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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Synthesis and analgesic/anti-inflammatory evaluation of fused heterocyclic ring systems incorporating phenylsulfonyl moiety
Bioorganic and Medicinal Chemistry, Volume 16, No. 12, Year 2008
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Description
A series of pyrazolo[1,5-a]pyrimidine, triazolo[1,5-a]pyrimidine, and pyrimido[1,2-a]benzimidazole ring systems incorporating phenylsulfonyl moiety were synthesized via the reaction of 3-(N,N-dimethylamino)-1-aryl-2-(phenylsulfonyl)prop-2-en-1-one derivatives 2a,b with appropriate nitrogen nucleophiles. The analgesic and anti-inflammatory activities of the newly synthesized compound were investigated in vivo. 3-Bromo-2-phenyl-6-(phenylsulfonyl)-7-(4-methylphenyl)pyrazolo[1,5-a]pyrimidine (5e) was found to have an excellent analgesic activity in comparison with indomethacin as a reference drug, while the highest anti-inflammatory effect was observed in the case of 2-(4-bromophenyl)-6-(phenylsulfonyl)-5-(4-methylphenyl)pyrazolo[1,5-a]pyrimidine (5d). From the structure-activity relationship (SAR) point of view, the analgesic/anti-inflammatory activity of pyrazolo[1,5-a]pyrimidine derivatives was found to be much higher than triazolo[1,5-a]pyrimidine and pyrimido[1,2-a]benzimidazole derivatives. © 2008 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Shaaban, Mohamed Rabie
Egypt, Giza
Faculty of Science
Saleh, Tamer S.
Egypt, Giza
National Research Centre
Mayhoub, Abdelrahman S.
Egypt, Cairo
Faculty of Pharmacy
Mansour, Ahmed Mohamed
Egypt, Cairo
Faculty of Pharmacy
Farag, Ahmad M.
Egypt, Giza
Faculty of Science
Statistics
Citations: 89
Authors: 5
Affiliations: 3
Identifiers
Doi:
10.1016/j.bmc.2008.05.011
ISSN:
09680896