Synthesis,analgesic, anti‐inflammatory and ulcerogenic index activities of novel 2‐methylthio‐3‐substituted‐5,6‐dimethyl thieno [2,3‐d] pyrimidin‐4(3H)‐ones |
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| Authors: | V Alagarsamy D Shankar S Meena K Thirumurugan T Durai Ananda Kumar |
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| Institution: | 1. Medicinal Chemistry Research Laboratory, Dayananda Sagar College of Pharmacy, Kumaraswamy Layout, Bangalore, India;2. Department of Pharmacy (CARISM), SASTRA University, Thirumalaisamudram, Thanjavur, India;3. Department of Pharmaceutical Chemistry, K.M. College of Pharmacy, Madurai, India |
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| Abstract: | A variety of novel 2‐methylthio‐3‐substituted amino‐5,6‐dimethyl thieno 2,3‐d] pyrimidin‐4(3H)‐ones were synthesized by reacting 3‐amino‐2‐methylthio‐5,6‐dimethyl thieno 2,3‐d] pyrimidin‐4(3H)‐one with different aldehydes and ketones. The starting material 3‐amino‐2‐methylthio‐5,6‐dimethyl thieno 2,3‐d] pyrimidin‐4(3H)‐one was synthesized from 2‐amino‐3‐carbethoxy‐4,5‐dimethyl thiophene. The compounds were investigated for their analgesic activity in albino mice, and for their anti‐inflammatory and ulcerogenic index activities in Wistar rats. The compound 2‐(1‐ethylpropylideneamino)‐2‐methylthio‐5,6‐dimethyl thieno 2,3‐d] pyrimidin‐4(3H)‐one (AS2) showed the most potent analgesic activity of the series. It also showed more potent anti‐inflammatory activity when compared to the reference standard, diclofenac sodium. The test compounds showed only mild ulcerogenic potential when compared to aspirin. Drug Dev Res 68:134–142, 2007. © 2007 Wiley‐Liss, Inc. |
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| Keywords: | thienopyrimidine thioureas pyrimidine analgesic anti‐inflammatory albino mice Wistar rats |
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