Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 18, Pages 5589-5593Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.06.076
Keywords
Phenylthiazole; Nitazoxanide; Anti-tubercular; Mycobacterium tuberculosis; Minimum inhibitory concentration (MIC)
Categories
Funding
- Council of Scientific and Industrial Research
- Ministry of Health (MOH)
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In search of potential therapeutics for tuberculosis, we describe herein synthesis and biological evaluation of some substituted 4-arylthiazol-2-amino derivatives as modified analogues of the antiprotozoal drug Nitazoxanide (NTZ), which has recently been reported as potent inhibitor of Mtb H(37)Rv (Mtb MIC = 52.12 mu M) with an excellent ability to evade resistance. Among the synthesized derivatives, the two compounds 7a ( MIC = 15.28 mu M) and 7c (MIC = 17.03 mu M) have exhibited about three times better Mtb growth inhibitory activity over NTZ and are free from any cytotoxicity (Vero CC50 of 244 and 300 mu M respectively). These two compounds represent promising leads for further optimization. (C) 2011 Elsevier Ltd. All rights reserved.
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