Department of Chemistry, Université du Québec à Montréal, PO Box 8888, Succ. Centre-Ville, Montréal, QC H3C 3P8, Canada.
Department of Chemistry, Université du Québec à Montréal, PO Box 8888, Succ. Centre-Ville, Montréal, QC H3C 3P8, Canada; INRS - Institut Armand-Frappier, Université du Québec, 531 Boul. des Prairies, Laval, QC H7V 1B7, Canada.
Drug Discov Today. 2021 Sep;26(9):2124-2137. doi: 10.1016/j.drudis.2021.02.025. Epub 2021 Mar 3.
Glycoconjugates are involved in several pathological processes. Glycomimetics that can favorably emulate complex carbohydrate structures, while competing with natural ligands as inhibitors, are gaining considerable attention owing to their improved hydrolytic stability, binding affinity, and pharmacokinetic (PK) properties. Of particular interest are the families of α-d-mannopyranoside analogs, which can be used as inhibitors against adherent invasive Escherichia coli infections. Bacterial resistance to modern antibiotics triggers the search for new alternative antibacterial strategies that are less susceptible to acquiring resistance. In this review, we highlight recent progress in the chemical syntheses of this family of compounds, one of which having reached clinical trials against Crohn's disease (CD).
糖缀合物参与多种病理过程。糖模拟物可以有利地模拟复杂的碳水化合物结构，同时作为抑制剂与天然配体竞争，由于其提高的水解稳定性、结合亲和力和药代动力学 (PK) 性质而受到极大关注。特别有趣的是 α-d-甘露吡喃糖苷类似物家族，它们可用作针对黏附侵袭性大肠杆菌感染的抑制剂。细菌对现代抗生素的耐药性促使人们寻找新的、不易产生耐药性的替代抗菌策略。在这篇综述中，我们强调了该化合物家族的化学合成的最新进展，其中一种化合物已进入针对克罗恩病 (CD) 的临床试验。
