Synthesis of 5,6-Dichloroindan-1-Acids and their Tetrazolyl Derivatives as Analgesic and Anti-inflammatory Agents

被引:0
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作者
Pal, Rajib Kumar [2 ]
Yasmin, Hasina [3 ]
Nahar, Lutfun [4 ]
Datta, Bidyut Kanti [5 ]
Chowdhury, Abul Kalam Azad [6 ]
Kundu, Joydeb Kumar [5 ]
Bachar, Sitesh Chandra [5 ]
Sarker, Satyajit Dey [1 ]
机构
[1] Wolverhampton Univ, Dept Pharm, Sch Appl Sci, Wolverhampton WV1 1LY, W Midlands, England
[2] NIA, NIH, Baltimore, MD 21224 USA
[3] State Univ Bangladesh, Dept Pharm, Dhaka 1209, Bangladesh
[4] De Montfort Univ, Leicester Sch Pharm, Leicester LE1 9BH, Leics, England
[5] Univ Dhaka, Fac Pharm, Dept Pharmaceut Technol, Dhaka 1000, Bangladesh
[6] Univ Dhaka, Fac Pharm, Dept Clin Pharm & Pharmacol, Dhaka 1000, Bangladesh
关键词
Indan acids; Indanyl tetrazoles; 5,6-dichloroindan-1-carboxylic acid; 5,6-dichloroindan-1-acetic Acid; 5-(5; 6; '-dichloroindan-1; '-yl)-tetrazole; '-yl)-methyltetrazole; Carrageenan; Analgesic activity; Anti-inflammatory activity; BIOLOGICAL EVALUATION; AMIDE DERIVATIVES; ACID; CARRAGEENIN; RAT; 5-(INDAN-1'-YL)METHYLTETRAZOLES; 5-(INDAN-1'-YL)TETRAZOLES; EDEMA; PAW;
D O I
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中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Indan derivatives, namely, 5-(5',6'-dichloroindan-1'-yl)-tetrazole (12a) and 5-(5', 6'-dichloroindan-1'-yl)methyltetrazole (12b), were synthesized conveniently from 5,6-dichloroindan-1-carboxylic acid (9a) and 5,6-dichloroindan-1-acetic acid (9b), respectively, as potential analgesic and anti-inflammatory agents. The analgesic and anti-inflammatory properties of 9a, 9b, 12a and 12b were evaluated by the acetic acid induced writhing in Swiss albino mice and the carrageenan-induced rat paw edema models, respectively. Compounds 9a and 12a exhibited significant analgesic activity with the doses of 50 and 100 mg/kg body weight, comparable to that of the positive controls, phenylbutazone, indomethacin and aminopyrine. The anti-inflammatory potencies of 9a and 12a were also comparable to that of the positive control, phenylbutazone. Compounds 9b and 12b showed analgesic and anti-inflammatory activities, but were weaker than that of compounds 9a and 12a.
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页码:874 / 882
页数:9
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