Synthesis of 2-mercapto-3-substituted-5,6-dimethylthieno[2,3-d] pyrimidin-4(3H)-ones as new analgesic, anti-inflammatory agents.
A new series of 2-mercapto-3-substituted-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-ones were synthesised by reacting 3-amino-2-mercapto-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one with different aldehydes and ketones. The starting material 3-amino-2-mercapto-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one was synthesised from 2-amino-3-carbethoxy-4,5-dimethyl thiophene by a novel innovative route. The title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic index activities. While the test compounds exhibited significant activity, among these compound AS1 showed more potent analgesic and anti-inflammatory activities and the compound AS3 showed equipotent analgesic and anti-inflammatory activities when compared to the reference standard diclofenac sodium.
Alagarsamy
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Medicinal Chemistry Research Laboratory, Dayananda Sagar College of Pharmacy, Bangalore 560 078, India. drvalagarsamy@gmail.com
Vijayakumar
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Raja Solomon
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D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D010147:Pain Measurement; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013276:Stomach Ulcer / Q000139:chemically induced; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011744:Pyrimidinones; D013438:Sulfhydryl Compounds; D013876:Thiophenes