A5091265699- Synthesis of β-Lactam Compounds
- Synthesis and Catalytic Reactions
- Asymmetric Synthesis and Catalysis
- Chemical Synthesis and Analysis
- Synthetic Organic Chemistry Methods
- Antibiotic Resistance in Bacteria
- Carbohydrate Chemistry and Synthesis
- Tuberculosis Research and Epidemiology
- Cancer therapeutics and mechanisms
- Microbial Natural Products and Biosynthesis
- Oxidative Organic Chemistry Reactions
- Chemical Synthesis and Reactions
- Antibiotics Pharmacokinetics and Efficacy
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Biological Evaluation
- Mycobacterium research and diagnosis
- Bipolar Disorder and Treatment
- Chemical Reaction Mechanisms
- Chemical synthesis and alkaloids
- HIV/AIDS drug development and treatment
- X-ray Diffraction in Crystallography
- Asymmetric Hydrogenation and Catalysis
- Crystallization and Solubility Studies
- Analytical Chemistry and Chromatography
- Quinazolinone synthesis and applications
University of Notre Dame
2016-2025
Notre Dame of Dadiangas University
2014-2021
Hsiri Therapeutics (United States)
2018
Wright State University
2016
University of Oklahoma Health Sciences Center
2013
Leibniz-Institut für Naturstoff-Forschung und Infektionsbiologie e. V. - Hans-Knöll-Institut (HKI)
2007-2009
Eli Lilly (United States)
2008
Leibniz Association
2007
Harvard University
2004
Boston University
2004
Unlike major histocompatibility proteins, which bind peptides, CD1 proteins display lipid antigens to T cells. Here, we report that CD1a presents a family of previously unknown lipopeptides from Mycobacterium tuberculosis , named didehydroxymycobactins because their structural relation mycobactin siderophores. cell activation was mediated by the αβ receptors and specific for structure acyl peptidic components these antigens. These studies identify means intracellular pathogen detection as...
Previous studies have suggested that bipolar patients are supersensitive to light suppression of melatonin and this may be a trait marker for genetic vulnerability. The present study was an attempt replicate extend observation. Propranolol hydrochloride effects were compared with because the documented influence beta-adrenergic receptors on production. Nighttime levels corticotropin cortisol also examined as potential vulnerability markers.Melatonin in euthymic (n= 29) tested before after...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTHydroxamate approach to the synthesis of .beta.-lactam antibioticsMarvin J. MillerCite this: Acc. Chem. Res. 1986, 19, 2, 49–56Publication Date (Print):February 1, 1986Publication History Published online1 May 2002Published inissue 1 February 1986https://pubs.acs.org/doi/10.1021/ar00122a004https://doi.org/10.1021/ar00122a004research-articleACS PublicationsRequest reuse permissionsArticle Views970Altmetric-Citations200LEARN ABOUT THESE...
A set of nine 2,7-dimethylimidazo[1,2-a]pyridine-3-carboxamides and one 2,6-dimethylimidazo[1,2-a]pyrimidine-3-carboxamide were synthesized. The compounds evaluated for their in vitro antituberculosis activity versus replicating, nonreplicating, multi- extensive drug resistant Mtb strains. MIC90 values seven these agents ≤1 μM against the various tuberculosis strains tested. representative compound this class (1) was screened nontubercular as well other nonmycobacteria organisms demonstrated...
Tuberculosis is a serious global health problem caused by the bacterium Mycobacterium tuberculosis. There an urgent need for discovery and development of new treatments, but this can only be accomplished through rapid reproducible M. tuberculosis assays designed to identify potent inhibitors. We developed automated 96-well assay utilizing recombinant strain expressing far-red fluorescent reporter determine activity novel compounds; allowed us measure growth monitoring both optical density...
Although the antimalarial agent artemisinin itself is not active against tuberculosis, conjugation to a mycobacterial-specific siderophore (microbial iron chelator) analogue induces significant and selective antituberculosis activity, including activity multi- extensively drug-resistant strains of Mycobacterium tuberculosis. The conjugate also retains potent activity. Physicochemical whole-cell studies indicated that ferric-to-ferrous reduction complex initiates expected bactericidal...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of .beta.-lactams from substituted hydroxamic acidsMarvin J. Miller, Phillip G. Mattingly, Marjorie A. Morrison, and James F. Kerwin Jr.Cite this: Am. Chem. Soc. 1980, 102, 23, 7026–7032Publication Date (Print):November 5, 1980Publication History Published online1 May 2002Published inissue 5 November 1980https://pubs.acs.org/doi/10.1021/ja00543a021https://doi.org/10.1021/ja00543a021research-articleACS PublicationsRequest reuse...
An artificial tris-catecolate siderophore with a tripodal backbone and its conjugates ampicillin amoxicillin were synthesized. Both exhibited significantly enhanced in vitro antibacterial activities against Gram-negative species compared to the parent drugs, especially Pseudomonas aeruginosa . The appeared be assimilated by an induced bacterial iron transport process as their inversely related concentration. easily synthesized has great potential for future development of various drug target...
Siderophores are multidentate iron(III) chelators used by bacteria for iron assimilation. Sideromycins, also called siderophore-antibiotic conjugates, a unique subset of siderophores that enter bacterial cells via siderophore uptake pathways and deliver the toxic antibiotic in "Trojan horse" fashion. Sideromycins represent novel delivery technology with untapped potential developing sophisticated microbe-selective antibacterial agents limit emergence resistance. The chemical synthesis series...
In order to address the dire need for new antibiotics treat specific strains of drug resistant Gram-negative bacterial infections, a mixed ligand analog natural Acinetobacter baumannii selective siderophore, fimsbactin, was coupled daptomycin, Gram-positive only antibiotic. The resulting conjugate 11 has potent activity against multidrug A. both in vitro and vivo. study also indicates that conjugation siderophores "drugs" are much larger than siderophore (iron transport agent) itself...
Many antibiotics lack activity against Gram-negative bacteria because they cannot permeate the outer membrane or suffer from efflux and, in case of β-lactams, are degraded by β-lactamases. Herein, we describe synthesis and studies a dual drug conjugate (1) siderophore linked to cephalosporin with an attached oxazolidinone. The component 1 is rapidly hydrolyzed purified ADC-1 β-lactamase release Conjugate active clinical isolates Acinetobacter baumannii as well strains producing large amounts...
Chemical syntheses and biological evaluation of biscatecholate-monohydroxamate mixed ligand sideromycins utilizing the carbacephalosporin β-lactam antibiotic loracarbef fluoroquinolone ciprofloxacin are described. The sideromycin (1b) had remarkably selective extremely potent antibacterial activity against Gram-negative pathogen Acinetobacter baumannii ATCC 17961 (MIC = 0.0078 μM). was inversely related to iron(III) concentration in testing media antagonized by presence competing parent...
A set of fourteen imidazo[1,2-a]pyridine-3-carboxamides was synthesized and screened against Mycobacterium tuberculosis H37Rv. The minimum inhibitory concentrations twelve these agents were ≤ 1 μM replicating bacteria five compounds (9, 12, 16, 17 18) had MIC values 0.006 μM. Compounds 13 18 a panel MDR XDR drug resistant clinical Mtb strains with the potency surpassing that candidate PA-824 by nearly 10 fold. in vivo pharmacokinetics evaluated male mice oral (PO) intravenous (IV) routes....
Background: Clinical trials of anti-Aβ monoclonal antibodies in Alzheimer disease (AD) infer target engagement from Aβ positron emission tomography (PET) and/or fluid biomarkers such as cerebrospinal (CSF) Aβ42/40.However, these measure deposits indirectly incompletely.In contrast, postmortem neuropathologic assessments allow direct investigation treatment effects on brain and many other pathologic features.Methods: From a clinical trial dominantly inherited AD, we measured...
As part of the four-center NIMH Genetics Initiative on Bipolar Disorder we carried out a genomic scan chromosomes 3, 5, 15, 16,17, and 22. Genotyping was performed set 540 DNAs from 97 families, enriched for affected relative pairs parents where available. We report here results initial 74 markers that have been typed this DNAs. The average distance between (theta) 12.3 cM. Nonparametric analysis excess allele sharing among sibling used SIBPAL program S.A.G.E. package to test three...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTTitanium trichloride reduction of substituted N-hydroxy-2-azetidinones and other hydroxamic acidsPhillip G. Mattingly Marvin J. MillerCite this: Org. Chem. 1980, 45, 3, 410–415Publication Date (Print):February 1, 1980Publication History Published online1 May 2002Published inissue 1 February 1980https://pubs.acs.org/doi/10.1021/jo01291a007https://doi.org/10.1021/jo01291a007research-articleACS PublicationsRequest reuse permissionsArticle...
A series of N-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)arylamides was synthesized by copper-catalyzed azide−alkyne cycloaddition (CuAAC) and afforded inhibitors cancer cell growth. For example, compound 13e had an IC50 46 nM against MCF-7 human breast tumor cells. Structure−activity relationship (SAR) studies demonstrated that (i) meta-phenoxy substitution the N-1-benzyl group is important for antiproliferative activity (ii) a variety heterocyclic substitutions aryl arylamide are tolerated....