Tomohiko Kinoshita

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Several p38 MAPK inhibitors have been shown to effectively block the production of cytokines such as IL-1β, TNFα, and IL-6. Inhibitors of p38 MAP kinase therefore have significant therapeutic potential for the treatment of autoimmune disease. Compound 2a was identified as a potent TNFα production inhibitor in vitro but suffered from poor oral(More)
Asymmetric intermolecular conjugate addition of α-amino acid derivatives with 4 via memory of chirality has been developed. The reactions proceeded in up to 98% ee with retention of configuration at the newly formed tetrasubstituted carbon center when R = Me. The product (R = Me) was transformed into manzacidin A.
An aminoquinazoline series targeting the essential bacterial enzyme GlmU (uridyltransferase) were previously reported (Biochem. J.2012, 446, 405). In this study, we further explored SAR through a combination of traditional medicinal chemistry and structure-based drug design, resulting in a novel scaffold (benzamide) with selectivity against protein kinases.(More)
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