SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME NOVEL 1- PHENYL 1-H-PYRAZOLO[3,4-D]PYRIMIDINE DERIVATIVES
AbstractNovel 1- Phenyl 1-H-Pyrazolo[3,4-d]Pyrimidine Derivatives were synthesized from the key intermediate chloro derivative (1).The conversion of chloro derivative(1) into 1,2,4 triazoles, 1,3,4 thiadiazoles and thiazoles was accomplished with the intermediacy of the ester(2) and hydrazide (3). Moreover triazole ring was annelated to the pyrazolopyrmidine core in two step reaction involving reaction with acid hydrazides followed by intramolecular cyclization in boiling glacial acetic acid Majority of the synthesized compounds showed variable antimicrobial activity on the hand tricyclic compounds(9a-b) were deprived from any antimicrobial activity against the tested micro-organisms. The hydrazine carbothioamide derivative (4) and 1,3,4 thiadiazole derivative (6) showed antimicrobial activity against Streptococcus pneumoniae and Bacillis subtilis comparable to ampicillin and a moderate antifungal activity against Asp. Fumigates and C. alb
Article Information
14
3236-44
571
1602
English
Ijpsr
Samy M. Ibrahim, M. Abou-Kul, Moustafa K. Soltan, and Ahmed M. El-Sayed
Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt
mostafakhames3@yahoo.com
19 January, 2015
24 February, 2015
12 March, 2015
10.13040/IJPSR.0975-8232.6(8).3236-44
01 August, 2015
Download