synthesis and biological activity of peptide derivatives of iodoquinazolinonesnitroimidazoles的合成和生物活性肽iodoquinazolinonesnitroimidazoles的衍生品.pdf

Molecules 2008, 13, 958-976 molecules ISSN 1420-3049 © 2008 by MDPI /molecules Full Paper Synthesis and Biological Activity of Peptide Derivatives of Iodoquinazolinones/Nitroimidazoles Rajiv Dahiya*, Anil Kumar and Rakesh Yadav Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura-281001 (UP), India *Author to whom correspondence should be addressed; Tel.: +91-9897417450; +91-565-6531680; E-mail: rajivdahiya04@yahoo.co.in or rajivdahiya77@ Received: 3 April 2008; in revised form: 18 April 2008 / Accepted: 19 April 2008 / Published: 24 April 2008 Abstract: Two substituted quinazolinyl/imidazolyl-salicylic acids 5, 6 were synthesized by the reaction of 6-iodo-2-methylbenzoxazin-4-one/5-nitroimidazole with 5-aminosalicylic acid (5-ASA). Coupling of compounds 5 and 6 with different amino acid ester hydrochlorides, dipeptide and tripeptide methyl esters yielded novel quinazolino/imidazolopeptide derivatives 5a-f and 6a-g. The chemical structures of all newly synthesized compounds were confirmed by means of FT-IR, 1H- and 13C-NMR, MS and elemental analysis. Selected peptide ester derivatives were further hydrolyzed by using lithium hydroxide (LiOH) to afford the corresponding acid derivatives 5b -d and 6e -g . a a a a All peptide derivatives were assayed for antimicrobial and anthelmintic activities against