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Mutations in the Pseudomonas aeruginosa Needle Protein Gene pscF Confer Resistance to Phenoxyacetamide Inhibitors of the Type III Secretion System
TLDR
The results implicate the PscF needle protein as an apparent new molecular target for T3 SS inhibitor discovery and suggest that three other chemically distinct T3SS inhibitors interact with one or more different targets or a different region of Pscf.
Characterization of a Novel Pyranopyridine Inhibitor of the AcrAB Efflux Pump of Escherichia coli
TLDR
MBX2319 is a potent EPI with possible utility as an adjunctive therapeutic agent for the treatment of infections caused by Gram-negative pathogens and was broadly active against Enterobacteriaceae species and Pseudomonas aeruginosa.
Identification of a Small-Molecule Entry Inhibitor for Filoviruses
TLDR
It is hypothesized that compound 7 binds to this hydrophobic pocket at or near the GP1 and GP2 interface and as a consequence inhibits EBOV infection of cells, but the details of the mechanism remain to be determined.
Discovery and Characterization of Inhibitors of Pseudomonas aeruginosa Type III Secretion
TLDR
Five inhibitors in three chemical classes were demonstrated to inhibit type III secretion selectively with minimal cytotoxicity and with no effects on bacterial growth or on the type II-mediated secretion of elastase.
Solute Restriction Reveals an Essential Role for clag3-Associated Channels in Malaria Parasite Nutrient Acquisition
TLDR
Findings indicate that plasmodial surface anion channel functions in nutrient acquisition for intracellular parasites, and antimalarial drug development targeting PSAC should be pursued.
3-(1H-tetrazol-5-yl)-4(3H)-quinazolinone sodium salt (MDL 427): a new antiallergic agent.
TLDR
These analogue sets demonstrated that an accessible electrophilic center and an acidic functionality were requirements for good antiallergic activity.
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.
TLDR
This work synthesized several inhibitory 2,6,9-trisubstituted purine derivatives and solved the crystal structure of one of these compounds, H717, in complex with human CDK2, providing a basis for the further development of more potent inhibitory drugs.
Recent advances in neurokinin receptor antagonists.
TLDR
In this review, the very recent advances in nonpeptide neurokinin receptor antagonists will be described with an emphasis on structure-activity relationships which have been developed.
Comparative In Vitro Activity Profiles of Novel Bis-Indole Antibacterials against Gram-Positive and Gram-Negative Clinical Isolates
TLDR
The bis-indole compounds show promise for the treatment of multidrug-resistant clinical pathogens and compared favorably to all comparator antibiotics.
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