A5055033818- Catalytic Alkyne Reactions
- Epigenetics and DNA Methylation
- Bacterial Genetics and Biotechnology
- Cyclization and Aryne Chemistry
- Computational Drug Discovery Methods
- Cystic Fibrosis Research Advances
- Chemistry and Chemical Engineering
- Synthetic Organic Chemistry Methods
- Click Chemistry and Applications
- Catalytic C–H Functionalization Methods
- Extraction and Separation Processes
- Pneumocystis jirovecii pneumonia detection and treatment
- Organic Chemistry Cycloaddition Reactions
- Various Chemistry Research Topics
- Alzheimer's disease research and treatments
- Asymmetric Synthesis and Catalysis
- Cholinesterase and Neurodegenerative Diseases
- Advanced Synthetic Organic Chemistry
- Asymmetric Hydrogenation and Catalysis
- HIV/AIDS drug development and treatment
- Biochemical and Molecular Research
- Gut microbiota and health
- Chemical Synthesis and Analysis
University of California, Los Angeles
2018-2022
SUNY Geneseo
2017-2020
Darmstadt University of Applied Sciences
1986
Abstract The chemistry of strained cyclic alkynes has undergone a renaissance over the past two decades. However, related species, allenes, especially heterocyclic derivatives, have only recently resurfaced and represent another class valuable intermediates. We report mild facile means to generate parent 3,4‐oxacyclic allene from readily accessible silyl triflate precursor, then trap it in (4+2), (3+2), (2+2) reactions provide variety cycloadducts. In addition, we describe catalytic,...
The SARS-CoV-2 pandemic has prompted scientists from many disciplines to work collaboratively toward an effective response. As academic synthetic chemists, we examine how best contribute this ongoing effort.
We report the discovery of a novel class compounds that function as dual inhibitors enzymes neutral sphingomyelinase-2 (nSMase2) and acetylcholinesterase (AChE). Inhibition these provides unique strategy to suppress propagation tau pathology in treatment Alzheimer's disease (AD). describe key SAR elements affect relative nSMase2 and/or AChE inhibitor effects potency, addition identification two analogs release tau-bearing exosomes vitro vivo. Identification nSMase2/AChE represents new...
We report the conversion of amides to carboxylic acids using nonprecious metal catalysis. The methodology strategically employs a nickel-catalyzed esterification 2-(trimethylsilyl)ethanol, followed by fluoride-mediated deprotection in single-pot operation. This approach circumvents catalyst poisoning observed attempts directly hydrolyze nickel selectivity and mildness this transformation are shown through competition experiments net-hydrolysis complex valine-derived substrate. strategy...
Transient strained cyclic intermediates have become valuable in modern synthetic chemistry. Although silyl triflate precursors to are most often employed, the instability of some triflates warrants development alternative precursors. We report syntheses tosylate cyclohexyne, 1,2-cyclohexadiene, and 1,2-cycloheptadiene. The resultant undergo trapping situ give cycloaddition products. Additionally, results competition experiments between tosylates reported.
We report an alternative approach to the unnatural nucleobase fragment seen in remdesivir (Veklury). Remdesivir displays broad-spectrum antiviral activity and is currently being evaluated Phase III clinical trials treat patients with COVID-19. Our route relies on formation of a cyanoamidine intermediate, which undergoes Lewis acid-mediated cyclization yield desired nucleobase. The strategically distinct from prior routes could further enable synthesis other small-molecule therapeutics.
ABSTRACT In Escherichia coli, DNA cytosine methyltransferase (Dcm) methylates the second in sequence 5′CCWGG3′ generating 5-methylcytosine. Dcm is not associated with a cognate restriction enzyme, suggesting impacts facets of bacterial physiology outside restriction-modification systems. Other than gene expression changes, there are few phenotypes that have been identified strains natural or engineered loss, and thus function has remained an enigma. Herein, we demonstrate does impact growth...
A course centered around transition-metal catalysis in modern drug discovery was designed to illustrate the central role of organic chemistry driving small-molecule development. The highlighted both fundamental and applied concepts, first with a focus on process, followed by foundational principles catalytic methods. Finally, these topics were unified last portion course, where case studies served highlight use synthesis drugs. Three graduate students taught mentorship from faculty member,...
Abstract The chemistry of strained cyclic alkynes has undergone a renaissance over the past two decades. However, related species, allenes, especially heterocyclic derivatives, have only recently resurfaced and represent another class valuable intermediates. We report mild facile means to generate parent 3,4‐oxacyclic allene from readily accessible silyl triflate precursor, then trap it in (4+2), (3+2), (2+2) reactions provide variety cycloadducts. In addition, we describe catalytic,...
While the role of DNA methylation in eukaryotes is well known, little known about prokaryotes. Dcm a cytosine methyltransferase E. coli that methylates second sequence 5′CCWGG3′. Although recognition sites are function catalyzed by and mechanism which impacts bacterial physiology not yet known. Our laboratory's microarray data indicates numerous gene expression changes at stationary phase upon addition inhibitor, 5‐azacytidine, suggesting for phase. Stationary competition experiments were...
In Escherichia coli , DNA cytosine methyltransferase (Dcm) methylates the second in sequence 5′CCWGG3, where W is A or T. Dcm an operon with very short patch repair ( vsr ) gene, endonuclease that repairs T‐G mismatches caused by deamination of 5‐methylcytosine. The role methylation and dcm E. unknown remains enigma. Growth curve analyses wild‐type, knockout strains at both 37°C 20°C indicated no effect genes on growth rate. Our laboratory's microarray data comparing expression patterns...