A5009777252- Synthesis and Characterization of Pyrroles
- Pharmacological Effects and Toxicity Studies
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- Organic Chemistry Cycloaddition Reactions
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- X-ray Diffraction in Crystallography
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- Synthesis and Reactions of Organic Compounds
- Crystal structures of chemical compounds
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Reactivity of Heterocycles
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- Synthesis and pharmacology of benzodiazepine derivatives
- Asymmetric Synthesis and Catalysis
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- Neuroscience and Neuropharmacology Research
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Chemical Synthesis and Analysis
- Cancer therapeutics and mechanisms
- Synthesis of Organic Compounds
St. James's Hospital
1991-2024
Howard University
2005-2015
University of Maryland Eastern Shore
2010
Trinity College Dublin
2007
University of Washington
2001
Marshall University
1995
Louisiana State University Agricultural Center
1967
A new series of novel enaminones has been synthesized from cyclic beta-dicarbonyl precursors which were condensed with morpholine, pyrrolidine, phenethylamine, hydrazines, substituted benzyl amines, and anilines. These compounds subsequently evaluated for anticonvulsant activity in a variety models by the National Institute Neurological Communicative Disorders Stroke our laboratory. Several these exhibited potent remarkable lack neurotoxicity. The most active analog, methyl...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis and anticonvulsant activity of enaminones. 2. Further structure-activity correlationsK. R. Scott, Ivan O. Edafiogho, Erica L. Richardson, Vida A. Farrar, Jacqueline Moore, Elizabeth I. Tietz, Christine N. Hinko, Hyejung Chang, Afif El-Assadi, Jesse M. NicholsonCite this: J. Med. Chem. 1993, 36, 14, 1947–1955Publication Date (Print):July 1, 1993Publication History Published online1 May 2002Published inissue 1 July...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis and Anticonvulsant Activity of Enaminones. 3. Investigations on 4'-, 3'-, 2'-Substituted Polysubstituted Anilino Compounds, Sodium Channel Binding Studies, Toxicity Evaluations1,2K. R. Scott, Gary O. Rankin, James P. Stables, Mariano S. Alexander, Ivan Edafiogho, Vida A. Farrar, Kymberle Kolen, Jacqueline Moore, Lyndia D. Sims, Ahn TonnuCite this: J. Med. Chem. 1995, 38, 20, 4033–4043Publication Date (Print):September 1, 1995Publication...
Organic-redox initiated polymerization technique based on the co-initiators system comprising benzoyl peroxide and N-phenyldiethanolamine was used at ambient temperature to fabricate pH-responsive hydrogels. The effects of changes in concentration system, ratio which combined, type solvent, pH hydrating medium, cross-linking agent azo-bond pH-sensitive properties hydrogels were investigated. Increasing decreasing two types agents, replacing DMSO by ethanol as solvent resulted with increased...
Multidrug resistance (MDR), mediated by P-glycoprotein (Pgp) has been identified as altering the disposition of structurally diverse compounds. Previous in vitro studies bovine brain microvascular endothelial cells and MCF/<i>Adr</i> [Adriamycin (doxorubicin)-resistant human breast cancer] displayed that transport enaminone anticonvulsants was influenced Pgp. Therefore objectives this study to further evaluate influence Pgp on pharmacokinetics tissue distribution analogs. <i>mdr1ab</i> (+/+)...
For most antiviral drugs, low or variable bioavailability is attributed to poor absorption, susceptibility efflux, first pass metabolism. Enaminones are beta dicarbonyl compounds, which display P-glycoprotein (P-gp) substrate properties with high efflux ratios. This study investigates the influence of DM27, an enaminone, on in vitro transport agents and possibility using DM27 as a P-gp inhibitor prevent certain antiretroviral agents.The [3H]amprenavir, [3H]saquinavir, [3H]ritonavir,...
Abstract The measurement of the urinary free cortisol–cortisone ratio has been reported to be a sensitive indicator renal 11 β ‐hydroxysteroid dehydrogenase type 2 (11 ‐HSD 2) activity. This converts biologically active cortisol inactive cortisone. A decrease in its activity (e.g. through disease or inhibition caused by therapeutic agent foodstuff) may increase levels and susceptibility towards hypertension. method presented here uses simple isocratic tandem column HPLC system. validated...
A small library of anilino enaminones was analyzed for potential anticonvulsant agents. We examined the effects three on neuronal activity output neurons, mitral cells (MC), in an olfactory bulb brain slice preparation using whole-cell patch-clamp recording. These compounds are known to be effective attenuating pentylenetetrazol-induced convulsions. Among tested, 5-methyl-3-(4-trifluoromethoxy-phenylamino)-cyclohex-2-enone (KRS-5Me-4-OCF<sub>3</sub>) showed potent inhibition MC with...
Summary: The anticonvulsant and toxic properties of methyl 4‐[( p ‐chlorophenyl)amino]‐6‐methyl‐2‐oxo‐cyclohex‐3‐en‐l‐oate (ADD 196022), were compared with those phenytoin (PHT), carbamazepine (CBZ), valproate (VPA). These compounds evaluated in mice rats using well‐standardized testing procedures. Results indicate that ADD 196022 is a very potent the maximal electroshock seizure (MES) model. compound was effective nontoxic doses after intraperitoneal (i.p.) administration oral rats. In...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis and anticonvulsant activity of imidooxy derivativesIvan O. Edafiogho, K. R. Scott, Jacqueline A. Moore, Vida Farrar, Jesse M. NicholsonCite this: J. Med. Chem. 1991, 34, 1, 387–392Publication Date (Print):January 1991Publication History Published online1 May 2002Published inissue 1 January 1991https://pubs.acs.org/doi/10.1021/jm00105a059https://doi.org/10.1021/jm00105a059research-articleACS PublicationsRequest reuse permissionsArticle...
Enaminones, enamines of B-dicarbonyl compounds have been known for many years. Their main therapeutic utility was as prodrugs various amines, stabilizing these active principally in basic media. Our laboratory discovered a series cyclic 1,3-diketo esters which were stable and possessed significant anticonvulsant activity. The most notable compound methyl 4- [(p chlorophenyl)amino)-6-methyl-2-oxocyclohex-3-en-1-oate, 15, desig nated ADD 196022 by the Anti-convulsant Drug Development (ADD)...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSpiro[4.5] and spiro[4.6] carboxylic acids: cyclic analogs of valproic acid synthesis anticonvulsant evaluationK. R. Scott, Jacqueline A. Moore, Theodore B. Zalucky, Jesse M. Nicholson, Jo Ann Lee, Christine N. HinkoCite this: J. Med. Chem. 1985, 28, 4, 413–417Publication Date (Print):April 1, 1985Publication History Published online1 May 2002Published inissue 1 April...
In 2012, 5‐(2‐aminopropyl)indole (5‐API, 5‐IT) was reported by Norwegian authorities to the European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) via Early Warning System (EWS). The 3‐ isomer, 3‐(2‐aminopropyl)indole (3‐API, AMT, alpha ‐methyltryptamine), has been available on recreational drugs market a somewhat longer time, having first EMCDDA Finnish in 2001. Both isomers are from online vendors of ‘legal highs’. Recently, three forensic drug cases (two tablets one powder) were...