A5090332646- Tuberculosis Research and Epidemiology
- Antibiotic Resistance in Bacteria
- Cancer therapeutics and mechanisms
- Mycobacterium research and diagnosis
- Enzyme Production and Characterization
- Carbohydrate Chemistry and Synthesis
- RNA and protein synthesis mechanisms
- Pneumonia and Respiratory Infections
- Drug Transport and Resistance Mechanisms
- Burkholderia infections and melioidosis
- Respiratory and Cough-Related Research
- Enzyme Catalysis and Immobilization
- Malaria Research and Control
- Antimicrobial Resistance in Staphylococcus
- Bacteriophages and microbial interactions
- Syphilis Diagnosis and Treatment
- Quinazolinone synthesis and applications
- Urinary Tract Infections Management
- HIV Research and Treatment
- Antimicrobial Peptides and Activities
- Glycosylation and Glycoproteins Research
- Reproductive tract infections research
St. Jude Children's Research Hospital
2014-2024
Microbiotix (United States)
2022-2024
Medicines for Malaria Venture
2022
National Institute of Allergy and Infectious Diseases
2022
National Institutes of Health
2022
University of Chicago
2010
University of Illinois Chicago
2010
Mycobacterium abscessus ( Mab ), a nontuberculous mycobacterial (NTM) species, is an emerging pathogen with high intrinsic drug resistance. Current standard-of-care therapy results in poor outcomes, demonstrating the urgent need to develop effective antimycobacterial regimens. Through synthetic modification of spectinomycin (SPC), we have identified distinct structural subclass N-ethylene linked aminomethyl SPCs (eAmSPCs) that are up 64-fold more potent against over parent SPC. Mechanism...
Spectinamides are a novel class of antitubercular agents with the potential to treat drug-resistant tuberculosis infections. Their activity is derived from both ribosomal affinity and their ability overcome intrinsic efflux mediated by Mycobacterium Rv1258c pump. This study explores structure-activity relationships through analysis 50 targeted spectinamides. Compounds evaluated for translational inhibition, MIC in pump deficient wild type strains, efficacy an acute model infection. The...
ABSTRACT Bacterial sexually transmitted infections are widespread and common, with Neisseria gonorrhoeae (gonorrhea) Chlamydia trachomatis (chlamydia) being the two most frequent causes. If left untreated, both can cause pelvic inflammatory disease, infertility, ectopic pregnancy, other sequelae. The recommended treatment for gonorrhea is ceftriaxone plus azithromycin (to empirically treat chlamydial coinfections). Antibiotic resistance to all existing therapies has developed in gonorrheal...
A new series of spectinomycin analogs with potency against drug-resistant bacterial pathogens was designed and developed a structure-based approach validated in vitro vivo.
New antibiotics that are active against multi-drug-resistant strains and difficult-to-treat bacterial infections needed. Synthetic modification of spectinomycin, a protein synthesis inhibitor, has been shown to increase antibacterial activity compared with spectinomycin. Aminomethyl spectinomycins Gram-negative Gram-positive pathogens. In this study, the ability aminomethyl treat biothreat pathogens is examined by MIC profiling, synergy testing, in vivo efficacy experiments. Compound 1950...
Human and animal malaria parasites increase their host erythrocyte permeability to a broad range of solutes as mediated by parasite-associated ion channels. Molecular pharmacological studies have implicated an essential role in parasite nutrient acquisition, but inhibitors suitable for development antimalarial drugs are missing. Here, we generated potent specific drug lead using <i>Plasmodium falciparum</i>, virulent human pathogen, derivatives MBX-2366, nanomolar affinity pyridazinone...
Abstract The spectinamides are novel, narrow-spectrum semisynthetic analogs of spectinomycin, modified to avoid intrinsic efflux by Mycobacterium tuberculosis . Spectinamides, including lead MBX-4888A (Lee-1810), exhibit promising therapeutic profiles in mice, as single drugs and partner agents with other anti-tuberculosis antibiotics rifampin and/or pyrazinamide. To demonstrate that this translates more effective cure, we first confirmed the role rifampin, or without pyrazinamide, essential...
ABSTRACT The spectinamides are novel, narrow-spectrum semisynthetic analogs of spectinomycin, modified to avoid intrinsic efflux by Mycobacterium tuberculosis . Spectinamides, including lead MBX-4888A (Lee-1810), exhibit promising therapeutic profiles in mice, as single drugs and partner agents with other anti-tuberculosis antibiotics rifampin and/or pyrazinamide. Here, we show that MBX-4888A, given injection the front-line standard care regimen, is treatment shortening multiple murine...
The most frequent ailment for which antibiotics are prescribed is otitis media (ear infections), commonly caused by
Abstract Review: 176 refs.