Ontology highlight
ABSTRACT:
SUBMITTER: Meissner A
PROVIDER: S-EPMC3816974 | biostudies-literature | 2013 Nov
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry 20130903 21
A series of 2-aminothiazoles was synthesized based on a HTS scaffold from a whole-cell screen against Mycobacterium tuberculosis (Mtb). The SAR shows the central thiazole moiety and the 2-pyridyl moiety at C-4 of the thiazole are intolerant to modification. However, the N-2 position of the aminothiazole exhibits high flexibility and we successfully improved the antitubercular activity of the initial hit by more than 128-fold through introduction of substituted benzoyl groups at this position. N- ...[more]