Compounds with antiparasitic activity and medicines containing same
申请人:Vial Henri
公开号:US20050176819A1
公开(公告)日:2005-08-11
The invention relates to compounds having an anti-parasitic, in particular antimalarial activity, characterized in that they correspond to general formula (I)
Applications in particular as compounds with anti-parasitic activity.
2-Mercaptoacetamidines as gastric antisecretory agents
作者:William A. Bolhofer、Charles N. Habecker、Adolph M. Pietruszkiewicz、Mary Lou Torchiana、Henry I. Jacoby、Clement A. Stone
DOI:10.1021/jm00189a015
日期:1979.3
A series of N-substituted 2-mercaptoacetamidines was synthesized and evaluated for gastricantisecretory activity in dogs stimulated with gastrin tetrapeptide. The most potent analogues showed 80--95% inhibition of acid secretion after an oral dose of 8 mg/kg. Thus, these compounds represent a new structural type having significant antisecretory activity. Disulfides had essentially the same antisecretory
The synthesis, antibacterial activity and DHP-susceptibility of a series of novel carbapenems, directly linked with heterocyclic moiety are described. Especially, the compounds linked pyrrolidine-carbapenem exhibited to have a good antibacterial activity against Staphylococcus aureus (MRSA) as well as Pseudomonas aeruginosa to maintain a good stability towards DHP-I.
Arylheteroalkylamine derivatives and their use as inhibitors of nitric oxide synthase
申请人:Cheshire David
公开号:US20050143379A1
公开(公告)日:2005-06-30
There are provided novel compounds of formula (I), wherein R
1
, R
2
, R
3
, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.
In the frame of the development of bis-cationic choline analogs, the RSA of bis-N-alkylamidines were studied and a new series of reverse-benzamidine derivatives was designed. Contrary to the lipophilicity, the basicity of alkylamidine compounds directly influences their antimalarial potencies. (C) 2010 Elsevier Ltd. All rights reserved.