Publication Type : Journal Article
Publisher : Letters in Drug Design & Discovery
Source : Letters in Drug Design & Discovery, Vol. 10, pp. 594-603, 2013.
Url : https://pubmed.ncbi.nlm.nih.gov/25468039/
Campus : Kochi
School : School of Pharmacy
Department : Pharmaceutical Chemistry & Analysis
Year : 2013
Abstract : A few celecosib like 1,5-diarylpyrazoles conjugated with nitric oxide (NO) donating nitrate ester group were synthesized and evaluated for their selective COX-2 inhibitory activity along with NO releasing ability of corresponding nitrate esters. Most of the synthesized compounds exhibited improved COX-2 inhibition when compared with the reference drug celecoxib. The nitrate ester derivatives (coxib prodrugs) 7 (nitrate ester of 1,5-diarylpyrazole with 2 carbon linker), and 9 (nitrate ester of 1,5-diarylpyrazole with 3 carbon linker), upon incubation in human whole blood were partly transformed into the corresponding alcohols 6, and 8 respectively. Molecular docking studies were performed on alcohol derivatives and revealed additional H-bond interactions compared to celecoxib.
Cite this Research Publication : Rao, B. N.; Muthuppalaniappan, M.; Dinavahi, S. S.; Viswanadha, S.; Bagul, C.; Srinivas, K.; Vakkalanka, S. K. V.; Atcha, K. R.; Kamal, A. Synthesis of 1, 5- Diarylpyrazoles as Potential COX-2 Inhibitors with Nitric Oxide Releasing Ability. Letters in Drug Design & Discovery, Vol. 10, pp. 594-603, 2013.