Design, Synthesis, Antiviral and Cytotoxicity Studies of Some 2-Phenyl-3-substituted quinazolin-4-(3H)-ones

Abstract

A series of novel 2-phenyl-3-substituted quinazolin-4-(3H)-one derivatives were synthesized and screened for antiviral activity against panel of human pathogenic viruses. The structures of the synthesized compounds were characterized by means of their IR, ¹H NMR data. The anti HIV activities of the new compounds were screened in vitro antiviral activity against replication of HIV-1 (IIIB) and HIV-2 (ROD) in MT-4 cells using AZT-as standard. All the compounds displayed cytostatic properties in T-lymphocytes MT-4 cells. The compound 4-[(4-oxo-2- phenylquinazolin-3(4H)-yl-amino]methyl amino benzoic acid (QPAB) (CC₅₀ = 11.90 μg/mL) was found to be more toxic in this series. 2-Amino-3-phenylquinazolin-4(3H)-one (BN) exhibited antiviral activity against Herpes Simplex virus-1,2 and vaccinia virus in HEL cells at the concentration of 10 and 12 μg/mL, whereas cytotoxicity was found to be 100 μg/mL (SI = 10). Among these compounds, compounds (QIS and QMB) exhibited antiviral activity against vesicular stomatitis virus in HeLa cells at the concentration of 12 μg/mL, whereas cytotoxicity was found to be 100 μg/mL (SI = 9).