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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 |
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| Authors: | Srivastava Brijesh Kumar Soni Rina Joharapurkar Amit Sairam Kalapatapu V V M Patel Jayendra Z Goswami Amitgiri Shedage Sandeep A Kar Sidhartha S Salunke Rahul P Gugale Shivaji B Dhawas Amol Kadam Pravin Mishra Bhupendra Sadhwani Nisha Unadkat Vishal B Mitra Prasenjit Jain Mukul R Patel Pankaj R |
| Institution: | Department of Medicinal Chemistry, Zydus Research Centre, Cadila Healthcare Ltd, Sarkhej-Bavla N.H. 8A, Moraiya, Ahmedabad 382210, India. brijeshsrivastava@zyduscadila.com |
| 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. |
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