University of California

Scriptgen Pharmaceuticals, Inc.

Zhe Li

Fred Ehrenkranz Cohen

James H McKerrow

George Lommel Kenyon

Mark A Wuonola

Philip Jon Rosenthal

Xiaowu Chen

Rongshi Li

Baoqing Gong

Christine Sun Ring

John D Bradley

C Richard Wobbe

Inhibitors of metazoan parasite proteases

The present invention provides azo and stilbene compounds having the structure: wherein XY is N.dbd.N, CH.dbd.CH, (C.dbd.O)--NH or NH--(C.dbd.O); wherein Z is CR.sub.6 or N; wherein R.sub.1, R.sub.2 and R.sub.5 are independently hydrogen, halogen, NO.sub.2 or CF.sub.3 ; wherein R.sub.3 is hydrogen, halogen, CF.sub.3, aryl or heteroaryl, NO.sub.2 or OCF.sub.3 ; wherein R.sub.4 is hydrogen, halogen, CF.sub.3, aryl or heteroaryl, NO.sub.2 or linear or branched chain alkoxy; wherein R.sub.6 is hydrogen or linear or branched alkyl; wherein R.sub.7 is hydrogen, cyano, hydroxyalkyl, carboxyl, halogen, hydroxyl, formyl, NO.sub.2 or halogen; and wherein R.sub.8 is hydroxyl or substituted or unsubstituted amino; and wherein R.sub.9 and R.sub.10 are independently hydrogen, CN or hydroxyalkyl. Said compounds are useful as antifungal therapeutics, fungicides and fungistats. The present invention also provides methods of inhibiting fungal RNA transcription and treating fungal infections in human and animal subjects and fungal infestations in plants.

Antifungal agents

Disclosed is a method for the inhibition of binding of a ligand to an RNA, the inhibition being mediated by a small organic molecule that binds to the RNA, thereby inhibiting ligand binding. A preferred class of small organic molecules are compounds exemplified by 2,5-Bis[3-(2-N,N-dimethylaminopropylamidino)phenyl]furan.

Small molecule inhibition of RNA/ligand binding

Compositions and methods are disclosed for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at least one compound of formula I

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Malden, MA, United States of America

Zhe Li