Bioorganic & Medicinal Chemistry Letters 2010-09-01

S-benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase.

Kenji Matsuno, Kazushige Takai, Yoshinobu Isaka, Yuka Unno, Masayuki Sato, Osamu Takikawa, Akira Asai

Index: Bioorg. Med. Chem. Lett. 20 , 5126-9, (2010)

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Abstract

S-benzylisothiourea 3a was discovered by its ability to inhibit indoleamine-2,3-dioxygenase (IDO) in our screening program. Subsequent optimization of the initial hit 3a lead to the identification of sub-muM inhibitors 3r and 10h, both of which suppressed kynurenine production in A431 cells. Synthesis and structure-activity relationship of S-benzylisothiourea analogues as small-molecule inhibitors of IDO are described.Copyright 2010 Elsevier Ltd. All rights reserved.