Synthesis and Biological Activity of Some New 4-(Aminoacyl)- Aminopyridines and 2-(Aminoacyl) Aminopyrimidine Derivatives PDF

Keywords

Aminopyrimidine, Aminopyridines, synthesis

Abstract

The synthesis of 4-(N-Tos- and N-Pht-aminoacyl)- aminopyridines (III-XIV) and 2-(N-Pht-aminoacyl)- aminopyrimidines (XV-XXIV) has been achieved employing the acid chloride and carbodiimide methods. Hydrazinolysis of 4-(N-Pht- Gly-or- Beta-Ala-) aminopyridines or 2-(N-Pht-L-Phe-or-Beta-Ala-) aminopyrimidines in ethanol afforded the desired 4-(Gly-or-Beta-Ala) aminopyridines (XXV-XXVI) amd 2-(L-Phe-or-Beta-Ala) aminopyrimidines (XXVII-XXVIII) respectively. 4-(N-Pht-or-N-Tos-dipeptidyl) aminopyridines (XXIX-XXXVI) are synthesised via the DCC method, and 2-(N-Tos-L-Val-L-Leu) aminopyrimidine (XXXVIII) via the azide method. The 2-(aminoacyl) aminopyrimidine derivatives (XV, XVI, XXI, XXII, XXVIII and XXXVII) and the 4-(aminoacyl)-aminopyridine and derivatives (XXV, XXVI) are found to possess various antimicrobial and antiungal properties (as compared to I & II) towards diferent microorganisms with MIC values ranging from 5 to 250 micrograms/ml.