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omega-(Imidazol-4-yl)alkane-1-sulfonamides: a new series of potent histamine H(3) receptor antagonists.
Authors:Matthew J Tozer  Ildiko M Buck  Tracey Cooke  S Barret Kalindjian  Michael J Pether  Katherine I M Steel
Institution:The James Black Foundation, 68 Half Moon Lane, Dulwich, SE24 9JE, London, UK. matt.tozer@medivir.com
Abstract:omega-(1H-Imidazol-4-yl)alkane-1-sulfonamides were prepared and found to be potent histamine H(3) receptor antagonists. High receptor affinity and a low difference in the data between the bioassays were achieved with 5-(1H-imidazol-4-yl)pentane-1-sulfonic acid 4-chlorobenzylamide (16). Good in vitro profiles were also obtained for 2-hydroxysulfonamide and vinylsulfonamide analogues. This complements and completes the existing set of imidazole-based sulfonamides and sulfamides.
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