Tsuyoshi Busujima

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MGAT2 (monoacylglycerol acyltransferase 2) is expected to be an attractive target for the drug treatment of obesity, diabetes, and other disease. We describe our exploration and structure-activity relationship (SAR) study of 2,3-dihydro-1H-isoindole-5-sulfonamide derivatives. In this study, we identified 29 as an orally available inhibitor of MGAT2 through(More)
Group 3-15 metal chlorides (Lewis acids) were classified on the basis of activity and aldehyde- and aldimine-selectivity in an addition reaction of a silyl enol ether. Based on the experimental results, metal chlorides (Lewis acids) were classified as follows: A, active; B, weak; C, inactive for the activation of the aldehyde and/or aldimines. Groups A and(More)
We previously reported 2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide 2 as on orally available monoacylglycerol acyltransferase 2 (MGAT2) inhibitor which exhibited an in vivo efficacy at an oral dose of 100 mg/kg in a mouse oral lipid tolerance test. Further optimization of compound 2 to improve the intrinsic(More)
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