The University of North Carolina at Chapel Hill

Florida State University Research Foundation, Inc.

Other

Duke University

Auburn University

Research Triangle Institute

University of Washington

The University of North Carolina at Charlotte

Richard Ray Tidwell

David W Boykin

W David Wilson

Christine C Dykstra

James E Hall

John R Perfect

Arvind Kumar

Chad F Stephens

Reto Brun

Mohamed A Ismail

Karl Werbovetz

Kenny V Brock

Joachim D Geratz

David A Stringfellow

Arvid Kumar

Reem K Arafa

Kwasi A Ohemeng

Maurice Daniel Givens

Byron L Blagburn

Edward J Dubovi

M Syed Rahmathullah

Dennis Edward Kyle

Max Grogl

Iris Francesconi

Dieter J Geratz

J Dieter Geratz

Bijan P Das

Donald Alan Patrick

Jaroslaw Spychala

Laixing Hu

Svetlana M Bakunova

Stanislav Bakunov

Michael H Gelb

John Robert Gillespie

Ronald I Swanstrom

James C Hudson

Frederick Simmons Buckner

Chad E Stephens

Scott Franzblau

John H Schwab

Katherine B Pryzwansky

Sonia K Anderle

Mariappan Anbazhagan

Daniel Gedder Silva

Sandra Ewald

Dorothy H Wood

The present invention relates to novel compounds that cross the blood-brain barrier and are effective inhibitors of neurological pathogens such as trypanosomes. The invention further relates to the use of these compounds for treating disorders related to trypanosomes and neurological pathogens.

Compounds for treatment of trypanosomes and neurological pathogens and uses thereof

Novel aza analogues of dicationic terphenyl compounds for use in combating microbial infections are described. The compounds include those of Formula (III): wherein one of A, Y, and Zis N; Aris phenylene; and Aris a nitrogen-containing aromatic group. An exemplary compound of Formula (III) is: 

Substituted pyridines as antiparasitic AZA teraryl compounds

Novel aza analogues of dicationic terphenyl compounds for use in combating microbial infections are described. Also described are processes for synthesizing the compounds. The presently disclosed compounds can include those of the formulas:  Land Lare selected from the group consisting of: 

Linear dicationic terphenyls and their aza analogues as antiparasitic agents

Disclosed herein are novel dicationic teraryl compounds and their aza analogues, including compounds of Formula (IIe): wherein p and q are each 0 and each A, Y and Z is CR. An exemplary compound of Formula (IIe) is: Methods for combating microbial infections, such as parasiticspecies, with novel dicationic terphenyl compounds and their aza analogues are included. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues are disclosed along with methods for evaluation of the compounds as potential anti-protozoan agents.

Teraryl components as antiparasitic agents

Novel dicationic 3,5-diphenylisoxazole compounds are described. Synthetic routes to these novel compounds are provided. Several of the compounds displayed in vitro activity versusandcomparable to that of furamidine. A majority of the novel compounds also were less toxic to VERO cells than furamidine.

Synthesis and antiprotozoal activity of dicationic 3,5-diphenylisoxazoles

Novel fused ring dicationic anti-protozoan compounds. Representative protozoan species include but are not limited to(T.b.r.) and. Prodrugs of these compounds can be used as an oral treatment for malaria and human African trypanosomiasis.

Fused ring dicationic anti-protozoan agents and their prodrugs

The present invention relates to novel 2,5-bis{[alkyl (or aryl) imino] aminophenyl}furans and thiophenes of the general formula in which R, R, Rand Rare each independently selected from the group consisting of H, alkyl, alkoxy, halide, and alkylhalide groups; Ris H, alkyl or aryl; Ris H, alkyl, aryl, or NRR, in which Rand Rare each independently selected from the group consisting of H, alkyl and aryl; and X is O, S or NR, in which Ris H or alkyl, and to the use of such compounds.

Synthesis and antimicrobial activity of novel dicationic 'reversed amidines'

Novel dicationic bichalcophene compounds are described. The presently disclosed novel dicationic bichalcophene compounds exhibit in vitro activity versus, orcomparable to that of pentamidine and furamidine. Some of the novel dicationic bichalcophene compounds displayed good activity in vivo in a murine model of ainfection.

Bichalcophenes and their prodrugs as antiprotozoal agents

A method for treating a microbial infection, including an infection from a protozoan pathogen, such asand, in a subject in need thereof by administering to the subject an effective amount of a dicationic imidazopyridine compound or a dicationic tetrahydro-imidazopyridine compound. Processes for synthesizing dicationic imidazopyridines and dicationic tetrahydro-imidazopyridines and the novel dicationic imidazopyridine and dicationic tetrahydro-imidazopyridine compounds themselves.

Dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines as antiprotozoal agents

A method of treating ainfection in a subject in need thereof by administering to the subject an effective amount of a cationic substituted benzofuran compound. Methods of treating microbial infections, including infections from protozoan pathogens, such as, a, and, and fungal pathogens, such as, and, in a subject in need thereof by administering to the subject an effective amount of a cationic substituted benzofuran compound. Methods of synthesizing novel cationic substituted benzofuran compounds and the novel compounds themselves.

Cationic substituted benzofurans as antimicrobial agents

The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)-(VI) as recited throughout the application.

Compounds, methods and compositions useful for the treatment of bovine viral diarrhea virus (BVDV) infection and hepatitis C virus (HCV) infection

A compound of Formula (I): wherein: wherein n is a number from 1 to 3, and Ris H or &#x2014;CONHRNRR, wherein Ris lower alkyl and Rand Rare each independently selected from the group consisting of H and lower alkyl.

Dicationic 2,5-diarylfuran aza-analogs as anti-protozoan agents

The present invention relates to novel 2,5-bis{[alkyl (or aryl) imino]aminophenyl}furans and thiophenes of the general formula in which R, R, Rand Rare each independently selected from the group consisting of H, alkyl, alkoxy, halide, and alkylhalide groups; Ris H, alkyl or aryl; Ris H, alkyl, aryl, or NRR, in which Rand Rare each independently selected from the group consisting of H, alkyl and aryl; and X is O, S or NR, in which Ris H or alkyl, and to the use of such compounds.

The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)&#x2013;(VI) as recited throughout the application.

Growing community of inventors

Pittsboro, NC, United States of America

Richard Ray Tidwell