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KMID : 0043319900130020142
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Archives of Pharmacal Research
1990 Volume.13 No. 2 p.142 ~ p.146
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Synthesis of Certain Mercapto-and Aminopyrimidine Derivatives as Potential Antimicrobial Agents
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El Kerdawy MM
Eisa HM/El Emam AA/Massoud MA/Nasr MN
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Abstract
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Reaction of ethyl 4-chloro-2-phenylpyrimidine-4-carboxylate (4) with 5-chloro-2-methylthiophenol or 3-aryl-4-phenyl-1,2,4-triazole-5-thiol yielded the corresponding thioethers (5) and (8a, b), respectively. Careful alkaline hydrolysis of (5) yielded the corresponding carboxylic acid (6). Reaction of (4) with p-aminoacetophenone yielded compound (10) which was reacted with certain aromatic aldehydes to afford the alpha, beta-unsaturated ketones (11a-d). Condensation of (11a-d) with malononitrile or phenylhydrazine yielded the 2-amino-3-cyanopyridines (12a-f) or the 2-pyrazolines (13a, b), respectively. Seven representative compounds were tested for their in vitro antimicrobial activity against some pathogenic micro-organisms, some of them were proved to be active.
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