A5035655436- Chemical Synthesis and Analysis
- Medical Imaging Techniques and Applications
- Catalytic C–H Functionalization Methods
- Advanced MRI Techniques and Applications
- Click Chemistry and Applications
- Synthesis and Biological Evaluation
- Synthesis and bioactivity of alkaloids
- Multicomponent Synthesis of Heterocycles
- Quinazolinone synthesis and applications
- Synthesis and Characterization of Heterocyclic Compounds
- Phenothiazines and Benzothiazines Synthesis and Activities
- Cardiac Imaging and Diagnostics
- Chemical synthesis and alkaloids
- Radiomics and Machine Learning in Medical Imaging
- Synthesis and Catalytic Reactions
- Catalytic Alkyne Reactions
- Carbohydrate Chemistry and Synthesis
- Quantum Chromodynamics and Particle Interactions
- Chemical Synthesis and Reactions
- Synthesis of Indole Derivatives
- Synthesis and pharmacology of benzodiazepine derivatives
- Antimicrobial Peptides and Activities
- Synthesis and Reactivity of Heterocycles
- Particle physics theoretical and experimental studies
- Synthesis and Biological Activity
University of Virginia
2015-2025
Institute of Biophysics and Biomedical Engineering
2023
Urology of Virginia
2021
Collaborative Group (United States)
2021
Central Drug Research Institute
2008-2020
Beijing Institute of Technology
2015
Academy of Scientific and Innovative Research
2013-2015
University of Virginia Health System
2007-2015
Indian Institute of Science Education and Research, Bhopal
2014
Medway Maritime Hospital
2003
Background Changes in energy substrate metabolism are first responders to hemodynamic stress the heart. We have previously shown that hexose‐6‐phosphate levels regulate mammalian target of rapamycin ( mTOR ) activation response insulin. now tested hypothesis inotropic stimulation and increased afterload also via glucose 6‐phosphate (G6P) accumulation. Methods Results subjected working rat heart ex vivo a high workload presence different energy‐providing substrates including glucose,...
Bioactivities of 42 didemnin congeners, either isolated from the marine tunicates Trididemnun solidum and Aplidium albicans or prepared synthetically semisynthetically, have been compared. The growth inhibition various murine human tumor cells plaque reduction HSV-1 VSV grown on cultured mammalian were used to assess cytotoxicity antiviral activity. Biochemical assays for macromolecular synthesis (protein, DNA, RNA) enzyme (dihydrofolate reductase, thymidylate synthase, DNA polymerase, RNA...
<h3>Background</h3> Randomised controlled trials (RCTs) are considered particularly likely to benefit from patient and public involvement (PPI). Decisions made by professional researchers at the outset may go on have a significant impact potential for PPI contributions. <h3>Objective</h3> To increase knowledge of within early development RCTs systematically describing reported level, nature acceptability proposed funders. <h3>Methods</h3> Documentation outline application process all that...
A simple and efficient one-pot protocol for the synthesis of NH-carbazoles has been described. The strategy comprises a reaction involving treatment 2-alkynyl indoles with arylacetylenes in presence an Au-Ag combination catalyst. salient feature involves sequential activation terminal internal alkynes leading to cascade hydroarylation 6-endo-dig carbocyclization reactions. generality method demonstrated by using series arylacetylenes.
Background Sustained pressure overload leads to changes in cardiac metabolism, function, and structure. Both time course causal relationships between these are not fully understood. Therefore, we studied spontaneously hypertensive rats (SHR) during early hypertension development compared them control Wistar Kyoto rats. Methods Results We serially evaluated myocardial glucose uptake rates (Ki) with dynamic 2‐[ 18 F] fluoro‐2‐deoxy‐D‐glucose positron emission tomography, ejection fraction left...
Abstract A new route to the synthesis of isocryptolepine alkaloid with antimalarial activity using a modified Pictet–Spengler reaction has been devised. The strategy was then used generate libraries based on three structural variants alkaloid. Compounds these in general were accessed steps through cyclization as key step. C‐2‐, C‐3‐, or N‐1‐linked (aminoaryl)indoles ( 8 , 12 13 ) required for obtained by treating corresponding indoles o ‐halonitrobenzene either nucleophilic replacement...
A rapid one-pot protocol for the synthesis of indole-based polyheterocycles via a sequential Lewis acid catalyzed intermolecular Michael addition and an intramolecular azide/internal alkyne 1,3-dipolar cycloaddition reaction has been described. The generality method demonstrated by treating series aromatic/aliphatic 2-alkynyl indoles with substituted (E)-1-azido-2-(2-nitrovinyl)benzenes to furnish annulated tetracyclic indolo[2,3-c][1,2,3]triazolo[1,5-a][1]benzazepines in good yields.
We proposed that metabolic remodeling in the form of increased uptake myocardial glucose analog (18)F-FDG precedes and triggers onset severe contractile dysfunction pressure-overload left ventricular hypertrophy vivo. To test this hypothesis, we used a mouse model transverse aortic constriction (TAC) together with PET assessed serial changes cardiac metabolism function over 7 d.Scans 16 C57BL/6 male mice were obtained using small-animal device under sevoflurane anesthesia. A 10-min...
We describe two simple straightforward syntheses of triazolo isoquinolines (3) and isochromenes (7) from 2-alkynylbenzaldehydes (1) as a common synthon. The synthetic strategy for 3 involves formation the (E)-1-(2-nitrovinyl)-2-(alkynyl)benzene species 2 via condensation synthon 1 with nitromethane followed by [3 + 2] cycloaddition/extrusion nitro group/regioselective 6-endo cyclization domino sequence. In yet another strategy, was condensed electrophilic iodo resulting...
An efficient method for the synthesis of new polycyclic skeletons: triaza-benzofluorenes and triaza-pentalenonaphthalene from bicyclic privileged structures imidazopyridine imidazothiazole, respectively, has been described using Pictet−Spengler cyclization.
A two-step protocol for the diversity-oriented synthesis of annulated indoles following MCR-post MCR modification concept is described. The reaction initially proceeds through annulation 2-(2,2-dibromovinyl)aniline, an isocyanate, and a terminal alkyne in three-component tandem format via Cu/Pd-catalyzed cross coupling to afford N-1 C-2 functionalized indole. In subsequent step, enyne–urea derivative undergoes chemo- regioselective 6-endo cyclization O-cyclized product presence Au(I)/AgNO3...
An efficient synthesis toward highly diversified α-carboline derivatives via a three-component tandem reaction using acid chlorides, terminal alkynes, and 2-aminoindole hydrochlorides has been described. The salient feature of the one-pot strategy involves regioselective [3 + 3]-cyclocondensation presence water in medium to facilitate cyclization. Nonaqueous conditions furnished products poor yields.
An efficient and rapid synthetic strategy for the naturally occurring indoloazepinone scaffold via a three-component reaction of indole-2-carboxamides, 1,3-disubstituted propargyl alcohols, I2 is described. The involves C–H functionalization–alkyne activation–intramolecular hydroamidation–deprotonation domino sequence. salient feature this sequence regioselective electrophilic 7-endo-dig iodo-cyclization during intramolecular hydroamidation to afford seven-membered azepinone ring annulated indole.
A one-pot protocol involving Zn/CuI/TFA-catalyzed domino three-component and subsequent carbocyclization reactions is described. The reaction proceeds via formation of propargyl amines from biphenyl-2-carbaldehydes/terminal alkynes/piperidine followed by the elimination piperidine ring closure to furnish phenanthrene derivatives in good yields. strategy involves C(sp)-H activation–CH functionalization with imine-alkyne activation–1,5 hydride shift−β-elimination piperidine–allene formation–6π...
Abstract A one pot synthesis of 1 H ‐benzo[g]indoles, tetrahydrobenzo[h]quinolines, and naphtho[1,2‐b]azepines from 2‐alkynyl benzaldehydes cyclic amino acids is reported. The salient feature the strategy involves formation three new bonds (one CN two CC bonds) by a metal‐free decarboxylation/cyclization/one‐carbon ring expansion sequence in pot.
A one-pot protocol for the diversity-oriented synthesis of two indole-based annulated polyheterocycles, ketoindoloquinoxalines and indolotriazoloquinoxalines, has been described. The salient features methodology involves either a metal/O2-catalyzed aminooxygenation or [3 + 2] cycloaddition pathway.
We describe a straightforward strategy for the synthesis of strongly fluorescent pyridoindoles by Pd-catalyzed oxidative annulations internal alkynes with C-3 functionalized indoles through CH/NH bond activation in one-pot tandem process. Mechanistic investigations reveal preferential NH indole followed CH during cyclization Photophysical properties exhibited highest fluorescence quantum yield nearly 80 %, emission color varying from blue to green orange depending on substructures....
Brown adipose tissue (BAT) is specialized in thermogenesis. The conversion of energy into heat brown adipocytes proceeds via stimulation β-adrenergic receptor (βAR)-dependent signaling and activation mitochondrial uncoupling protein 1 (UCP1). We have previously demonstrated a functional role for pannexin-1 (Panx1) channels white tissue; however, it not known whether Panx1 play the regulation adipocyte function. Here, we tested hypothesis that are involved thermogenesis.In an immortalized...
In concussion, clinical and physiological recovery are increasingly recognized as diverging definitions. This study investigated whether central microglial activation persisted in participants with concussion after receiving an unrestricted return-to-play (uRTP) designation using [18F]DPA-714 PET, vivo marker of microglia activation.Eight (5 M, 3 F) current athletes (Group 1) 10 5 healthy collegiate students 2) were enrolled. Group 1 completed a pre-injury (Visit1) screen, follow-up Visit2...
[reaction: see text] A mild, efficient, one-pot protocol for the cyclization of nitro-aryl substrates using SnCl(2) has been described. The mechanistic course reaction suggests involvement a hydroxylamine intermediate leading to an intramolecular via N-N bond formation. versatility methodology demonstrated by two derived from dihydroisoquinolines and dihydro-beta-carbolines. led formation indazoles in high yields purities.