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Synthesis, analgesic, anti‐inflammatory and ulcerogenic index activities of novel 2‐methylthio‐3‐substituted‐5,6‐dimethyl thieno [2,3‐ d ] pyrimidin‐4(3 H )‐ones
Author(s) -
Alagarsamy V.,
Shankar D.,
Meena S.,
Thirumurugan K.,
Ananda Kumar T. Durai
Publication year - 2007
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.20171
Subject(s) - diclofenac sodium , chemistry , analgesic , aspirin , anti inflammatory , ulcer index , stereochemistry , pharmacology , biochemistry , chromatography , medicine , stomach , gastric mucosa
A variety of novel 2‐methylthio‐3‐substituted amino‐5,6‐dimethyl thieno [2,3‐ d ] pyrimidin‐4(3 H )‐ones were synthesized by reacting 3‐amino‐2‐methylthio‐5,6‐dimethyl thieno [2,3‐ d ] pyrimidin‐4(3 H )‐one with different aldehydes and ketones. The starting material 3‐amino‐2‐methylthio‐5,6‐dimethyl thieno [2,3‐ d ] pyrimidin‐4(3 H )‐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(3 H )‐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.