Studies on Synthesis of Pyrimidine Derivatives and their Pharmacological Evaluation

T A Naik,K H Chikhalia

doi:10.1155/2007/507590

Abstract

1,3,4-Oxadiazoles were associated with broad spectrum of biological activities including antituberculosis, anticonvulsant, anti-inflammatory, insecticidal, antifungal, analgesic and antitumor properties. Morpholine derivatives find their wide spectrum of antimicrobial activity and exhibit anthelmintic, bactericidal and insecticidal activity. Pyrimidine derivatives are also reported to possess antibacterial, antimicrobial, antifungal, anticancer and anticonvulsant activities. Encouraged by this observations we decided to synthesised novel pyrimidine derivatives.

Highlights

The biological significance of the pyrimidine derivatives has led us to the synthesis of substituted pyrimidine
The nitrogen containing fragment may be an amidine, urea, thiourea or guanidine and acetyl acetone serves as an excellent illustrative example in that it readily undergoes reaction with formamidine,[4] guanidin,[5] urea,[6] or thiourea[7] to produce the corresponding 4,6-dimethyl pyrimidine
The results of the compounds synthesized given for antibacterial screening are mentioned in following table along with standard drugs

Summary

Introduction

The biological significance of the pyrimidine derivatives has led us to the synthesis of substituted pyrimidine. 4- CH3·C6H4 4-N(CH3)2·C6H4 2-OH·C6H4 4-OH·C6H4 4-Cl·C6H4 2,4-(Cl)2·C6H3 4-F·C6H4 2-OCH3·C6H4 4-OCH3·C6H4 3,4,5-(OCH3)3·C6H2 To a solution of 2-Morpholino-3-pyridinylic acid-hydrazide (0.1 mole, 22.2 g.), CS2 (0.1 mole, 7.6 ml) and 20% KOH solution (10 ml) in methanol (82 ml) was added and refluxed for eight hours. After the completion of reaction, the resultant mixture was poured in crushed ice. Product was filtered, washed with water and crystallized from ethanol to give white needles of the title compound.

Results

Conclusion