DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW IMIDAZO[2,1-B] THIAZOLE DERIVATIVES AS SELECTIVE COX-2 INHIBITORS

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SHAHRASBI MAHSA; AZAMI MOVAHED MAHSA; GHORBAN DADRAS ORKIDEH; DARAEI BAHRAM; ZARGHI AFSHIN

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Journal: Iranian Journal of Pharmaceutical Research Year:2018 | Volume:17 | Issue:4 Page(s): 1288-1296

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Title

DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW IMIDAZO[2,1-B] THIAZOLE DERIVATIVES AS SELECTIVE COX-2 INHIBITORS

Author(s)

Keywords

DESIGN

SYNTHESIS

CYCLOOXYGENASE-2 INHIBITION

IMIDAZO [2

1-B] THIAZOLE

MOLECULAR MODELING

Abstract

A new series of imidazo [2, 1-b] thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX- 2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity of COX-2 inhibitory activity were affected by the type and size of amine on C-5 of imidazo [2, 1-b] thiazole ring. Our data identified N, N-dimethyl-1- (6-(4- (methylsulfonyl) phenyl) imidazo [2, 1-b] thiazol-5-yl) methanamine (6a) as a potent and selective COX-2 inhibitor (IC50 COX-1>100 mM; IC50 COX-2=0.08 mM; selectivity index=313.7). Our results indicated that both potency and selectivity of COX-2 inhibitory activity were affected by the type and size of amine on C-5 of imidazo [2, 1-b] thiazole ring.

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APA: Copy

SHAHRASBI, MAHSA, AZAMI MOVAHED, MAHSA, GHORBAN DADRAS, ORKIDEH, DARAEI, BAHRAM, & ZARGHI, AFSHIN. (2018). DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW IMIDAZO[2,1-B] THIAZOLE DERIVATIVES AS SELECTIVE COX-2 INHIBITORS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 17(4), 1288-1296. SID. https://sid.ir/paper/288897/en

Vancouver: Copy

SHAHRASBI MAHSA, AZAMI MOVAHED MAHSA, GHORBAN DADRAS ORKIDEH, DARAEI BAHRAM, ZARGHI AFSHIN. DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW IMIDAZO[2,1-B] THIAZOLE DERIVATIVES AS SELECTIVE COX-2 INHIBITORS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2018;17(4):1288-1296. Available from: https://sid.ir/paper/288897/en

IEEE: Copy

MAHSA SHAHRASBI, MAHSA AZAMI MOVAHED, ORKIDEH GHORBAN DADRAS, BAHRAM DARAEI, and AFSHIN ZARGHI, “DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW IMIDAZO[2,1-B] THIAZOLE DERIVATIVES AS SELECTIVE COX-2 INHIBITORS,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 17, no. 4, pp. 1288–1296, 2018, [Online]. Available: https://sid.ir/paper/288897/en

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