Abstract
Phthalimide and hydrazine pharmacophores have been demonstrated to be inhibitors of cyclooxygenases (COX) and lipoxygenases (LOX) and to possess a marked analgesic and anti-inflammatory activity. A new group of hybrid analogs of phthalimide and hydrazine (2-(arylmethylideneamino) isoindolines), possessing a variety of substituents (OMe, OH, NO2, Cl, and F) at different positions of the aryl ring, were synthesized and their analgesic and anti-inflammatory effects were evaluated. In vivo screening showed that all the analogs possessed analgesic and anti-inflammatory activity and compounds 10g, 10h and 10e were the most potent as analgesic and compounds 10b, 10c and 10i were the most potent as anti-inflammatory agents.
Keywords: Analgesic, anti-inflammatory, hydrazone, isoindoline, phthalimide.
Current Pharmaceutical Design
Title:Design and Synthesis of 2-(Arylmethylideneamino) Isoindolines as New Potential Analgesic and Anti-Inflammatory Agents: A Molecular Hybridization Approach
Volume: 22 Issue: 37
Author(s): Maryam Iman, Hamed Shafaroodi, Asghar Davood, Masoud Abedini, Pouyan Pishva, Mehrnoush Taherkhani, Ahmad Reza Dehpour and Abbas Shafiee
Affiliation:
Keywords: Analgesic, anti-inflammatory, hydrazone, isoindoline, phthalimide.
Abstract: Phthalimide and hydrazine pharmacophores have been demonstrated to be inhibitors of cyclooxygenases (COX) and lipoxygenases (LOX) and to possess a marked analgesic and anti-inflammatory activity. A new group of hybrid analogs of phthalimide and hydrazine (2-(arylmethylideneamino) isoindolines), possessing a variety of substituents (OMe, OH, NO2, Cl, and F) at different positions of the aryl ring, were synthesized and their analgesic and anti-inflammatory effects were evaluated. In vivo screening showed that all the analogs possessed analgesic and anti-inflammatory activity and compounds 10g, 10h and 10e were the most potent as analgesic and compounds 10b, 10c and 10i were the most potent as anti-inflammatory agents.
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Iman Maryam, Shafaroodi Hamed, Davood Asghar, Abedini Masoud, Pishva Pouyan, Taherkhani Mehrnoush, Dehpour Reza Ahmad and Shafiee Abbas, Design and Synthesis of 2-(Arylmethylideneamino) Isoindolines as New Potential Analgesic and Anti-Inflammatory Agents: A Molecular Hybridization Approach, Current Pharmaceutical Design 2016; 22 (37) . https://dx.doi.org/10.2174/1381612822666160701072127
DOI https://dx.doi.org/10.2174/1381612822666160701072127 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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