Synthesis and antimycobacterial activity of 5-formylaminopyrimidines; analogs of antibacterial purines

Pyrimidine analogs of antimycobacterial purines have been synthesized and their biological activities evaluated. Several 5-formamidopyrimidines exhibited profound activity against Mycobacterium tuberculosis in vitro (IC 90 ⩽ 1.5 μg/mL), and they were essentially inactive against other bacteria.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-06, Vol.19 (12), p.3297-3299
Main Authors: Brændvang, Morten, Charnock, Colin, Gundersen, Lise-Lotte
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimycobacterial
Biological and medical sciences
Dose-Response Relationship, Drug
Medical sciences
Mycobacterium tuberculosis
Mycobacterium tuberculosis - drug effects
Pharmacology. Drug treatments
Purines - chemistry
Pyrimidine
Pyrimidines - chemical synthesis
Pyrimidines - pharmacology
Ring-opening
Structure-Activity Relationship
Tuberculosis
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Description
Summary:Pyrimidine analogs of antimycobacterial purines have been synthesized and their biological activities evaluated. Several 5-formamidopyrimidines exhibited profound activity against Mycobacterium tuberculosis in vitro (IC 90 ⩽ 1.5 μg/mL), and they were essentially inactive against other bacteria.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.04.082