New tilomisole-based benzimidazothiazole derivatives as anti-inflammatory agents: Synthesis, in vivo, in vitro evaluation, and in silico studies

Autor:	Sara A. Darwish, Mohamed M. El-Kerdawy, Ahmad R. Elsheakh, Rehab S. Abdelrahman, Moataz A. Shaldam, Hatem A. Abdel-Aziz, Ghada S. Hassan, Mariam A. Ghaly
Rok vydání:	2021
Předmět:	Cyclooxygenase 2 Inhibitors Molecular Structure Organic Chemistry Anti-Inflammatory Agents Non-Steroidal Anti-Inflammatory Agents Biochemistry Rats Molecular Docking Simulation Structure-Activity Relationship Celecoxib Cyclooxygenase 2 Drug Discovery Animals Edema Benzimidazoles Molecular Biology
Zdroj:	Bioorganic chemistry. 120
ISSN:	1090-2120
Popis:	New tilomisole-based benzimidazothiazole derivatives were designed and synthesized in this work. Their anti-inflammatory activity was assessed through the in vivo carrageenan rat paw edema model, and the in vitro COX inhibition assay. Compounds 13, 20, 30, 40, 43, and 46 demonstrated values of inhibition of induced edema in the in vivo assay comparable to celecoxib. All the synthesized compounds expressed their activity on COX-2 enzyme more than COX-1, proving their advantageous selectivity. In addition, compounds 13, 16, 20, 25, and 46 displayed lower IC
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::328f35f227b0dbe4f3589fc1d086e34c https://pubmed.ncbi.nlm.nih.gov/35121552 Zobrazit plný text záznamu Full Text from ScienceDirect