US 5,204,352 A · Compounds exhibiting anti-parasitic activity and a method for their use

Abstract

Novel compounds are provided which exhibit high levels of anti-parasitic activity, specifically against parasites of the genus Trypanosoma. The compounds are comprised of aryl-substituted quaternary heteroaromatic salts which include a positively charged imidazolium or other heterocyclic ring, a linking group, a phenyl ring, and a polar functional group. The polar functional group is preferably a quanylhydrazone or a heterocyclic hydrazone. A method is also provided for treating the diseases associated with Trypanosoma parasites which comprises administering to infected animals or humans an effective amount of a compound of the present invention.

Claims20

Dependent claims

A compound having the general formula:

##STR82## wherein A represents an optional heterocyclic ring fused to the imidazolium ring wherein the compounds are selected from the group consisting of ##STR83## wherein R.sub.1 is a straight or branched aliphatic group having from one to ten carbon atoms;
R.sub.3 represents CH.sub.3, Br, hydrogen or NO.sub.2 ;
Z represents I, Br, TsO or Cl;
L represents --CH.sub.2 O--, --CH.dbd.CH or a single bond;
and
X represents substituted guanylhydrazone or unsubstituted guanylhydrazone and
Z.crclbar. represents an anion which forms a physiologically acceptable salt with the rest of the compound.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application

07/102,445Filed 29 Sep 1987

Granted

20 Apr 1993

Term ends

Not estimatedThe source records don’t support an estimate.

Classification5 codes

C07D 213/53
Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom: nitrogen atoms
C07D 233/64
Having two double bonds between ring members or between ring members and non-ring members: with substituted hydrocarbon radicals attached to ring…
C07D 471/04
In which the condensed system contains two hetero rings: ortho-condensed systems
C07D 513/04
In which the condensed system contains two hetero rings: ortho-condensed systems

Compounds exhibiting anti-parasitic activity and a method for their use

Life of this patent

Compounds exhibiting anti-parasitic activity and a method for their use

Life of this patent

Abstract

Claims20