New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents

被引：101

作者：

Ballell, Lluis ^{[1
]}

Field, Robert A.

Chung, Gavin A. C.

Young, Robert J.

机构：

[1] Univ E Anglia, Sch Chem Sci & Pharm, Ctr Carbohydrate Chem, Norwich NR4 7TJ, Norfolk, England

[2] GlaxoSmithKline, Med Res Ctr, Stevenage SG1 2NY, Herts, England

[3] GlaxoSmithKline, MMPD CEDD, DDW, Tres Cantos 28760, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 06期

基金：

英国生物技术与生命科学研究理事会;

关键词：

anti-mycobacterial; anti-tubercular; thiopyrazolopyrimidines; SAR; SULFOTRANSFERASE INHIBITORS; DISCOVERY; TUBERCULOSIS; DESIGN;

D O I：

10.1016/j.bmcl.2006.12.066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The multiple parallel synthesis of a series of N,S-bis-alkylated thiopyrazolo[3,4-d]pyrimidines, based on sequential S- then N-alkylation, is reported. These compounds showed significant anti-mycobacterial activity (MICs down to < 2 mu/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：1736 / 1740

页数：5

共 33 条

[11] Microplate Alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium [J].

Collins, LA ;

Franzblau, SG .

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1997, 41 (05) :1004-1009

[12] The growing burden of tuberculosis - Global trends and interactions with the HIV epidemic [J].

Corbett, EL ;

Watt, CJ ;

Walker, N ;

Maher, D ;

Williams, BG ;

Raviglione, MC ;

Dye, C .

ARCHIVES OF INTERNAL MEDICINE, 2003, 163 (09) :1009-1021

[13] Small-molecule inhibitors of the cell cycle [J].

Crews, CM ;

Mohan, R .

CURRENT OPINION IN CHEMICAL BIOLOGY, 2000, 4 (01) :47-53

[14] Prospects for new antitubercular drugs [J].

Duncan, K ;

Barry, CE .

CURRENT OPINION IN MICROBIOLOGY, 2004, 7 (05) :460-465

[15]

ELION GB, 1993, J MED VIROL, P2

[16] Synthesis and antimycobacterial activity of 6-arylpurines:: The requirements for the N-9 substituent in active antimycobacterial purines [J].

Gundersen, LL ;

Nissen-Meyer, J ;

Spilsberg, B .

JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (06) :1383-1386

[17] Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor - Study of Lck- and FynT-dependent T cell activation [J].

Hanke, JH ;

Gardner, JP ;

Dow, RL ;

Changelian, PS ;

Brissette, WH ;

Weringer, EJ ;

Pollok, K ;

Connelly, PA .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1996, 271 (02) :695-701

[18] Combination of molecular modeling and quantitative structure-activity relationship analysis in the study of antimycobacterial activity of pyridine derivatives [J].

Klimesová, V ;

Palát, K ;

Waisser, K ;

Klimes, J .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 207 (1-2) :1-6

[19] New benzimidazole derivatives as antimycobacterial agents [J].

Klimesová, V ;

Kocí, J ;

Waisser, K ;

Kaustová, J .

FARMACO, 2002, 57 (04) :259-265

[20] Intracellular targets of cyclin-dependent kinase inhibitors: identification by affinity chromatography using immobilised inhibitors [J].

Knockaert, M ;

Gray, N ;

Damiens, E ;

Chang, YT ;

Grellier, P ;

Grant, K ;

Fergusson, D ;

Mottram, J ;

Soete, M ;

Dubremetz, JF ;

Le Roch, K ;

Doerig, C ;

Schultz, PG ;

Meijer, L .

CHEMISTRY & BIOLOGY, 2000, 7 (06) :411-422

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