Abstract
During the last few years, condensed thienopyrimidine derivatives have received considerable attention. The therapeutic importance of thienopyrimidines prompted us to synthesize some of spiro(benzothieno[2,3-d]pyrimidine-4-one) derivatives. Some of the novel benzothino-pyrimidine derivatives 3a, 9b, 10b, 11a, 11b, and 11c showed considerable potent anti-inflammatory and analgesic activity of superior G.I.T. safety profile in experimental rats in comparing to indomethacin and tramadol as reference drugs.
Highlights
Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely used therapeutics, primarily used for the treatment of pain and inflammation in arthritis for significant side effects of gastrointestinal lesions, bleeding, and nephrotoxicity
As a part of our continuing program on the synthesis of anti-inflammatory and analgesic compounds as therapeutics agents, we have earlier reported a series of heterocyclic moieties that have anti-inflammatory and analgesic activities [13,14]
This report deals with the synthesis and the pharmacological evaluation of a series of benzothieno[2,3-d]pyrimidines substituted at C-2 with various groups
Summary
Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely used therapeutics, primarily used for the treatment of pain and inflammation in arthritis for significant side effects of gastrointestinal lesions, bleeding, and nephrotoxicity. The discovery of new safer anti-inflammatory drugs represents a challenging goal for such a research area, fused pyrimidines continue to attract considerable attention of researchers because of their great practical usefulness, primarily, due to a very wide spectrum of their biological activities. Thienopyrimidine derivatives are characterized by a very broad spectrum of biological activities, such as anticancer [1,2,3,4], antiviral [5,6], antimicrobial [7,8,9], analgesic and anti-inflammatory [10,11,12,13,14] anticonvulsant [15,16], thymidine phosphorylase inhibitors [17], antiHIV [18], and antihistaminic [19]. The present work is an extension of our ongoing efforts towards the synthesis and evaluation of some new substituted thieno[2,3-d]pyrimidine derivatives as analgesic and anti-inflammatory agents
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