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Dual evaluation of some novel 2-amino-substituted coumarinylthiazoles as anti-inflammatory-antimicrobial agents and their docking studies with COX-1/COX-2 active sites.

Journal of enzyme inhibition and medicinal chemistry (2013-06-20)
Navneet Chandak, Pawan Kumar, Pawan Kaushik, Parul Varshney, Chetan Sharma, Dhirender Kaushik, Sudha Jain, Kamal R Aneja, Pawan K Sharma
ABSTRACT

Synthesis of total eighteen 2-amino-substituted 4-coumarinylthiazoles including sixteen new compounds (3a-o and 5b) bearing the benzenesulfonamide moiety is described in the present report. All the synthesized target compounds were examined for their in vivo anti-inflammatory (AI) activity and in vitro antimicrobial activity. Results revealed that six compounds (3 d, 3 f, 3 g, 3 h, 3 j and 3 n) exhibited pronounced anti-inflammatory activity comparable to the standard drug indomethacin. AI results were further confirmed by the docking studies of the most active (3n) and the least active compound (3a) with COX-1 and COX-2 active sites. In addition, most of the compounds exhibited moderate antimicrobial activity against Gram-positive bacteria as well as fungal yeast, S. cervisiae. Comparison between 3 and 5 indicated that incorporation of additional substituted pyrazole nucleus into the scaffold significantly enhanced AI activity.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Dimethyl sulfoxide-d6, 99.9 atom % D
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Dimethyl sulfoxide-d6, 99.5 atom % D
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Tetramethylsilane, ACS reagent, NMR grade, ≥99.9%
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Dimethyl sulfoxide-d6, "100%", 99.96 atom % D, contains 0.03 % (v/v) TMS
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Dimethyl sulfoxide-d6, anhydrous, 99.9 atom % D
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Dimethyl sulfoxide-d6, "Special HOH", ≥99.9 atom % D
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Dimethyl sulfoxide-d6, "100%", 99.96 atom % D
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Tetramethylsilane, electronic grade, ≥99.99% trace metals basis