Pfizer Corporation

Stephen J Ray

Kenneth Richardson

The invention provides antifungal compounds of the formula: ##STR1## and pharmaceutical salts thereof, wherein

Triazole antifungal agents

An antifungal agent of the formula: ##STR1## wherein R is phenyl group which may be substituted by 1 to 3 substituents each independently selected from halo and CF.sub.3 ; R.sup.1 is either (a) a phenyl group substituted by a group of the formula --N.dbd.CH--N(C.sub.1 -C.sub.4 alkyl).sub.2, ##STR2## or (b) a 5- or 6-membered aromatic heterocyclic group which may be benzo-fused and substituted by 1 or 2 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl and halo-(C.sub.1 or C.sub.2 alkyl), said heterocyclic group being attached to the nitrogen atom of the piperazine ring by a carbon atom;

2-aryl-3-(substituted piperazinyl)-1-(1H-1,2,4-triazolyl)propanol-2-ol

Compounds of the formula: ##STR1## and pharmaceutically-acceptable acid addition salts thereof, wherein R.sup.1 is at the 3 or 4 position and is phenyl or phenyl substituted by halo, (C.sub.1 -C.sub.4)alkoxy, or (C.sub.2 -C.sub.5)alkoxycarbonyl; R.sup.2 is at the 2 or 7 position and is a group of the formula X(CH.sub.2).sub.n NR.sup.3 R.sup.4 where X is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --; n is 1, 2, 3 or 4; and each of R.sup.3 and R.sup.4 is hydrogen or (C.sub.1 -C.sub.4)alkyl, or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a 1-pyrrolidinyl or piperidino group; Y is hydrogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy or (C.sub.2 -C.sub.5)-alkoxycarbonyl at the 4, 5, 6 or 7 position; and wherein R.sup.2 is at the 2-position, R.sup.1 is at the 3- or 4-position, or alternatively when R.sup.2 is at the 7-position, R.sup.1 is at the 3-position; are useful for the treatment of diarrhea in humans and animals.

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Deal, United Kingdom

Stephen J Ray