Rutgers, the State University of New Jersey

The Johns Hopkins University

The Texas A&m University System

Joel S Freundlich

Sean Ekins

Richard H Ebright

David Alland

Divya Awasthi

Pradeep Kumar

Matthew B Neiditch

Glenn Capodagli

Yon W Ebright

Craig Arthur Townsend

James C Sacchettini

Gyanu Lamichhane

Juan Shen

Nicole M Parrish

Evan P Lloyd

Mark Jaskowski

Inna V Kriger

Thomas R Ioerger

Vijay Gawandi

Ricardo Gallardo-Macias

Amit Kaushik

Shao-Gang Li

Pankaj Kumar

Shaogang Li

Nisha Mittal

The invention provides compounds of formula I: and salts thereof wherein R-Rhave any of the meanings described in the specification. The compounds are useful for treating bacterial infections (e.g. tuberculosis).

Therapeutic indazoles

The invention provides compounds of formula (I) or (II) and tautomers and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula (I) or (II) or a tautomer or salt thereof, methods of making a compound of formula (I) or (II) or a tautomer or salt thereof, and methods of using a compound of formula (I) or (II) or a tautomer or salt thereof as, e.g., inhibitors of bacterial RNA polymerase or as antibacterial agents. 

Antibacterial agents: arylalkylcarboxamido phloroglucinols

The invention provides compounds of formula (I): and salts thereof wherein R-Rhave any of the meanings described in the specification. The compounds are useful for treating bacterial infections (e.g. tuberculosis). 

New antimicrobials targeting L,D-transpeptidases, non-classical cysteine peptidases, have been developed and their unique chemical structures identified. Carbapenems and penems of the present invention are unique among &#x3b2;-lactams as they acylate and inhibit L,D-transpeptidases, which likely results in their superior antimicrobial potency. These new antimicrobial agents can be used alone, or in combination with other classic antimicrobial agents that target D,D transpeptidases, when treating bacterial infections.

Inhibitors of bacterial growth

The invention provides compounds that are inhibitors of bacterial RNA polymerase. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.

Inhibitors of bacterial RNA polymerase: arylpropanoyl, arylpropenoyl, and arylcyclopropanecarboxyl phloroglucinols

The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.

Inhibitors of mycobacterium tuberculosis malate synthase, methods of making and uses thereof

Growing community of inventors

New Brunswick, NJ, United States of America

Joel S Freundlich