title: Synthesis and evaluation of new carbonic anhydrase inhibitors.
abstract: A series of new sulfamide derivatives have been synthesized, their structures were confirmed by (1)H NMR and ESI-MS. Some target compounds were assessed by the tool of Dock6, and inhibition effects of all the new compounds on carbonic anhydrase II have been investigated. In addition, some compounds have been investigated for their antihypoxic effects in mice. Results indicated that nine target compounds exhibit as effectively as acetazolamide and 10 compounds have more potent inhibition effects on carbonic anhydrase II than acetazolamide. Three of them (I-8, I-18 and I'-3) can prolong markedly the survival time of mice in hypoxia, which are worth carrying out further studies.
authors.affiliation: Department of Environmental Medicine, Institute of Health and Environmental Medicine, Academy of Military Medical Sciences, Tianjin, China. zhonghai.x@163.com
authors.forename: Zhonghai
authors.initials: Z
authors.lastname: Xiao
authors.forename: Ruifeng
authors.initials: R
authors.lastname: Duan
authors.forename: Wenyu
authors.initials: W
authors.lastname: Cui
authors.forename: Yanfang
authors.initials: Y
authors.lastname: Zhang
authors.forename: Shouguo
authors.initials: S
authors.lastname: Zhang
authors.forename: Fangjin
authors.initials: F
authors.lastname: Chen
authors.forename: Yankun
authors.initials: Y
authors.lastname: Zhang
authors.forename: Jiaying
authors.initials: J
authors.lastname: Liu
authors.forename: Dongxiang
authors.initials: D
authors.lastname: Zhang
authors.forename: Yuan
authors.initials: Y
authors.lastname: Meng
authors.forename: Lin
authors.initials: L
authors.lastname: Wang
authors.forename: Hai
authors.initials: H
authors.lastname: Wang
mesh_terms: D000818:Animals; D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors / Q000378:metabolism*; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D000860:Hypoxia / Q000188:drug therapy*; D051379:Mice; D008958:Models, Molecular; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D013449:Sulfonamides; D024402:Carbonic Anhydrase II