期刊
LETTERS IN DRUG DESIGN & DISCOVERY
卷 3, 期 7, 页码 506-512出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/157018006778194790
关键词
carbohydrazides; hydrazones; pyrrole; synthesis; tuberculostatics
Sixteen pyrrole containing hydrazones were synthesized from isoniazid (INH) or from 1H-1-pyrrolylcarbohydrazides. Nine products exhibited 92-100% inhibitory activity against Mycobacterium tuberculosis H(37)Rv at 6.25 mu g/mL (Microplate Alamar Blue Assay). Two leads showed MICs 0.78 and > 0.1 mu g/mL, SIs > 12.82 and > 100. Drug likeness was assessed by Lipinski rule of five.
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