University of Florida Research Foundation, Incorporated

Robert William Huigens, Iii

Yasmeen Abouelhassan

Hendrik Luesch

Akash Basak

Hongfen Yang

Shouguang Jin

Gena Burch

Aaron Garrison

Nicholas G Paciaroni

Verrill M Norwood, Iv

The present invention provides phenazine derivatives, such as compounds of Formula (I). The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides compositions, kits, uses, and methods that involve the compounds of the invention, which may be useful in preventing or treating a microbial infection (e.g., a bacterial infection or mycobacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium or mycobacterium), killing a microorganism (e.g., a bacterium or mycobacterium), inhibiting the formation and/or growth of a biofilm, reducing or clearing a biofilm, and/or disinfecting a surface.

3-substituted phenazine derivatives as antimicrobial agents

The present invention provides novel compounds of Formula (I') and (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for killing a microorganism (e.g., bacteria, fungi, viruses, protozoa, or multicellular parasites), the prevention and/or treatment of infectious diseases (e.g., infections by microorganisms, bacterial infection, cystic fibrosis infection, foreign body infection, urinary tract infection (UTI), or infections leading to biofilms), controlling and/or eradicating biofilms (e.g., bacterial biofilms), preventing biofilm formation, sterilizing a surface, and/or eradicating persister cells (e.g., in a subject in need thereof or in a subject involving a biofilm). 

N-arylated analogues and uses thereof

The present disclosure provides compounds of Formulae (I-A), (II'), (III-A), (IV&#x2032;), and (V-A), wherein the compounds are derived from or based on yohimbine. The provided compounds may be useful in treating or preventing a disease (e.g., proliferative disease, cancers, inflammatory diseases, autoimmune diseases, and infectious diseases) in a subject in need thereof. The present disclosure provides methods of preparing compounds of Formulae (I-A), (II&#x2032;), (III-A), (IV&#x2032;), and (V-A). Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein. 

Analogs of yohimbine and uses thereof

The present disclosure provides compounds of any one of Formulae (I'), (I), (IA), (II&#x2032;), (II), (IIA), (IIIA), (III&#x2033;), (III&#x2032;), (III), (IIIA), (IV), (V&#x2032;), (V), (VI), (VII), (VIII&#x2032;), (VIII), (IX&#x2032;), (IX), and (X). The compounds described herein may be useful in treating and/or preventing a broad range of diseases (e.g., proliferative disease (e.g., cancers (e.g., non-small cell lung cancer, or glioma), inflammatory diseases, autoimmune diseases), CNS disorder (e.g., drug addiction), metabolic disorder (e.g., diabetes), or infectious disease (e.g., bacterial infection or parasitic infection (e.g., malaria))). Also provided in the present disclosure are pharmaceutical compositions, methods of synthesis of a compound described herein, kits, methods, and uses including or using a compound described herein. 

Analogs of vincamine and uses thereof

The present invention provides novel phenazine derivatives, such as compounds of Formula (I) (e.g., Formulae (II)-(XIX)), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the compounds of the invention and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection or mycobacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium or mycobacterium), killing a microorganism (e.g., a bacterium or mycobacterium), inhibiting the formation and/or growth of a biofilm, reducing or clearing a biofilm, and/or disinfecting a surface.

Phenazine derivatives as antimicrobial agents

The present invention provides halogenated quinoline derivatives, such as compounds of Formula (I) or (I'), and pharmaceutically acceptable salts thereof, and methods of preparing the halogenated quinoline derivatives. The halogenated quinoline derivatives are expected to be antimicrobial agents and may act through an iron(II)-dependent mode of action. The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the halogenated quinoline derivatives and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium), killing a microorganism (e.g., a bacterium), inhibiting the formation and/or growth of a biofilm, reducing or removing a biofilm, and/or disinfecting a surface. 

Halogenated quinoline derivatives as antimicrobial agents

The present invention provides novel phenazine derivatives, such as compounds of Formula (I) and (II), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the compounds of the invention and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium), killing a microorganism (e.g., a bacterium), inhibiting the formation and/or growth of a biofilm, or reducing or clearing a biofilm. 

Growing community of inventors

Williston, FL, United States of America

Robert William Huigens, Iii