- Synthesis of 5, 6-dichloroindan-1-acids and their tetrazolyl derivatives as analgesic and anti-inflammatory agents
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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.
- Pal, Rajib Kumar,Yasmin, Hasina,Nahar, Lutfun,Datta, Bidyut Kanti,Kundu, Joydeb Kumar,Bachar, Sitesh Chandra,Chowdhury, Abul Kalam Azad,Sarker, Satyajit Dey
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p. 874 - 882,9
(2020/08/31)
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- ALLOSTERIC PROTEIN KINASE MODULATORS
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The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
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Page/Page column 73
(2010/04/30)
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