1.
Bioorg Med Chem Lett
; 17(10): 2740-4, 2007 May 15.
Article
in English
| MEDLINE
| ID: mdl-17418567
ABSTRACT
The biological evaluation of imidazopiperidines as FAS II inhibitors of Mycobacterium tuberculosis growth has been carried out with a view to assessment of potential as lead compounds for the development of a new TB drug. A summary of the hit evaluation and current challenges is described herein.
Subject(s)
Anti-Bacterial Agents/pharmacology , Benzamides/pharmacology , Mycobacterium tuberculosis/drug effects , Piperidines/pharmacology , Anti-Bacterial Agents/chemistry , Benzamides/chemistry , Microbial Sensitivity Tests , Molecular Structure , Piperidines/chemistry , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 17(6): 1736-40, 2007 Mar 15.
Article
in English
| MEDLINE
| ID: mdl-17239593
ABSTRACT
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 2mug/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling.