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Bioorg Med Chem Lett ; 27(15): 3454-3459, 2017 08 01.
Article in English | MEDLINE | ID: mdl-28587823

ABSTRACT

A non-diaryl quinoline scaffold 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one was identified by screening of diverse set of compounds against M. smegmatis ATP synthase. Herein, we disclose our efforts to develop the structure activity relationship against Mycobacterium tuberculosis (Mtb.H37Rv strain) around the identified hit 1. A scaffold hopping approach was used to identify compounds 14a, 14b and 24a with improved activity against MTb.H37Rv.


Subject(s)
ATP Synthetase Complexes/antagonists & inhibitors , Antitubercular Agents/chemistry , Antitubercular Agents/pharmacology , Mycobacterium tuberculosis/enzymology , Quinolines/chemistry , Quinolines/pharmacology , ATP Synthetase Complexes/metabolism , Antitubercular Agents/chemical synthesis , Drug Design , Humans , Mycobacterium tuberculosis/drug effects , Pyrazines/chemical synthesis , Pyrazines/chemistry , Pyrazines/pharmacology , Quinolines/chemical synthesis , Structure-Activity Relationship , Tuberculosis/drug therapy , Tuberculosis/microbiology
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