- 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
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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 (3d, 3f, 3g, 3h, 3j and 3n) 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.
- Chandak, Navneet,Kumar, Pawan,Kaushik, Pawan,Varshney, Parul,Sharma, Chetan,Kaushik, Dhirender,Jain, Sudha,Aneja, Kamal R.,Sharma, Pawan K.
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p. 476 - 484
(2014/08/05)
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- Synthesis of Some New Types of Thiazolyl Coumarins
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3-Acetyl coumarins I react with substituted sulfanilamides in the presence of iodine to give substituted 3-(2-arylamino-4-thiazolyl)-2H-1-benzopyran-2-ones (II). The structures of these compounds have been confirmed and they were converted into their acet
- Rao, V. Rajeswar,Rao, G. Mohan,Kumar, V. Ravi,Vardhan, V. Aditya
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