Discovery of new antitubercular oxazolyl thiosemicarbazones

J Med Chem. 2006 Jun 15;49(12):3448-50. doi: 10.1021/jm060339h.

Dharmarajan Sriram ¹, Perumal Yogeeswari, Rathinasababathy Thirumurugan, Roheet Kumar Pavana

Affiliations

Affiliation

1 Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science, Pilani-333031, India. [email protected]

PMID: 16759086 DOI: 10.1021/jm060339h

Abstract

Twenty 4-(5-cyclobutyloxazol-2-yl)thiosemicarbazones were synthesized and evaluated for preliminary in vitro and in vivo activity against Mycobacterium tuberculosis H37Rv (MTB) and multidrug-resistant Mycobacterium tuberculosis (MDR-TB). Among them, (4-bromophenyl)(phenyl)methanone N-(5-cyclobutyl-1,3-oxazol-2-yl)thiosemicarbazone 6q was found to be the most active compound in vitro with minimum inhibitory concentration of 0.05 microg/mL against MTB and MDR-TB. In the in vivo animal model 6q decreased the Bacterial load in lung and spleen tissues with 2.1 log 10 and 3.72 log 10 protections, respectively, at 50 mg/kg body weight dose.

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