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Synthesis, antimicrobial and cytotoxic activity of novel 4-phenoxy and 4-(substitutedamino) pyrazolo [3, 4-d] pyrimidine derivatives

Mohammed Kamal Abd El Hameid, Hala Bakr El-Nassan, Khaled Omar Ahmed

A series of new pyrazolopyrimidines was synthesized. Antimicrobial screening was done for the novel molecules to discover their activity against some test organisms, Staphylococcus aureus (ATCC 25923) (as example for Gram-positive bacteria), Escherichia. coli (ATCC 25922), Enterobacter cloacae (ATCC23048), Klebsiella (ATCC23495), Salmonella typhimurium (as examples for Gram-negative bacteria) and Candida albicans (as example for fungi). The antimicrobial screening results showed that some of these compounds exhibited a significant antimicrobial activity, where, compounds (5c) and (5e) showed the highest antimicrobial activity with MIC of 16 µg/mL,whilst, compounds (4d), (5g) and (5h) displayed antifungal activity against Candida albicans. Besides, eight of the newly synthesized compounds were selected by National cancer Institute NCI (U.S.A) to be screened for their cytotoxic activity. The test compounds showed limited cytotoxic activity. The cytotoxicity results suggested that substitution at position 4 of pyrazolo [3, 4-d] pyrimidine with aryloxy or substitutedanilino moietieswas preferred to aralkylaminomoiety. Besides, introduction of small lipophilic group likemethyl group in the para position of aryloxy or anilino moiety enhanced the cytotoxic activity. The results of cytotoxic screening were in good agreement with the calculated log P of the test compounds.