Design and Synthesis of Novel Indolizine Analogues as COX-2 Inhibitors: Computational Perspective and in vitro Screening

被引：20

作者：

Sandeep, Chandrashekharappa ^{[1
]}

Venugopala, Katharigatta Narayanaswamy ^{[2
,3
]}

Khedr, Mohammed A. ^{[3
,4
]}

Padmashali, Basavaraj ^{[5
,6
]}

Kulkarni, Rashmi Sanganna ^{[7
]}

Venugopala, Rashmi ^{[8
]}

Odhav, Bharti ^{[2
]}

机构：

[1] GKVK, TIFR, NCBS, Inst Stem Cell Biol & Regenerat Med, Bellary Rd, Bangalore 560065, Karnataka, India

[2] Durban Univ Technol, Dept Biotechnol & Food Technol, ZA-4001 Durban, South Africa

[3] King Faisal Univ, Dept Pharmaceut Sci, Coll Clin Pharm, Al Hasa 31982, Saudi Arabia

[4] Helwan Univ, Dept Pharmaceut Chem, Fac Pharm, Cairo 11795, Egypt

[5] Sahyadri Sci Coll Autonomous, Dept Chem, Shimoga 577203, India

[6] Rani Channamma Univ, Sch Basic Sci, Dept Studies & Res Chem, Belagavi 591156, Karnataka, India

[7] Jain Univ, Dept Chem, Bangalore 560019, Karnataka, India

[8] Univ KwaZulu Natal, Dept Publ Hlth Med, Howard Coll Campus, ZA-4001 Durban, South Africa

来源：

INDIAN JOURNAL OF PHARMACEUTICAL EDUCATION AND RESEARCH | 2017年 / 51卷 / 03期

基金：

新加坡国家研究基金会;

关键词：

Cox-2; Inhibition; Indolizine Analogues; Synthesis; Characterization; Molecular Docking; PLANT ANTITUMOR AGENTS; N-FUSED HETEROCYCLES; QUINOLIZIDINE ALKALOIDS; HETEROAROMATIC-COMPOUNDS; ANTIINFLAMMATORY AGENTS; RECEPTOR ANTAGONISTS; ANOPHELES-ARABIENSIS; EFFICIENT SYNTHESIS; POTENT INHIBITORS; DERIVATIVES;

D O I：

10.5530/ijper.51.3.73

中图分类号：

G40 [教育学];

学科分类号：

040101 ; 120403 ;

摘要：

Design and synthesis of a new series of ethyl 7-methoxy-2-substituted-3-(substituted benzoyl) indolizine-1-carboxylates 2a-i was achieved and screened for their in vitro inhibitory activity against COX-2 enzyme. Compound 2a and 2c emerged as promising COX-2 enzyme inhibitor with IC50 of 6.56 and 6.94 mu M respectively from the synthesized series when compared to Celecoxib and Indomethacin as selective and nonselective standards, respectively. Computational docking study identified the possible reasons for such activity that may be due to the cis configuration of the indolizines that resulted in the most stable conformation similar to that of Indomethacin.

引用

页码：452 / 460

页数：9

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