quinoxaline derivatives as potential influenza NS1A protein inhibitorsYou, Lei / Cho, Eun Jeong / Leavitt, John / Ma, Li-Chung / Montelione, Gaetano T. / Anslyn, Eric V. / Krug, Robert M. / Ellington, Andrew / Robertus, Jon D. et al. | 2011
- 3012
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A green expedient synthesis of pyridopyrimidine-2-thiones and their antitubercular activityRajesh, Stephen Michael / Kumar, Raju Suresh / Libertsen, Lawzer Arun / Perumal, Subbu / Yogeeswari, Perumal / Sriram, Dharmarajan et al. | 2011
- 3017
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Synthesis and in vitro cytotoxic evaluation of N-alkylbromo and N-alkylphthalimido-isatinsSingh, Pardeep / Kaur, Sharanjeet / Kumar, Vipan / Bedi, P.M.S. / Mahajan, M.P. / Sehar, Irum / Pal, Harish Chandra / Saxena, Ajit Kumar et al. | 2011
- 3021
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Structure and characteristics of reassembled fluorescent protein, a new insight into the reassembly mechanismsIsogai, Masami / Kawamoto, Yoshihiro / Inahata, Kazuto / Fukada, Harumi / Sugimoto, Kenji / Tada, Toshiji et al. | 2011
- 3025
-
Novel 3-chlorooxazolidin-2-ones as antimicrobial agentsShiau, Timothy P. / Turtle, Eric D. / Francavilla, Charles / Alvarez, Nichole J. / Zuck, Meghan / Friedman, Lisa / O’Mahony, Donogh J.R. / Low, Eddy / Anderson, Mark B. / Najafi, Ramin (Ron) et al. | 2011
- 3029
-
Novel N-chloroheterocyclic antimicrobialsFrancavilla, Charles / Turtle, Eric D. / Kim, Bum / O’Mahony, Donogh J.R. / Shiau, Timothy P. / Low, Eddy / Alvarez, Nichole J. / Celeri, Chris E. / D’Lima, Louisa / Friedman, Lisa C. et al. | 2011
- 3034
-
Dibenzylideneacetone analogues as novel Plasmodium falciparum inhibitorsAher, Rahul Balasaheb / Wanare, Gajanan / Kawathekar, Neha / Kumar, Ravi Ranjan / Kaushik, Naveen Kumar / Sahal, Dinkar / Chauhan, Virander Singh et al. | 2011
- 3037
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Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitorYoung, Robert J. / Alderton, Wendy / Angell, Anthony D.R. / Beswick, Paul J. / Brown, David / Chambers, C. Lynn / Crowe, Miriam C. / Dawson, John / Hamlett, Christopher C.F. / Hodgson, Simon T. et al. | 2011
- 3041
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Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related α-glucosidase inhibitors and liver X receptor antagonistsMotoshima, Kazunori / Sugita, Kazuyuki / Hashimoto, Yuichi / Ishikawa, Minoru et al. | 2011
- 3041
-
Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related a-glucosidase inhibitors and liver X receptor antagonistsMotoshima, K. / Sugita, K. / Hashimoto, Y. / Ishikawa, M. et al. | 2011
- 3046
-
Semisynthesis of triptolide analogues: Effect of γ-lactone and C-14 substituents on cytotoxic activitiesAoyagi, Yutaka / Hitotsuyanagi, Yukio / Hasuda, Tomoyo / Fukaya, Haruhiko / Takeya, Koichi / Aiyama, Ritsuo / Matsuzaki, Takeshi / Hashimoto, Shusuke et al. | 2011
- 3046
-
Semisynthesis of triptolide analogues: Effect of g-lactone and C-14 substituents on cytotoxic activitiesAoyagi, Y. / Hitotsuyanagi, Y. / Hasuda, T. / Fukaya, H. / Takeya, K. / Aiyama, R. / Matsuzaki, T. / Hashimoto, S. et al. | 2011
- 3050
-
The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitorsXiang, Yibin / Hirth, Bradford / Asmussen, Gary / Biemann, Hans-Peter / Bishop, Kimberly A. / Good, Andrew / Fitzgerald, Maria / Gladysheva, Tatiana / Jain, Annuradha / Jancsics, Katherine et al. | 2011
- 3057
-
Design and synthesis of benzoxazole containing indole analogs as peroxisome proliferator-activated receptor-γ/δ dual agonistsGim, Hyo Jin / Cheon, Ye-Jin / Ryu, Jae-Ha / Jeon, Raok et al. | 2011
- 3057
-
Design and synthesis of benzoxazole containing indole analogs as peroxisome proliferator-activated receptor-g/d dual agonistsGim, H. J. / Cheon, Y. J. / Ryu, J. H. / Jeon, R. et al. | 2011
- 3062
-
Synthesis and antitumor activity of 5-[1-(3-(dimethylamino)propyl)-5-halogenated-2-oxoindolin-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamidesLv, Kai / Wang, Li-Li / Liu, Ming-Liang / Zhou, Xin-Bo / Fan, Shi-Yong / Liu, Hong-Ying / Zheng, Zhi-Bing / Li, Song et al. | 2011
- 3066
-
Synthesis and biological evaluation of benzyl styrylsulfonyl derivatives as potent anticancer mitotic inhibitorsChahrour, Osama / Abdalla, Ashraf / Lam, Frankie / Midgley, Carol / Wang, Shudong et al. | 2011
- 3070
-
Chitosan gallate as potential antioxidant biomaterialCho, Young-Sook / Kim, Se-Kwon / Je, Jae-Young et al. | 2011
- 3074
-
Synthesis and in vitro antitumor activity of new butenolide-containing dithiocarbamatesWang, Xiao-Juan / Xu, Hai-Wei / Guo, Lin-Lin / Zheng, Jia-Xin / Xu, Bo / Guo, Xiao / Zheng, Chen-Xin / Liu, Hong-Min et al. | 2011
- 3078
-
Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discoveryErlanson, Daniel A. / Arndt, Joseph W. / Cancilla, Mark T. / Cao, Kathy / Elling, Robert A. / English, Nicki / Friedman, Jessica / Hansen, Stig K. / Hession, Cathy / Joseph, Ingrid et al. | 2011
- 3084
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Regioselective one pot synthesis of 3,3′-diindolylethylene derivatives and study of their cytotoxic activityMandal, Madhumita / Kumar, Deepak / Roy, Rajneeta / Sen, Rupashree / Das, Padma / Chatterjee, Mitali / Jaisankar, Parasuraman et al. | 2011
- 3084
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Regioselective one pot synthesis of 3,3prime-diindolylethylene derivatives and study of their cytotoxic activityMandal, M. / Kumar, D. / Roy, R. / Sen, R. / Das, P. / Chatterjee, M. / Jaisankar, P. et al. | 2011
- 3088
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Virtual screening identification of novel severe acute respiratory syndrome 3C-like protease inhibitors and in vitro confirmationHanh Nguyen, Thi Thanh / Ryu, Hwa-Ja / Lee, Se-Hoon / Hwang, Soonwook / Breton, Vincent / Rhee, Joon Haeng / Kim, Doman et al. | 2011
- 3092
-
Synthesis, modelling and kinetic assays of potent inhibitors of purple acid phosphataseMohd-Pahmi, Siti Hajar / Hussein, Waleed M. / Schenk, Gerhard / McGeary, Ross P. et al. | 2011
- 3095
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1,5-Substituted nipecotic amides: Selective PDE8 inhibitors displaying diastereomer-dependent microsomal stabilityDeNinno, Michael P. / Wright, Stephen W. / Visser, Michael S. / Etienne, John B. / Moore, Dianna E. / Olson, Thanh V. / Rocke, Benjamin N. / Andrews, Melissa P. / Zarbo, Cynthia / Millham, Michele L. et al. | 2011
- 3099
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Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptorsMayorov, Alexander V. / Cai, Minying / Palmer, Erin S. / Tanaka, Dustin K. / Cain, James P. / Dedek, Matthew M. / Tan, Bahar / Trivedi, Dev / Hruby, Victor J. et al. | 2011
- 3099
-
Cyclic lactam hybrid a-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptorsMayorov, A. V. / Cai, M. / Palmer, E. S. / Tanaka, D. K. / Cain, J. P. / Dedek, M. M. / Tan, B. / Trivedi, D. / Hruby, V. J. et al. | 2011
- 3103
-
Revisiting glitazars: Thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodentsRaval, Preeti / Jain, Mukul / Goswami, Amitgiri / Basu, Sujay / Gite, Archana / Godha, Atul / Pingali, Harikishore / Raval, Saurin / Giri, Suresh / Suthar, Dinesh et al. | 2011
- 3103
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Revisiting glitazars: Thiophene substituted oxazole containing a-ethoxy phenylpropanoic acid derivatives as highly potent PPARa/g dual agonists devoid of adverse effects in rodentsRaval, P. / Jain, M. / Goswami, A. / Basu, S. / Gite, A. / Godha, A. / Pingali, H. / Raval, S. / Giri, S. / Suthar, D. et al. | 2011
- 3110
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Design, synthesis and antiproliferative activity of novel aminosubstituted benzothiopyranoisoindolesChristodoulou, Antonios / Kostakis, Ioannis K. / Kourafalos, Vassilios / Pouli, Nicole / Marakos, Panagiotis / Trougakos, Ioannis P. / Tsitsilonis, Ourania E. et al. | 2011
- 3113
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Triamino pyrimidines and pyridines as histamine H4 receptor modulatorsMeduna, Steven P. / Savall, Brad M. / Cai, Hui / Edwards, James P. / Thurmond, Robin L. / McGovern, Patricia M. et al. | 2011
- 3117
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Synthesis and antiproliferative activity of new cytotoxic azanaphthoquinone pyrrolo-annelated derivatives: Part IIShanab, Karem / Schirmer, Eva / Wulz, Eva / Weissenbacher, Barbara / Lassnig, Sigrid / Slanz, Rita / Fösleitner, Germana / Holzer, Wolfgang / Spreitzer, Helmut / Schmidt, Peter et al. | 2011
- 3122
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Synthesis and in vitro evaluation of [18F]fluoroethyl triazole labelled [Tyr3]octreotate analogues using click chemistryIddon, Lisa / Leyton, Julius / Indrevoll, Bård / Glaser, Matthias / Robins, Edward G. / George, Andrew J.T. / Cuthbertson, Alan / Luthra, Sajinder Kaur / Aboagye, Eric O. et al. | 2011
- 3128
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Design of novel and potent cPLA2α inhibitors containing an α-methyl-2-ketothiazole as a metabolically stable serine trapMete, Antonio / Andrews, Glen / Bernstein, Mike / Connolly, Stephen / Hartopp, Paul / Jackson, Clive G. / Lewis, Richard / Martin, Iain / Murray, David / Riley, Rob et al. | 2011
- 3128
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Design of novel and potent cPLA2a inhibitors containing an a-methyl-2-ketothiazole as a metabolically stable serine trapMete, A. / Andrews, G. / Bernstein, M. / Connolly, S. / Hartopp, P. / Jackson, C. G. / Lewis, R. / Martin, I. / Murray, D. / Riley, R. et al. | 2011
- 3134
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Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose controlSemple, Graeme / Ren, Albert / Fioravanti, Beatriz / Pereira, Guillherme / Calderon, Imelda / Choi, Karoline / Xiong, Yifeng / Shin, Young-Jun / Gharbaoui, Tawfik / Sage, Carleton R. et al. | 2011
- 3142
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SAR studies on a series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamides: Potent inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virusGentles, Robert G. / Ding, Min / Zheng, Xiaofan / Chupak, Louis / Poss, Michael A. / Beno, Brett R. / Pelosi, Lenore / Liu, Mengping / Lemm, Julie / Wang, Ying-Kai et al. | 2011
- 3148
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Simultaneous DSC-FTIR microspectroscopy used to screen and detect the co-crystal formation in real timeWu, Tieh-kang / Lin, Shan-Yang / Lin, Hong-Liang / Huang, Yu-Ting et al. | 2011
- 3152
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Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk)Rosenthal, Andrew S. / Tanega, Cordelle / Shen, Min / Mott, Bryan T. / Bougie, James M. / Nguyen, Dac-Trung / Misteli, Tom / Auld, Douglas S. / Maloney, David J. / Thomas, Craig J. et al. | 2011
- 3159
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Biological evaluation of 3′-O-alkylated analogs of salacinol, the role of hydrophobic alkyl group at 3′ position in the side chain on the α-glucosidase inhibitory activityTanabe, Genzoh / Otani, Tetsu / Cong, Wenying / Minematsu, Toshie / Ninomiya, Kiyofumi / Yoshikawa, Masayuki / Muraoka, Osamu et al. | 2011
- 3159
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Biological evaluation of 3prime-O-alkylated analogs of salacinol, the role of hydrophobic alkyl group at 3prime position in the side chain on the a-glucosidase inhibitory activityTanabe, G. / Otani, T. / Cong, W. / Minematsu, T. / Ninomiya, K. / Yoshikawa, M. / Muraoka, O. et al. | 2011
- 3163
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The discovery of novel 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamides as vasopressin V1A receptor antagonistsNapier, Susan / Wishart, Grant / Arbuckle, William / Baker, James / Barn, David / Bingham, Matilda / Brown, Angus / Byford, Alan / Claxton, Chris / Craighead, Mark et al. | 2011
- 3168
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Synthesis of benzologues of Nitazoxanide and Tizoxanide: A comparative study of their in vitro broad-spectrum antiprotozoal activityNavarrete-Vazquez, Gabriel / Chávez-Silva, Fabiola / Argotte-Ramos, Rocío / Rodríguez-Gutiérrez, María del Carmen / Chan-Bacab, Manuel Jesús / Cedillo-Rivera, Roberto / Moo-Puc, Rosa / Hernández-Nuñez, Emanuel et al. | 2011
- 3172
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2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitorsDai, Chaoyang / Li, Dansu / Popovici-Muller, Janeta / Zhao, Lianyun / Girijavallabhan, Vinay M. / Rosner, Kristin E. / Lavey, Brian J. / Rizvi, Razia / Shankar, Bandarpalle B. / Wong, Michael K.C. et al. | 2011
- 3177
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Dual function inhibitors of relevance to chronic obstructive pulmonary diseaseDou, Dengfeng / He, Guijia / Alliston, Kevin R. / Groutas, William C. et al. | 2010
- IFC
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Editorial board| 2011