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Preparation and properties in vitro and in vivo of antitubercular pyrroles
Author(s) -
Hearn Michael J.,
Chen Michaeline F.,
Terrot Marianne S.,
Webster Eleanor R.,
Cynamon Michael H.
Publication year - 2010
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.352
Subject(s) - chemistry , pyrrole , in vitro , in vivo , ethanol , combinatorial chemistry , catalysis , organic chemistry , biochemistry , microbiology and biotechnology , biology
1‐Acylamino‐2,5‐dimethylpyrroles were prepared in the exploration of heterocyclic structures useful for their antitubercular activity. The pyrroles were conveniently formed from the reaction of aromatic acid hydrazides with hexane‐2,5‐dione in water or ethanol, without resorting to acid catalysis . In each case, the procedure provided a single pyrrole in pure form, and the product was identified without difficulty on the basis of highly characteristic spectrometric features. Some members of this class have significant activities against drug‐resistant tuberculosis in vitro and offer substantial protection in a rigorous mouse model of the disease. J. Heterocyclic Chem., (2010).