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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Design, synthesis, and biological evaluation of substituted hydrazone and pyrazole derivatives as selective COX-2 inhibitors: Molecular docking study
Bioorganic and Medicinal Chemistry, Volume 19, No. 11, Year 2011
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Description
New arylhydrazone derivatives and a series of 1,5-diphenyl pyrazoles were designed and synthesized from 1-(4-chlorophenyl)-4,4,4-trifuorobutane-1,3-dione 1. The newly synthesized compounds were investigated in vivo for their anti-inflammatory activities using carrageenan-induced rat paw oedema model. Moreover, they were tested for their inhibitory activity against ovine COX-1 and COX-2 using an in vitro cyclooxygenase (COX) inhibition assay. Some of the new compounds (2f, 6a and 6d) showed a reasonable in vitro COX-2 inhibitory activity, with IC50 value of 0.45 μM and selectivity index of 111.1. A virtual screening was carried out through docking the designed compounds into the COX-2 binding site to predict if these compounds have analogous binding mode to the COX-2 inhibitors. Docking study of the synthesized compounds 2f, 6a and 6d into the active site of COX-2 revealed a similar binding mode to SC-558, a selective COX-2 inhibitor. © 2011 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Elsayed, Magda A.A.
Egypt, Mansoura
Faculty of Pharmacy
Abdel-Aziz, Naglaa I.
Egypt, Mansoura
Mansoura University
Abdel-Aziz, Alaa A.M.
Egypt, Mansoura
Mansoura University
Saudi Arabia, Riyadh
College of Pharmacy
El-Azab, Adel S.
Saudi Arabia, Riyadh
College of Pharmacy
Egypt, Cairo
Faculty of Pharmacy
Asiri, Yousef Abdu
Saudi Arabia, Riyadh
College of Pharmacy
ELTahir, Kamal Eldin Hussein
Saudi Arabia, Riyadh
College of Pharmacy
Statistics
Citations: 143
Authors: 6
Affiliations: 4
Identifiers
Doi:
10.1016/j.bmc.2011.04.027
ISSN:
09680896
e-ISSN:
14643391