Letters in Drug Design & Discovery

Author(s): Dhruvin R. Shah, Rahul P. Modh, Dhara V. Desai and Kishor H. Chikhalia

DOI: 10.2174/1570180810666131122003517

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Novel Urea/Thiourea Derivatives of Quinazolin-4(3H)-one: Design, Synthesis, Antimicrobial and Anti-TB Study

Page: [560 - 571] Pages: 12

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Abstract

In an attempt to control multidrug resistant dilemma, a library of quinazolinone based on two novel series was rationalized and synthesized with simple and efficient etiquette. A number of compounds encompass ethyl thioureidic backbone, structurally related to PETT (Phenyl Ethyl Thiazolyl Thiourea) congeners. All the final synthesized compounds were characterized by IR, 1H NMR, 13C NMR, mass and elemental analysis. The newly synthesized compounds were studied for efficacy against several bacteria (Staphylococcus Aureus, Bacillus Cereus, Escherichia Coli, Pseudomonas Aeruginosa, Klebsiella Pneumoniae, Salmonella Typhi, Proteus Vulgaris, Shigella Flexneria) and fungi (Candida Albicans, Aspergillus Niger, Aspergillus Clavatus) using the broth dilution technique. Moreover, these compounds were also screened for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using the BACTEC MGIT method.

Keywords: Antimicrobial, Antimycobacterial, Minimum Inhibitory Concentration, Quinazolinone; Synthesis, Thiourea, Urea.