Abstract
A variety of novel 2-mercapto-3-(substituted amino)-5,6,7,8-tetrahydro-3H-benzo(4,5) thieno(2,3-d)pyrimidin-4-ones were synthesized by reacting 3-Amino-2-mercapto-5,6,7,8- tetrahydro-3H-benzo(4,5)thieno(2,3-d)pyrimidin-4-one with different aldehydes and ketones; the starting material 3-amino-2-mercapto-5,6,7,8-tetrahydro-3H-benzo(4,5)thieno(2,3-d)pyrimidin- 4-one was synthesized from 2-amino-3-carbethoxy-4,5,6,7-tetrahydrobenzo 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, compounds AS1, AS2 and AS3 showed more potent analgesic activity. The compound AS3 showed more potent anti-inflammatory activity when compared to the reference standard diclofenac sodium. Interestingly the test compounds showed only mild ulcerogenic potential when compared to aspirin.
Highlights
Quinazolines and condensed quinazolines are found to possess potent analgesic and antiinflammatory activities
On our going medicinal chemistry research programme we have found that quinazolines and condensed quinazolines exhibit potent central nervous system (CNS) activities like analgesic, anti-inflammatory1 and anticonvulsant
The title compounds were synthesized by reacting 3-amino-2-mercapto-5,6,7,8-tetrahydro-3Hbenzo[4,5]thieno[2,3-d]pyrimidin-4-one with a variety of aldehydes and ketones
Summary
Synthesis of some novel 2-mercapto-3-(substituted amino)5,6,7,8-tetrahydro-3H-benzo[4,5]thieno[2,3-d]pyrimidin-4-ones as analgesic and anti-inflammatory agents.
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