Title of article :
Synthesis, Antiviral and Cytotoxic Activities of Some Novel 2, 3-Disubstituted Quinazolin-4(3H)-Ones
Author/Authors :
selvam, P. Arulmigu Kalasalingam College of Pharmacy, India , Chennama, B. Perouar College of Pharmaceutical Science for Grils, India , Murugesh, N. Institue of Pharmacology - Madurai Medical college, India , Chandramohan, M. Bahar Ratna Kamarajar Liver Hospital and Research Center, India , Clerco, E.D.E Katholieke Universiteit - Rega Institue for Medical Research, Belgium , Pannecouque, C. Katholieke Universiteit - Rega Institue for Medical Research, Belgium
Abstract :
2-substituted benzoxazin-4-ones were condensed with trimethoprim and pyrimethamine to form the 2, 3-disubstituted quinazolin-4(3H)-ones. Their chemical structure was elucidated by means of spectral (FT-IR, IH-NMR, MS) and elemental analysis. The antiviral activity and cytotoxicity of the compounds were tested in HeLa cells (Vesicular stomatitis virus and Respiratory syncytial virus), HEL cells (Herpes simplex- l and -2), Vero cells(Parainfluenza-3 , Reovirus-l , Sindbis virus, Coxsackie virus B4 and Punta Toro Virus) and MT-4 cells (HIV-l and 2) cell cultures. Among the new derivatives evaluated, 3-[4-amino5(4-chlorophenyl)-6-ethylpyrimidin-2-yl ]-2-ethyl/phenyl-quinazolin-4(3H)-one (5b andSa) exhibited some activity with an MIC of 9.6 ug/ml, against Parainfluenza-3 virus, Reo-lvirus and Punta Toro virus in Vero cells. Compounds 5a, Sb and 5c also displayed markedcytostatic activity in lymphocyte (MT-4) cells. They were not active against HIV-l or -2 atnon-cytostatic concentrations.
Keywords :
Quinazolin , 4(3H) , one , Trimethoprim , Pyrimethamine , anti , HIV activity
Journal title :
Quarterly Journal of Applied Chemical Research (JACR)
Journal title :
Quarterly Journal of Applied Chemical Research (JACR)