Synthesis And Biological Activity Of Some New 4-(Aminoacyl) Aminopyridines And 2-(Aminoacyl) Aminopyrimidine Derivatives

Abstract

The synthesis of 4-(N-Tos and N-Pht-aminoacyI) aminopyridines (III - XIV) and 2-(N-Pht-aminoacyl)-aminopyriniidines (XV-XXIV) has been achieved employing the acid chloride and carbodiimide methods. Hydrazinolysis of 4-(N-Pht-Gly or -B-Ala-) aminopyridines or 2-(N-Pht-L-Phe- or -B-Ala-) aminopyrimidines in ethanol afforded the desired 4-(GIy- or B-Ala) aminopyridines (XXV - XXVI) and 2-(L-Phe- or B-Ala) aminopyrimidines (XXVII - XXVIII) respectively. 4-(N-Pht- or N-Tos-dipeptidyl) aminopyridines (XXIX - XXXVI) are synthesized via the DCC method and 2-(N-Tos-L-Val-L-Leu) aminopyrimidine (XXXVII) via the azide method. The amino acid derivatives (XV, XVI, XXI, XXII, XXV, XXVI, XXVIII) and the dipeptide (XXXVII) are found to be active against a number of microorganisms.