- Synthesis and Biological Activity of 2,6-disubstituted 3-Aryl-4(3H)-pyrimidones as Potential CNS Agents
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The reaction of N-arylamidines (III) with appropriate 2-alkynoic ester gives 2,6-disubstituted 3-aryl-4(3H)-pyrimidones (IV) in one step except in the reaction of N-(2-trifluoromethylphenyl/biphenyl)-S-methylisothiourea with ethyl propiolate, where the required pyrimidones (IVa17/IVa20) along with the adduct (Va/Vb) have been isolated; these adducts on cyclisation yield the corresponding pyrimidinones (IVa17/IVa20). 2,3,6-Triphenyl-4(3H)-pyrimidone (IVh1) on treatment with P2S5 furnishes the corresponding thione (VI).Some of these compounds have shown significant central muscle relaxant, hypnotic, anticonvulsant, CNS depressant, antiinflammatory and diuretic activities.
- Gupta, K. A.,Saxena, Anil K.,Jain, Padam C.,Dua, P. R.,Prasad, C. R.,Anand, Nitya
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p. 789 - 794
(2007/10/02)
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- Synthesis & Pharmacological Evaluation of Ethyl 3-Substituted-phenyl-2-methylmercapto/ phenyl/ methyl-4(3H)-pyrimidone-5-carboxylates
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A number of ethyl 3-substituted-phenyl-2-methylmercapto/ phenyl/ methyl-4(3H)-pyrimidone-5-carboxylates (V) have been prepared by the reaction of amidines (III) with diethyl ethoxymethylenemalonate.In order to confirm the structure (V), ethyl 3-(2'-methylphenyl)-2-methylmercapto-4(3H)pyrimidone-5-carboxylate (103) has been transformed into the earlier synthesised 3-(2'-methylphenyl)-2-methylmercapto-4(3H)-pyrimidone (115) by decarboxylation of 3-(2'-methylphenyl)-2-methylmercapto-4(3H)-pyrimidone-5-carboxylic acid (114), obtained by the alkaline hydrolysis of 103.Someof these compounds have shown antiinflammatory, diuretic and antipassive cutaneous anaphylaxis activities.
- Gupta, K. A.,Saxena, Anil K.,Jain, Padam C.
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p. 228 - 233
(2007/10/02)
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