Discovery Of A Novel Series Of N Phenylindoline 5 Sulfonamide Shifting the hydrophobic group to the adjacent position followed by introduction of a bicyclic central core to restrict the substituent orientation produced n phenylindoline 5 sulfonamide derivative 10b, which displayed much improved potency, with an ic 50 value of 1.0 nm. this compound also exhibited excellent selectivity (greater than 30,000. Optimization of a novel series of n phenylindoline 5 sulfonamide based acyl coa:monoacylglycerol acyltransferase 2 inhibitors: mitigation of cyp3a4 time dependent inhibition and phototoxic liabilities. bioorganic & medicinal chemistry 2015, 23 (15) , 4544 4560. doi: 10.1016 j.bmc.2015.06.003.
Discovery Of A Novel Series Of N Phenylindoline 5 Sulfonamide We previously reported the discovery of a novel series of n phenylindoline 5 sulfonamide derivatives as potent, selective, and orally bioavailable mgat2 inhibitors, as exemplified by 2 (fig. 1). 13 compound 2 exhibited potent mgat2 inhibitory activity and suppressed the elevation of tg in a mouse oral fat tolerance test (oftt) after oral administration. these attractive profiles motivated us. Abstract. acyl coa:monoacylglycerol acyltransferase 2 (mgat2) has attracted interest as a novel target for the treatment of obesity and metabolic diseases. starting from n phenylbenzenesulfonamide derivative 1 with moderate potency for mgat2 inhibition, we explored an effective location of the hydrophobic group at the 1 position to enhance. Shifting the hydrophobic group to the adjacent position followed by introduction of a bicyclic central core to restrict the substituent orientation produced a n phenylindoline 5 sulfonamide. N (2,4 difluorophenyl) 2,3 dihydro 1h indole 5 sulfonamide (19). to a mixture of compound 18 (6.30 g, 15.35 mmol) in acoet (100 ml) was added 4 m hcl in acoet (15 ml) at rt. the mixture was stirred at rt overnight. the mixture was neutralized with saturated aqueous nahco 3 solution at 0 °c and extracted with acoet. the organic layer was.
Bb55 7888 вђ Chemdiv Building Block N Phenylindoline 5 Sulfonamide Shifting the hydrophobic group to the adjacent position followed by introduction of a bicyclic central core to restrict the substituent orientation produced a n phenylindoline 5 sulfonamide. N (2,4 difluorophenyl) 2,3 dihydro 1h indole 5 sulfonamide (19). to a mixture of compound 18 (6.30 g, 15.35 mmol) in acoet (100 ml) was added 4 m hcl in acoet (15 ml) at rt. the mixture was stirred at rt overnight. the mixture was neutralized with saturated aqueous nahco 3 solution at 0 °c and extracted with acoet. the organic layer was. We previously identified a novel series of n phenylindoline 5 sulfonamide derivatives exemplified by 2 as potent and orally bioavailable mgat2 inhibitors. despite its attractive potency, further assessment revealed that this compound exhibited time dependent inhibition (tdi) of cytochrome p450 3a4 (cyp3a4). Discovery of a novel series of n phenylindoline 5 sulfonamide derivatives as potent, selective, and orally bioavailable acyl coa:monoacylglycerol acyltransferase 2 inhibitors j. med. chem. , 58 ( 2015 ) , pp. 3892 3909.
918473 15 1 N Methyl 2 Oxo N Phenylindoline 5 Sulfonamideењ е ејџгђѓз We previously identified a novel series of n phenylindoline 5 sulfonamide derivatives exemplified by 2 as potent and orally bioavailable mgat2 inhibitors. despite its attractive potency, further assessment revealed that this compound exhibited time dependent inhibition (tdi) of cytochrome p450 3a4 (cyp3a4). Discovery of a novel series of n phenylindoline 5 sulfonamide derivatives as potent, selective, and orally bioavailable acyl coa:monoacylglycerol acyltransferase 2 inhibitors j. med. chem. , 58 ( 2015 ) , pp. 3892 3909.
92245 85 7 N Phenylindoline 5 Sulfonamide Chemscene Llc
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