A5033797472- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Enzyme function and inhibition
- Reproductive tract infections research
- HIV/AIDS Research and Interventions
- Computational Drug Discovery Methods
- Adolescent Sexual and Reproductive Health
- Amino Acid Enzymes and Metabolism
- Pharmacogenetics and Drug Metabolism
- Autism Spectrum Disorder Research
- Peptidase Inhibition and Analysis
- HIV Research and Treatment
- Inflammatory mediators and NSAID effects
- Ferrocene Chemistry and Applications
- Game Theory and Voting Systems
- Fluorine in Organic Chemistry
- Biopolymer Synthesis and Applications
- Neuroendocrine regulation and behavior
- Synthesis of Organic Compounds
- Biomedical and Engineering Education
- Innovative Microfluidic and Catalytic Techniques Innovation
- HIV-related health complications and treatments
- Protein Degradation and Inhibitors
- Zebrafish Biomedical Research Applications
- Vitamin K Research Studies
Duke University
2014-2023
Center for Autism and Related Disorders
2019
Duke University Hospital
2019
Duke Medical Center
2019
Novartis (Switzerland)
1994
The preparation of a series 1-glutarylindoline-2(S)-carboxylic acid derivatives, 6a-v and 21a-c, is described. above compounds were tested for inhibition angiotensin converting enzyme. structure-activity relationship the also discussed. Compound 6u, most potent member series, had an in vitro IC50 4.8 X 10(-9) M. 6v, ethyl ester lowered blood pressure 70 mm spontaneous hypertensive rats at oral dose 30 mg/kg.
Gels are one of the soft material platforms being evaluated to deliver topically acting anti-HIV drugs (microbicides) vaginal environment. For each drug, its loaded concentration, gel properties and applied volume, frequency dosing can be designed optimize PK and, thence, PD. These factors also impact user sensory perceptions acceptability. Deterministic compartmental modeling deployment drug delivery achieved by test gels help delineate how multiple parameters characterizing vehicle,...
The design and preparation of ortho-substituted benzofused macrocyclic lactams are described. were designed as neutral endopeptidase 24.11 (NEP) inhibitors. Docking studies carried out in a model thermolysin (TLN) using the MACROMODEL QXP modeling programs to select suitable ring sizes. These predicted that 11-, 12-, 13-membered would be active both enzymes TLN NEP. Good predictability experimental results, within this series, binding lesser extent NEP was observed. A visual comparison,...
The synthesis of N-(3-mercaptopropionyl)-N-arylglycines (14a-x),- N-arylalanines (15a,b),-N-cycloalkylglycines (16a-k), and -1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids (17a-d), -1,2,3,4-tetrahydroquinoline-2-carboxylic (18a-f), -indoline-2-carboxylic (19a-k) is described. In vitro inhibition angiotensin converting enzyme (ACE) reported for each compound, the structure--activity relationship series discussed. in vivo ACE antihypertensive effects representative compounds from are most...
The synthesis and biological activities of biarylamide-substituted diaminoindanes as microsomal triglyceride transfer protein (MTP) inhibitors are described. One the more potent compounds, 8aR, inhibited both secretion apoB from Hep G2 cells MTP-mediated triglycerides between synthetic acceptor donor liposomes with IC(50) values 0.7 70 nM, respectively. In normolipidemic rats dogs, oral administration 8aR dose-dependently reduced plasma total cholesterol. Moreover, in also prevented...
Play-based observations allow researchers to observe autistic children across a wide range of ages and skills. We recorded playing with toys in the center room at corner table while caregiver remained seated off side used video tracking technology track children's movement location. examined how time spent regions whether or not they approached each region during play related their cognitive, social, communication, adaptive skills determine if child location can meaningfully demonstrate...
The design, synthesis, and biochemical profile of meta-substituted benzofused macrocyclic lactams are described. were designed to have a degree flexibility allowing the amide bond occupy two completely different conformations while maintaining sufficient rigidity allow for strong interaction between enzyme inhibitor. Using TFIT, novel molecular superimposition program, it was shown that meta analogs could be readily superimposed onto our ACE inhibitor template whereas no low-energy...
The synthesis of two new series dicarboxylic acid dipeptides and sulfhydryl-containing inhibitors are described. in vitro enkephalinase inhibition data some vivo analgesic presented for these compounds. For the dibenzylglutaric structure-activity relationships activity discussed. reverse amides, i.e., 4-amino-2,4-dibenzylbutyric derivatives, also Two showed good potency mouse jump-latency hot-plate test after peripheral administration at moderate low doses.
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDual Angiotensin Converting Enzyme/Thromboxane Synthase InhibitorsGary M. Ksander, Mark Erion, Andrew Yuan, Clive G. Diefenbacher, Lena El-Chehabi, Don Cote, and Nigel LevensCite this: J. Med. Chem. 1994, 37, 12, 1823–1832Publication Date (Print):June 1, 1994Publication History Published online1 May 2002Published inissue 1 June 1994https://pubs.acs.org/doi/10.1021/jm00038a011https://doi.org/10.1021/jm00038a011research-articleACS PublicationsRequest...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTAngiotensin converting enzyme inhibitors: N-substituted D-glutamic acid .gamma.-dipeptidesGary M. Ksander, Andrew Yuan, Clive G. Diefenbacher, and James L. StantonCite this: J. Med. Chem. 1985, 28, 11, 1606–1611Publication Date (Print):November 1, 1985Publication History Published online1 May 2002Published inissue 1 November 1985https://pubs.acs.org/doi/10.1021/jm00149a011https://doi.org/10.1021/jm00149a011research-articleACS PublicationsRequest...
Motivated by real-world applications such as the allocation of public housing, we examine problem assigning a group agents to vertices (e.g., spatial locations) network so that diversity level is maximized. Specifically, are two types (characterized features), and measure number who have at least one neighbor different type. This known be NP-hard, focus on developing approximation algorithms with provable performance guarantees. We first present local-improvement algorithm for general graphs...
This study conducted a needs assessment and feasibility testing of Going Places, novel park-based active transportation intervention that aims to improve physical activity access parks recreation. Participants (n=19) were recruited from park sites serving predominantly racial/ethnic minority low income communities in North Carolina, United States. Surveys administered participants (n=17), accelerometer-based step data was collected (n=6), one focus group (n=6). Feasibility assessed based on...
We develop a rigorous mathematical analysis of zero-shot learning with attributes. In this setting, the goal is to label novel classes no training data, only detectors for attributes and description how those are correlated target classes, called class-attribute matrix. first non-trivial lower bound on worst-case error best map from even perfect attribute detectors. The characterizes theoretical intrinsic difficulty problem based available information -- matrix practically computable it. Our...
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”
Abstract Das Anilin (I) ergibt über die Verbindungen (III) mit (IV) das Mercaptopropionyl‐glycin (V).
Abstract Die mit dem Anhydrid (II) zugänglich gemachten Verbindungen (III), (IV) und (VI) werden auf ACE‐inhibierende Aktivität untersucht; Als wirksamste erweisen sich dabei (III) (VIa).
Abstract Wie im Formelschema skizziert, werden die Indoline (VII) dargestellt.