DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW 1, 4-DIHYDROPYRIDINE (DHP) DERIVATIVES AS SELECTIVE CYCLOOXYGENASE-2 INHIBITORS

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SABAKHI IMAN; TOPUZYAN VIGEN; HAJIMAHDI ZAHRA; DARAEI BAHRAM; AREFIA HADI; ZARGHIA AFSHIN

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Journal: Iranian Journal of Pharmaceutical Research Year:2015 | Volume:14 | Issue:4 Page(s): 1087-1093

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Title

DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW 1, 4-DIHYDROPYRIDINE (DHP) DERIVATIVES AS SELECTIVE CYCLOOXYGENASE-2 INHIBITORS

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Keywords

SYNTHESIS

4-DIHYDROPYRIDINE (DHP) DERIVATIVES

COX-2 INHIBITORS

MOLECULAR MODELING

Abstract

As a continuous research for discovery of new COX-2 INHIBITORS, chemical SYNTHESIS, in vitro biological activity and molecular docking study of a new group of 1, 4-dihydropyridine (DHP) derivatives were presented. Novel synthesized compounds possessing a COX-2 SO2Me pharmacophore at the para position of C-4 phenyl ring, different hydrophobic groups (R1) at C-2 position and alkoxycarbonyl groups (COOR2) at C-3 position of 1, 4-dihydropyridine, displayed selective inhibitory activity against COX-2 isozyme. Among them, compound 5e was identified as the most potent and selective COX-2 inhibitor with IC50 value of 0.30 mM and COX-2 selectivity index of 92. Molecular docking study was performed to determine probable binding models of compound 5e. The study showed that the p-SO2Me-phenyl fragment of 5e inserted inside secondary COX-2 binding site (Arg513, Phe518, Gly519, and His90). The structure activity relationships acquired reveal that compound 5e with methyl and ethoxycarbonyl as R1 and COOR2 substitutions has the necessary geometry to provide selective inhibition of the COX-2 isozyme and it can be a good basis for the development of new hits.

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APA: Copy

SABAKHI, IMAN, TOPUZYAN, VIGEN, HAJIMAHDI, ZAHRA, DARAEI, BAHRAM, AREFIA, HADI, & ZARGHIA, AFSHIN. (2015). DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW 1, 4-DIHYDROPYRIDINE (DHP) DERIVATIVES AS SELECTIVE CYCLOOXYGENASE-2 INHIBITORS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 14(4), 1087-1093. SID. https://sid.ir/paper/288394/en

Vancouver: Copy

SABAKHI IMAN, TOPUZYAN VIGEN, HAJIMAHDI ZAHRA, DARAEI BAHRAM, AREFIA HADI, ZARGHIA AFSHIN. DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW 1, 4-DIHYDROPYRIDINE (DHP) DERIVATIVES AS SELECTIVE CYCLOOXYGENASE-2 INHIBITORS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2015;14(4):1087-1093. Available from: https://sid.ir/paper/288394/en

IEEE: Copy

IMAN SABAKHI, VIGEN TOPUZYAN, ZAHRA HAJIMAHDI, BAHRAM DARAEI, HADI AREFIA, and AFSHIN ZARGHIA, “DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW 1, 4-DIHYDROPYRIDINE (DHP) DERIVATIVES AS SELECTIVE CYCLOOXYGENASE-2 INHIBITORS,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 14, no. 4, pp. 1087–1093, 2015, [Online]. Available: https://sid.ir/paper/288394/en

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