A medicinal chemists’ guide to the unique difficulties of lead optimization for tuberculosis (English)
- New search for: Dartois, Véronique
- New search for: Barry, Clifton E. 3rd
- New search for: Dartois, Véronique
- New search for: Barry, Clifton E. 3rd
In:
Bioorganic and Medicinal Chemistry Letters
;
23
, 17
;
4741-4750
;
2013
-
ISSN:
- Article (Journal) / Electronic Resource
-
Title:A medicinal chemists’ guide to the unique difficulties of lead optimization for tuberculosis
-
Contributors:Dartois, Véronique ( author ) / Barry, Clifton E. 3rd ( author )
-
Published in:Bioorganic and Medicinal Chemistry Letters ; 23, 17 ; 4741-4750
-
Publisher:
-
Publication date:2013-07-03
-
Size:10 pages
-
ISSN:
-
DOI:
-
Type of media:Article (Journal)
-
Type of material:Electronic Resource
-
Language:English
-
Keywords:
-
Source:
Table of contents – Volume 23, Issue 17
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.
- 4727
-
Graphical contents list| 2013
- 4741
-
A medicinal chemists’ guide to the unique difficulties of lead optimization for tuberculosisDartois, Véronique / Barry, Clifton E. 3rd et al. | 2013
- 4751
-
Peripherally restricted CB1 receptor blockersChorvat, Robert J. et al. | 2013
- 4761
-
Selective orexin receptor antagonistsLebold, Terry P. / Bonaventure, Pascal / Shireman, Brock T. et al. | 2013
- 4770
-
Increase of anti-HIV activity of C-peptide fusion inhibitors using a bivalent drug design approachLing, Yanbo / Xue, Huifang / Jiang, Xifeng / Cai, Lifeng / Liu, Keliang et al. | 2013
- 4774
-
Peroxisome proliferator-activated receptor delta antagonists inhibit hepatitis C virus RNA replicationBan, Shintaro / Ueda, Youki / Ohashi, Masao / Matsuno, Kenji / Ikeda, Masanori / Kato, Nobuyuki / Miyachi, Hiroyuki et al. | 2013
- 4779
-
Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrugPark, Hee Dong / Lee, Sung-Hack / Kim, Tae Hoon / Lee, Sun Hwa / Cho, Kwan Hyung / Kim, Aeri et al. | 2013
- 4785
-
Design, synthesis, and anti-tumor activities of novel triphenylethylene–coumarin hybrids, and their interactions with Ct-DNAChen, Hua / Li, Shuai / Yao, Yuchao / Zhou, Likai / Zhao, Jianpeng / Gu, Yunjing / Wang, Kerang / Li, Xiaoliu et al. | 2013
- 4790
-
Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agentsWang, Tong / Sepulveda, Mario / Gonzales, Paul / Gately, Stephen et al. | 2013
- 4794
-
Design and synthesis of bicyclic heterocycles as potent γ-secretase modulatorsOehlrich, Daniel / Rombouts, Frederik J.R. / Berthelot, Didier / Bischoff, François P. / De Cleyn, Michel A.J. / Jaroskova, Libuse / Macdonald, Gregor / Mercken, Marc / Surkyn, Michel / Trabanco, Andrés A. et al. | 2013
- 4794
-
Design and synthesis of bicyclic heterocycles as potent @c-secretase modulatorsOehlrich, D. / Rombouts, F. J. R. / Berthelot, D. / Bischoff, F. P. / De Cleyn, M. A. J. / Jaroskova, L. / Macdonald, G. / Mercken, M. / Surkyn, M. / Trabanco, A. A. et al. | 2013
- 4801
-
Promotion effect of constituents from the root of Polygonum multiflorum on hair growthSun, Ya Nan / Cui, Long / Li, Wei / Yan, Xi Tao / Yang, Seo Young / Kang, Jung Il / Kang, Hee Kyoung / Kim, Young Ho et al. | 2013
- 4806
-
Semisynthesis and quantitative structure–activity relationship (QSAR) study of some cholesterol-based hydrazone derivatives as insecticidal agentsYang, Chun / Shao, Yonghua / Zhi, Xiaoyan / Huan, Qu / Yu, Xiang / Yao, Xiaojun / Xu, Hui et al. | 2013
- 4813
-
Adipogenetic effects of retrofractamide A derivatives in 3T3-L1 cellsMourad, Ahmed Aboul-Fotouh / Nakamura, Seikou / Ueno, Tsubasa / Minami, Takahiro / Yagi, Takanari / Yasue, Haruka / Komatsu, Ryoko / Yoshikawa, Masayuki / Taye, Ashraf Mohamed / El-Moselhy, Mohamed Ahmed et al. | 2013
- 4817
-
Investigation into the functional impact of the vancomycin C-ring aryl chloridePinchman, Joseph R. / Boger, Dale L. et al. | 2013
- 4820
-
A convenient synthesis of lubeluzole and its enantiomer: Evaluation as chemosensitizing agents on human ovarian adenocarcinoma and lung carcinoma cellsCavalluzzi, Maria Maddalena / Viale, Maurizio / Bruno, Claudio / Carocci, Alessia / Catalano, Alessia / Carrieri, Antonio / Franchini, Carlo / Lentini, Giovanni et al. | 2013
- 4824
-
3,4-Dihydroxy- and 3,4-methylenedioxy- phenanthrene-type alkaloids with high selectivity for D2 dopamine receptorMoreno, Laura / Cabedo, Nuria / Ivorra, María Dolores / Sanz, María-Jesús / Castel, Arturo López / Carmen Álvarez, M. / Cortes, Diego et al. | 2013
- 4828
-
Synthesis and antifungal activities of miltefosine analogsRavu, Ranga Rao / Chen, Ying-Lien / Jacob, Melissa R. / Pan, Xuewen / Agarwal, Ameeta K. / Khan, Shabana I. / Heitman, Joseph / Clark, Alice M. / Li, Xing-Cong et al. | 2013
- 4832
-
Novel selective inhibitors of aminopeptidases that generate antigenic peptidesPapakyriakou, Athanasios / Zervoudi, Efthalia / Theodorakis, Emmanuel A. / Saveanu, Loredana / Stratikos, Efstratios / Vourloumis, Dionisios et al. | 2013
- 4837
-
Synthesis of quaternary α-amino acid-based arginase inhibitors via the Ugi reactionGolebiowski, Adam / Whitehouse, Darren / Beckett, R. Paul / Van Zandt, Michael / Ji, Min Koo / Ryder, Todd R. / Jagdmann, Erik / Andreoli, Monica / Lee, Yung / Sheeler, Ryan et al. | 2013
- 4837
-
Synthesis of quaternary @a-amino acid-based arginase inhibitors via the Ugi reactionGolebiowski, A. / Whitehouse, D. / Beckett, R. P. / Van Zandt, M. / Ji, M. K. / Ryder, T. R. / Jagdmann, E. / Andreoli, M. / Lee, Y. / Sheeler, R. et al. | 2013
- 4842
-
QM-polarized ligand docking accurately predicts the trend in binding affinity of a series of arylmethylene quinuclidine-like derivatives at the @a4@b2 and @a3@b4 nicotinic acetylcholine receptors (nAChRs)Kombo, D. C. / Grinevich, V. P. / Hauser, T. A. / Sidach, S. / Bencherif, M. et al. | 2013
- 4842
-
QM-polarized ligand docking accurately predicts the trend in binding affinity of a series of arylmethylene quinuclidine-like derivatives at the α4β2 and α3β4 nicotinic acetylcholine receptors (nAChRs)Kombo, David C. / Grinevich, Vladimir P. / Hauser, Terry A. / Sidach, Serguei / Bencherif, Merouane et al. | 2013
- 4848
-
A FRET-based assay for the discovery of West Nile Virus NS2B-NS3 protease inhibitorsAdamek, Rebecca N. / Maniquis, Roxanne V. / Khakoo, Sabaha / Bridges, Michael D. / Salzameda, Nicholas T. et al. | 2013
- 4851
-
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidaseFonseca-Berzal, Cristina / Merchán Arenas, Diego R. / Romero Bohórquez, Arnold R. / Escario, José A. / Kouznetsov, Vladimir V. / Gómez-Barrio, Alicia et al. | 2013
- 4851
-
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing @b-galactosidaseFonseca-Berzal, C. / Merchan Arenas, D. R. / Romero Bohorquez, A. R. / Escario, J. A. / Kouznetsov, V. V. / Gomez-Barrio, A. et al. | 2013
- 4857
-
Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic painBeebe, Xenia / Yeung, Clinton M. / Darczak, Daria / Shekhar, Shashank / Vortherms, Timothy A. / Miller, Loan / Milicic, Ivan / Swensen, Andrew M. / Zhu, Chang Z. / Banfor, Patricia et al. | 2013
- 4862
-
Psammaplysin F: A unique inhibitor of bacterial chromosomal partitioningRamsey, Deborah M. / Amirul Islam, Md. / Turnbull, Lynne / Davis, Rohan A. / Whitchurch, Cynthia B. / McAlpine, Shelli R. et al. | 2013
- 4867
-
Neuroactive diol and acyloin metabolites from cone snail-associated bacteriaLin, Zhenjian / Marett, Lenny / Hughen, Ronald W. / Flores, Malem / Forteza, Imelda / Ammon, Mary Anne / Concepcion, Gisela P. / Espino, Samuel / Olivera, Baldomero M. / Rosenberg, Gary et al. | 2013
- 4870
-
Access to 7@b-analogs of codeine with mixed @m/@d agonist activity via 6,7-@a-epoxide openingMagnus, P. / Ghavimi, B. / Coe, J. W. et al. | 2013
- 4870
-
Access to 7β-analogs of codeine with mixed μ/δ agonist activity via 6,7-α-epoxide openingMagnus, Philip / Ghavimi, Bahman / Coe, Jotham W. et al. | 2013
- 4875
-
Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)Dragovich, Peter S. / Bair, Kenneth W. / Baumeister, Timm / Ho, Yen-Ching / Liederer, Bianca M. / Liu, Xiongcai / Liu, Yongbo / O’Brien, Thomas / Oeh, Jason / Sampath, Deepak et al. | 2013
- 4886
-
Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanolSadek, Bassem / Shehab, Safa / Więcek, Małgorzata / Subramanian, Dhanasekaran / Shafiullah, Mohamed / Kieć-Kononowicz, Katarzyna / Adem, Abdu et al. | 2013
- 4892
-
De novo design and synthesis of a @m-conotoxin KIIIA peptidomimeticBrady, R. M. / Zhang, M. / Gable, R. / Norton, R. S. / Baell, J. B. et al. | 2013
- 4892
-
De novo design and synthesis of a μ-conotoxin KIIIA peptidomimeticBrady, Ryan M. / Zhang, Minmin / Gable, Robert / Norton, Raymond S. / Baell, Jonathan B. et al. | 2013
- 4896
-
Synthesis and binary QSAR study of antitubercular quinolylhydrazidesManvar, Atul / Khedkar, Vijay / Patel, Jignesh / Vora, Vipul / Dodia, Narsinh / Patel, Gautam / Coutinho, Evans / Shah, Anamik et al. | 2013
- 4903
-
A novel necroptosis inhibitor—necrostatin-21 and its SAR studyWu, Zhijie / Li, Ying / Cai, Yu / Yuan, Junying / Yuan, Chengye et al. | 2013
- 4907
-
Search for a novel SIRT1 activator: Structural modification of SRT1720 and biological evaluationMatsuya, Yuji / Kobayashi, Yuta / Uchida, Sayumi / Itoh, Yukihiro / Sawada, Hideyuki / Suzuki, Takayoshi / Miyata, Naoki / Sugimoto, Kenji / Toyooka, Naoki et al. | 2013
- 4911
-
Discovery of 7-azaindole based anaplastic lymphoma kinase (ALK) inhibitors: Wild type and mutant (L1196M) active compounds with unique binding modeGummadi, Venkateshwar Rao / Rajagopalan, Sujatha / Looi, Chung-Yeng / Paydar, Mohammadjavad / Renukappa, Girish Aggunda / Ainan, Bharathi Raja / Krishnamurthy, Narasimha Rao / Panigrahi, Sunil Kumar / Mahasweta, Kumari / Raghuramachandran, Sangeetha et al. | 2013
- 4919
-
Synthesis and structure–activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agentsGao, Chao / Ye, Ting-Hong / Wang, Ning-Yu / Zeng, Xiu-Xiu / Zhang, Li-Dan / Xiong, Ying / You, Xin-Yu / Xia, Yong / Xu, Ying / Peng, Cui-Ting et al. | 2013
- 4923
-
Structure–cytotoxic activity relationship of sesquilignan, morinol AYamauchi, Satoshi / Kawahara, Saya / Wukirsari, Tuti / Nishiwaki, Hisashi / Nishi, Kosuke / Sugahara, Takuya / Akiyama, Koichi / Kishida, Taro et al. | 2013
- 4931
-
Synthesis and biological evaluation of amino analogs of Ludartin: Potent and selective cytotoxic agentsLone, Shabir H. / Bhat, Khursheed A. / Shakeel-u-Rehman / Majeed, Rabiya / Hamid, Abid / Khuroo, Mohd A. et al. | 2013
- 4935
-
Syntheses of procyanidin B2 and B3 gallate derivatives using equimolar condensation mediated by Yb(OTf)3 and their antitumor activitiesSuda, Manato / Katoh, Miyuki / Toda, Kazuya / Matsumoto, Kiriko / Kawaguchi, Koichiro / Kawahara, Sei-ichi / Hattori, Yasunao / Fujii, Hiroshi / Makabe, Hidefumi et al. | 2013
- 4940
-
A monosaccharide-modified peptide phage library for screening of ligands to carbohydrate-binding proteinsArai, Kanako / Tsutsumi, Hiroshi / Mihara, Hisakazu et al. | 2013
- 4944
-
Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5Gong, Xudong / Wang, Guan / Ren, Jing / Liu, Zheng / Wang, Zhen / Chen, Tiantian / Yang, Xiaojun / Jiang, Xiangrui / Shen, Jingshan / Jiang, Hualiang et al. | 2013
- 4948
-
Novel β-dicarbonyl derivatives as inhibitors of aminopeptidase N (APN)Ma, Chunhua / Li, Xiaoguang / liang, Xuewu / Jin, Kang / Cao, Jiangying / Xu, Wenfang et al. | 2013
- 4948
-
Novel @b-dicarbonyl derivatives as inhibitors of aminopeptidase N (APN)Ma, C. / Li, X. / liang, X. / Jin, K. / Cao, J. / Xu, W. et al. | 2013
- 4953
-
Identification of GNE-293, a potent and selective PI3Kδ inhibitor: Navigating in vitro genotoxicity while improving potency and selectivitySafina, Brian S. / Sweeney, Zachary K. / Li, Jun / Chan, Bryan K. / Bisconte, Angelina / Carrera, Diane / Castanedo, Georgette / Flagella, Michael / Heald, Robert / Lewis, Cristina et al. | 2013
- 4953
-
Identification of GNE-293, a potent and selective PI3K@d inhibitor: Navigating in vitro genotoxicity while improving potency and selectivitySafina, B. S. / Sweeney, Z. K. / Li, J. / Chan, B. K. / Bisconte, A. / Carrera, D. / Castanedo, G. / Flagella, M. / Heald, R. / Lewis, C. et al. | 2013
- 4960
-
Design, synthesis and biological evaluation of novel triaryl (Z)-olefins as tamoxifen analoguesAbdellatif, Khaled R.A. / Belal, Amany / Omar, Hany A. et al. | 2013
- 4964
-
Preparation and antitrypanosomal activity of secochiliolide acid derivativesSiless, Gastón E. / Lozano, Esteban / Sánchez, Marianela / Mazzuca, Marcia / Sosa, Miguel A. / Palermo, Jorge A. et al. | 2013
- 4968
-
Antibacterial activity of quinoxalines, quinazolines, and 1,5-naphthyridinesParhi, Ajit K. / Zhang, Yongzheng / Saionz, Kurt W. / Pradhan, Padmanava / Kaul, Malvika / Trivedi, Kalkal / Pilch, Daniel S. / LaVoie, Edmond J. et al. | 2013
- 4975
-
Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activitiesNair, Padma / Yamamoto, Takashi / Largent-Milnes, Tally M. / Cowell, Scott / Kulkarni, Vinod / Moye, Sharif / Navratilova, Edita / Davis, Peg / Ma, Shou-Wu / Vanderah, Todd W. et al. | 2013
- 4979
-
The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophoreWashburn, David G. / Holt, Dennis A. / Dodson, Jason / McAtee, Jeff J. / Terrell, Lamont R. / Barton, Linda / Manns, Sharada / Waszkiewicz, Anna / Pritchard, Christina / Gillie, Dan J. et al. | 2013
- 4985
-
Selected furanochalcones as inhibitors of monoamine oxidaseRobinson, Sarel J. / Petzer, Jacobus P. / Petzer, Anél / Bergh, Jacobus J. / Lourens, Anna C.U. et al. | 2013
- 4990
-
Synthesis and cytotoxic activity evaluation of 2,3-thiazolidin-4-one derivatives on human breast cancer cell linesSala, Marina / Chimento, Adele / Saturnino, Carmela / Gomez-Monterrey, Isabel M. / Musella, Simona / Bertamino, Alessia / Milite, Ciro / Sinicropi, Maria Stefania / Caruso, Anna / Sirianni, Rosa et al. | 2013
- 4996
-
Synthesis and structure activity relationship of imidazo[1,2-a]pyridine-8-carboxamides as a novel antimycobacterial lead seriesRamachandran, Sreekanth / Panda, Manoranjan / Mukherjee, Kakoli / Choudhury, Nilanjana Roy / Tantry, Subramanyam J. / Kedari, Chaitanya Kumar / Ramachandran, Vasanthi / Sharma, Sreevalli / Ramya, V.K. / Guptha, Supreeth et al. | 2013
- 5002
-
Regioselective synthesis of 6-aryl-benzo[h][1,2,4]-triazolo[5,1-b]quinazoline-7,8-diones as potent antitumoral agentswu, Liqiang / Zhang, Chong / Li, Weilin et al. | 2013
- 5006
-
Convenient synthesis of heterobifunctional poly(ethylene glycol) suitable for the functionalization of iron oxide nanoparticles for biomedical applicationsPassemard, Solène / Staedler, Davide / Učňová, Lucia / Schneiter, Guillaume Stéphane / Kong, Phally / Bonacina, Luigi / Juillerat-Jeanneret, Lucienne / Gerber-Lemaire, Sandrine et al. | 2013
- 5011
-
Structure activity relationship study of benzo[d]thiazol-2(3H)one based σ receptor ligandsBhat, Rohit / Fishback, James A. / Matsumoto, Rae R. / Poupaert, Jacques H. / McCurdy, Christopher R. et al. | 2013
- 5011
-
Structure activity relationship study of benzo[d]thiazol-2(3H)one based @s receptor ligandsBhat, R. / Fishback, J. A. / Matsumoto, R. R. / Poupaert, J. H. / McCurdy, C. R. et al. | 2013
- 5014
-
2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitorsSiu, Michael / Pastor, Richard / Liu, Wendy / Barrett, Kathy / Berry, Megan / Blair, Wade S. / Chang, Christine / Chen, Jacob Z. / Eigenbrot, Charles / Ghilardi, Nico et al. | 2013
- 5022
-
Corrigendum to “The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus” [Bioorg. Med. Chem. Lett. 22 (2012) 7100–7105]Pfefferkorn, Jeffrey A. / Tu, Meihua / Filipski, Kevin J. / Guzman-Perez, Angel / Bian, Jianwei / Aspnes, Gary E. / Sammons, Matthew F. / Song, Wei / Li, Jian-Cheng / Jones, Christopher S. et al. | 2013
- IFC
-
Editorial board| 2013