RESUMEN
Synthesis of some new 2-(N-tosyl- or N-phthalylaminoacyl or free aminoacyl or N-tosyldipeptidyl- or N-phthalyldipeptidyl)aminopyrazine derivatives (II-XXX) are described. All 2-(aminoacyl)aminopyrazines (XIV-XVIII) have been found to be biologically active against a number of microorganism.
Asunto(s)
Antibacterianos/síntesis química , Pirazinas/síntesis química , Bacterias/efectos de los fármacos , Fenómenos Químicos , Química , Pirazinas/farmacologíaRESUMEN
3-Nitro-9-(N-phthalyl- and N-tosylaminoacyl)carbazoles (II-XI) have been synthesized by the action of 3-nitro-9H-carbazole (I) on N-phthalyl- or N-tosylamino acid in THF-Et3N medium using the DCC method. Treatment of the 3-nitro derivatives (II-XI) with Sn/HCl gave the corresponding 3-amino-9-(N-phthalyl- or N-tosylaminoacyl)carbazoles (XII-XIX). Hydrazinolysis of the N-phthalylcarbazoles derivatives (III-VII) in ethanol gave the corresponding 3-nitro-9-(aminoacyl) carbazoles (XX-XXIII). Compounds (II-XI and XXI, XXII) were found to be active against some microorganisms.
Asunto(s)
Carbazoles/síntesis química , Bacterias/efectos de los fármacos , Carbazoles/análisis , Carbazoles/farmacología , Fenómenos Químicos , Química Física , Pruebas de Sensibilidad MicrobianaRESUMEN
Synthesis of a series of N-(2-acetylaminothiazole-5-sulphonyl) amino acids (II-VI) and some of their corresponding methyl esters (VII-XI) is described. Coupling of N-tosyl-or N-phthalylamino acid with 2-amino-2-thiazoline using the DCC method furnishes 2-(N-tosyl- or N-phthalylamino acyl) amino-2-thiazoline (XII-XXI). Hydrazinolysis of 2-(N-Pht-L-Phe or N-Pht-L-Ala) amino-2-thiazoline in ethanol afforded 2-(L-Phe or L-Ala) amino-2-thiazoline (XXII and XXIII) respectively. Synthesis of the dipeptide 2-(N-Tos-L-Val-L-Leu) amino-2-thiazoline (XXIV) has been achieved employing the azide method. Sixteen thiazole- and thiazoline-amino acid derivatives were found to be active against a number of microorganisms.
