Molecules, Vol. 28, Pages 3416: Identification of Novel Cyclooxygenase-1 Selective Inhibitors of Thiadiazole-Based Scaffold as Potent Anti-Inflammatory Agents with Safety Gastric and Cytotoxic Profile

Molecules, Vol. 28, Pages 3416: Identification of Novel Cyclooxygenase-1 Selective Inhibitors of Thiadiazole-Based Scaffold as Potent Anti-Inflammatory Agents with Safety Gastric and Cytotoxic Profile Molecules doi: 10.3390/molecules28083416 Authors: Michelyne Haroun Maria Fesatidou Anthi Petrou Christophe Tratrat Panagiotis Zagaliotis Antonis Gavalas Katharigatta N. Venugopala Hafedh Kochkar Promise M. Emeka Nancy S. Younis Dalia Ahmed Elmaghraby Mervt M. Almostafa Muhammad Shahzad Chohan Ioannis Vizirianakis Aliki Papadimitriou-Tsantarliotou Athina Geronikaki Major obstacles faced by the use of nonsteroidal anti-inflammatory drugs (NSAID) are their gastrointestinal toxicity induced by non-selective inhibition of both cyclooxygenases (COX) 1 and 2 and their cardiotoxicity associated with a certain class of COX-2 selective inhibitors. Recent studies have demonstrated that selective COX-1 and COX-2 inhibition generates compounds with no gastric damage. The aim of the current study is to develop novel anti-inflammatory agents with a better gastric profile. In our previous paper, we investigated the anti-inflammatory activity of 4-methylthiazole-based thiazolidinones. Thus, based on these observations, herein we report the evaluation of anti-inflammatory activity, drug action, ulcerogenicity and cytotoxicity of a series of 5-adamantylthiadiazole-based thiazolidinone derivatives. The in vivo anti-inflammatory activity revealed that the compou...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research