Synthesis of pyrimidine incorporated piperazine derivatives and their antimicrobial activity

Thiophene substituted chalcones (1a-e) were cyclised with thiourea in presence of potassium hydroxide to get 4-substituted-6-(thiophen-2-yl)pyrimidine-2-thiols (2a-e) which were then stirred with methyl iodide to obtain 4-substituted-2-(methylsulfanyl)-6-(thiophen-2-yl)pyrimidines (3a-e). Compounds...

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Bibliographic Details
Published in:Indian journal of pharmaceutical sciences 2014-07, Vol.76 (4), p.332-338
Main Authors: Thriveni, K, Padmashali, B, Siddesh, M, Sandeep, C
Format: Article
Language:English
Subjects:
Agreements
Antimicrobial agents
Aqueous solutions
Chemical synthesis
Derivatives
Drugs
Ethanol
Methods
Pharmacology, Experimental
Potassium
Properties
Pyrimidines
Research Paper
Structure-activity relationship (Pharmacology)
Structure-activity relationships
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Summary:Thiophene substituted chalcones (1a-e) were cyclised with thiourea in presence of potassium hydroxide to get 4-substituted-6-(thiophen-2-yl)pyrimidine-2-thiols (2a-e) which were then stirred with methyl iodide to obtain 4-substituted-2-(methylsulfanyl)-6-(thiophen-2-yl)pyrimidines (3a-e). Compounds (3a-e) were refluxed with different N-methylpiperazine and N-phenylpiperazine to afford 4-substituted-2-(4-methylpiperazin-1-yl)-6-(thiophen-2-yl)pyrimidines (4a-e) and 4-substituted-2-(4-phenylpiperazin-1-yl)-6-(thiophen-2-yl)pyrimidines (5a-e). The structures of all the newly synthesised compounds 4b, 4d, 5a and 5b showed good antibacterial activity at 40µg/mlconcentration. Compounds 4a, 4d, 4e, 5c and 5e showed significant antifungal activity at 40 µg/ml concentration compared with standard drugs.
ISSN:0250-474X
1998-3743