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ID: ALA5241134

Journal: Bioorg Med Chem Lett

Title: Discovery of orally bioavailable inhibitors of MALT1 with in vivo activity for psoriasis.

Authors: Nunettsu Asaba K, Okimura K, Adachi Y, Tokumaru K, Goto Y, Fujii S, Watanabe A, Sakai C, Sakurada E, Amikura K, Aoki T.

Abstract: We report the design, synthesis, and biological activity of a series of compounds that exhibit potent mucosa-associated lymphoid tissue lymphoma translocation 1 (MALT1) inhibition. Structural transformation of the substructures of a starting compound gave amidomethyl derivatives and sulfonylguanidine derivatives that exhibited potent inhibition of MALT1. Compound 37 had good oral bioavailability and showed anti-psoriatic activity in an imiquimod-induced psoriasis mouse model after oral administration.

CiteXplore: 36720321

DOI: 10.1016/j.bmcl.2023.129155