Title of article :
Bioisosteric replacement of dihydropyrazole of 4S-(−)-3-(4-chlorophenyl)-N-methyl-N′-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole
Author/Authors :
Brijesh Kumar Srivastava، نويسنده , , Rina Soni، نويسنده , , Amit Joharapurkar، نويسنده , , Kalapatapu V.V.M. Sairam، نويسنده , , Jayendra Z. Patel، نويسنده , , Amitgiri Goswami، نويسنده , , Sandeep A. Shedage، نويسنده , , Sidhartha S. Kar، نويسنده , , Rahul P. Salunke، نويسنده , , Shivaji B. Gugale، نويسنده , , Amol Dhawas، نويسنده , , Pravin Kadam، نويسنده , , Bhupendra Mishra، نويسنده , , Nisha Sadhwani، نويسنده , , Vishal B. Unadkat، نويسنده , , Prasenjit Mitra، نويسنده , , Mukul R. Jain، نويسنده , , Pankaj R. Patel، نويسنده ,
Abstract :
Design, synthesis and conformational analysis of few imidazole and oxazole as bioisosters of 4S-(−)-3-(4-chlorophenyl)-N-methyl-N′-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) 2 is reported. Computer assisted conformational analysis gave a direct clue for the loss of CB1 antagonistic activity of the ligands without a fine docking simulation for the homology model.
Keywords :
Bioisosteric replacement , CB1 receptor antagonist , imidazole , oxazole , homology model , Conformational analysis
