Preparation and properties in vitro and in vivo of antitubercular pyrroles

✍ Scribed by Michael J. Hearn; Michaeline F. Chen; Marianne S. Terrot; Eleanor R. Webster; Michael H. Cynamon

• Publisher: Journal of Heterocyclic Chemistry
• Year: 2010
• Tongue: English
• Weight: 123 KB
• Volume: 47
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.352

✦ Synopsis

Abstract

magnified image 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).