Journal of Medicinal Chemistry 1980-05-01

Soft drugs. 3. A new class of anticholinergic agents.

N Bodor, R Woods, C Raper, P Kearney, J J Kaminski

文献索引：J. Med. Chem. 23(5) , 474-80, (1980)

全文：HTML全文

摘要

A new class of antimuscarinic drugs was designed and synthesized. The compounds are "soft" quaternary ammonium esters in which there is only one carbon atom separating the ester oxygen and the quaternary head. The compounds are potent anticholinergics when derived from hindered "umbrella" acids and cholinergics when derivatives of simple aliphatic acids. The more potent anticholinergics have up to 10 times higher acetylcholine antagonist activity than atropine, but they have a much shorter duration of action. The compounds cleave hydrolytically with simultaneous destruction of the quaternary head. The compounds are promising as selective, local agents, particularly as inhibitors of eccrine sweating.

相关化合物

  • α-苯基环戊基乙酸

相关文献：

Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.

2014-09-01

[Bioorg. Med. Chem. 22(17) , 4968-97, (2014)]

Studies on the metabolic clearance of ciclotropium to alpha-phenylciclopentylacetic acid using a new enantiospecific metabolite assay.

1992-11-01

[Arzneimittelforschung 42(11) , 1354-8, (1992)]

Design, pharmacokinetic, and pharmacodynamic evaluation of soft anticholinergics based on tropyl alpha-phenylcyclopentylacetate.

2002-02-01

[Pharmazie 57(2) , 115-21, (2002)]

664. Chemical constitution and sex-hormonal activity: the synthesis of of some 1-cyclopentyl-and 1-cyclohexyl-1: 2-diarylethylenes. Hey DH and Musgrave OC.

[J. Chem. Soc. , 3156-64, (1949)]

更多文献...