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Article

Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.

Journal of medicinal chemistry - 14 Aug 2014

Bellale Eknath, Naik Maruti, V B Varun, Ambady Anisha, Narayan Ashwini, Ravishankar Sudha, Ramachandran Vasanthi, Kaur Parvinder, McLaughlin Robert, Whiteaker James, Morayya Sapna, Guptha Supreeth, Sharma Sreevalli, Raichurkar Anandkumar, Awasthy Disha, Achar Vijayshree, Vachaspati Prakash, Bandodkar Balachandra, Panda Manoranjan, Chatterji Monalisa

Abstract excerpt

Diarylthiazole (DAT), a hit from diversity screening, was found to have potent antimycobacterial activity against Mycobacterium tuberculosis (Mtb). In a systematic medicinal chemistry exploration, we demonstrated chemical opportunities to optimize the potency and physicochemical properties. The effort led to more than 10 compounds with submicromolar MICs and desirable physicochemical properties. The potent...

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PMID: 24967731
DOI: 10.1021/jm500833f

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