Kelvin Cooper

In vitro and in vivo characterization of Bisphosphocin Nu-3—a novel broad-spectrum antimicrobial compound with high potency against resistant pathogens

Kelvin Cooper, Kanneganti G. K. Murthy, Thomas Balzer, Steve Parkinson et autres

ABSTRACT Lakewood-Amedex Biotherapeutics Inc. has developed a new class of antimicrobials called the Bisphosphocin class, with Nu-3 as a leading candidate, which is currently in clinical development for treating mildly infected diabetic foot ulcers (iDFUs). Nu-3 acts through a novel mechanism of …

Novel Development of Predictive Feature Fingerprints to Identify Chemistry-Based Features for the Effective Drug Design of SARS-CoV-2 Target Antagonists and Inhibitors Using Machine Learning

Kelvin Cooper, Christopher Baddeley, Bernie French, Katherine Gibson et autres

A unique approach to bioactivity and chemical data curation coupled with random forest analyses has led to a series of target-specific and cross-validated predictive feature fingerprints (PFF) that have high predictability across multiple therapeutic targets and disease stages involved in the severe …

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Novel Development of Predictive Feature Fingerprints to Identify Chemistry-Based Features for Effective Drug Design of SARS-CoV-2 Target Antagonists and Inhibitors Using Machine Learning

Kelvin Cooper, Christopher J. Baddeley, Bernie French, Katherine Gibson et autres

A unique approach to bioactivity and chemical data curation coupled with Random forest analyses has led to a series of target-specific and cross-validated Predictive Feature Fingerprints (PFF) that have high predictability across multiple therapeutic targets and disease stages involved in the SARS-CoV-2 …

Novel Development of Predictive Feature Fingerprints to Identify Chemistry-Based Features for Effective Drug Design of SARS-CoV-2 Target Antagonists and Inhibitors Using Machine Learning

Kelvin Cooper, Christopher J. Baddeley, Bernie French, Katherine Gibson et autres

A unique approach to bioactivity and chemical data curation coupled with Random forest analyses has led to a series of target-specific and cross-validated Predictive Feature Fingerprints (PFF) that have high predictability across multiple therapeutic targets and disease stages involved in the SARS-CoV-2 …

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The challenge of new chemical entities attrition

Kelvin Cooper

The pharmaceutical industry is facing many challenges to the successful delivery of new medicines from its research and development (R&D) efforts. Central to these productivity challenges is the declining survival of small molecule drug candidates from the preclinical stage through to Food …

Correction to Discovery of the Hemifumarate and (α- l -Alanyloxy)methyl Ether as Prodrugs of an Antirheumatic Oxindole: Prodrugs for the Enolic OH Group

Ralph P. Robinson, Lawrence A. Reiter, Wayne E. Barth, Anthony M. Campeta et autres

Ether, ester, and carbonate derivatives of the antirheumatic oxindole 1 were prepared and screened as potential prodrugs of 1. This effort led to the discovery of the (alpha-L-alanyloxy)-methyl ether and hemifumarate derivatives of 1 which deliver the drug efficiently into the circulation …

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trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor

Lawrence A. Reiter, Kevin M. Koch, Anthony D. Piscopio, Henry J. Showell et autres

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The SAR of UK-78,282: A novel blocker of human T cell Kv1.3 potassium channels

Laurence E. Burgess, Kevin M. Koch, Kelvin Cooper, Michael S. Biggers et autres

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The development of non-steroidal dual inhibitors of both human 5α-reductase isozymes

Julian Blagg, Stephen A. Ballard, Kelvin Cooper, Paul W. Finn et autres

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ChemInform Abstract: Discovery of the Hemifumarate and (α‐L‐Alanyloxy)methyl Ether as Prodrugs of an Antirheumatic Oxindole: Prodrugs for the Enolic OH Group.

Ralph P. Robinson, Lawrence A. Reiter, Wayne E. Barth, Anthony M. Campeta et autres

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …

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Biarylcarboxylic Acids and -amides: Inhibition of Phosphodiesterase Type IV versus [3H]Rolipram Binding Activity and Their Relationship to Emetic Behavior in the Ferret

Allen J. Duplantier, Michael S. Biggers, Robert Chambers, John B. Cheng et autres

In addition to having desirable inhibitory effects on inflammation, anaphylaxis, and smooth muscle contraction, PDE-IV inhibitors also produce undesirable side effects including nausea and vomiting. In general, compounds that inhibit PDE-IV also potently displace [3H]rolipram from a high-affinity binding site in rat …

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Discovery of the Hemifumarate and (α- l -Alanyloxy)methyl Ether as Prodrugs of an Antirheumatic Oxindole: Prodrugs for the Enolic OH Group

Ralph P. Robinson, Lawrence A. Reiter, Wayne E. Barth, Anthony M. Campeta et autres

Ether, ester, and carbonate derivatives of the antirheumatic oxindole 1 were prepared and screened as potential prodrugs of 1 . This effort led to the discovery of the (α- l -alanyloxy)methyl ether and hemifumarate derivatives of 1 which deliver the drug efficiently …

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