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

作者：Saravanan Sakthi^*; Selvam Periyasamy; Lakra Dhani Ram; De Clercq E

来源：Asian Journal of Chemistry, 2011, 23(1): 260-264.

• Cytotoxieity
• Antiviral

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, (1)H 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-Iymphocytes MT-4 cells. The compound 4-[(4-oxo-2-phenylquinazolin-3(4H)-yl-amino]methyl amino benzoic acid (QPAB) (CC(50) = 11.90 mu g/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 mu g/mL, whereas cytotoxicity was found to be 100 mu g/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 mu g/mL, whereas cytotoxicity was found to be 100 mu g/mL (SI = 9).

• 出版日期2011-1