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• W2077335457 abstract "A novel class of lymphocyte function-associated antigen-1 (LFA-1) inhibitors is described. Discovered during the process to improve the physicochemical and metabolic properties of BIRT377 (1, Figure 1), a previously reported hydantoin-based LFA-1 inhibitor, these compounds are characterized by an imidazole-based 5,5-bicyclic scaffold, the 1,3,3-trisubstituted 1H-imidazo[1,2-α]imidazol-2-one (i.e. structure 3). The structure−activity relationship (SAR) shows that electron−withdrawing groups at C5 on the imidazole ring benefit potency and that oxygen-containing functional groups attached to a C5-sulfonyl or sulfonamide group further improve potency. This latter gain in potency is attributed to the interaction(s) of the functionalized sulfonyl/sulfonamide groups with the protein, likely polar−polar in nature, as suggested by SAR data. X-ray studies revealed that these bicyclic inhibitors bind to the I-domain of LFA-1 in a pattern similar to that of compound 1." @default.
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• W2077335457 date "2004-09-29" @default.
• W2077335457 modified "2023-10-10" @default.
• W2077335457 title "Second-Generation Lymphocyte Function-Associated Antigen-1 Inhibitors: 1<i>H</i>-Imidazo[1,2-α]imidazol-2-one Derivatives" @default.
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• W2077335457 doi "https://doi.org/10.1021/jm049657b" @default.
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