A5063313711- Chemistry and Chemical Engineering
- Phosphodiesterase function and regulation
- Synthetic Organic Chemistry Methods
- Computational Drug Discovery Methods
- Cholinesterase and Neurodegenerative Diseases
- Chemical Synthesis and Analysis
- Receptor Mechanisms and Signaling
- Synthesis and Catalytic Reactions
- Trypanosoma species research and implications
- Click Chemistry and Applications
- Chemical synthesis and alkaloids
- Tea Polyphenols and Effects
- Oxidative Organic Chemistry Reactions
- Malaria Research and Control
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and Reactions of Organic Compounds
- Traditional and Medicinal Uses of Annonaceae
- Neurotransmitter Receptor Influence on Behavior
- Carbohydrate Chemistry and Synthesis
- Synthesis and Biological Evaluation
- Fluorine in Organic Chemistry
- Phytochemicals and Antioxidant Activities
- Pharmaceutical studies and practices
- Sexual function and dysfunction studies
- HIV/AIDS drug development and treatment
Montclair State University
2016-2025
Weatherford College
2013
Princeton University
2005-2010
Bristol-Myers Squibb (United States)
1999-2007
Lexicon Pharmaceuticals (United States)
2004-2005
Bristol-Myers Squibb (Germany)
2000-2002
Kyowa Kirin (Japan)
1997
University of Mississippi
1989-1994
Pennsylvania State University
1989-1991
University of Pittsburgh
1990
A series of 3,9-disubstituted [(alkylthio)methyl]- and (alkoxymethyl)-K-252a derivatives was synthesized with the aim enhancing separating neurotrophic properties from undesirable NGF (trk kinase) PKC inhibitory activities K-252a. Data this reveal that substitution in 3- 9-positions K-252a these groups reduces trk kinase approximately 100- to >500-fold while maintaining or certain cases activity. From research, 3,9-bis[(ethylthio)methyl]-K-252a (8) identified as a potent selective agent...
Controlling malaria requires new drugs against Plasmodium falciparum. The P. falciparum cGMP-dependent protein kinase (PfPKG) is a validated target whose inhibitors could block multiple steps of the parasite's life cycle. We defined structure–activity relationship (SAR) pyrrole series for PfPKG inhibition. Key pharmacophores were modified to enable full exploration chemical diversity and gain knowledge about an ideal core scaffold. In vitro potency recombinant human PKG used determine...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTMicrobial Metabolites of Ophiobolin A and Antimicrobial Evaluation OphiobolinsErguang Li, Alice M. Clark, David P. Rotella, Charles D. HuffordCite this: J. Nat. Prod. 1995, 58, 1, 74–81Publication Date (Print):January 1995Publication History Published online1 July 2004Published inissue 1 January 1995https://pubs.acs.org/doi/10.1021/np50115a009https://doi.org/10.1021/np50115a009research-articleACS PublicationsRequest reuse permissionsArticle...
(-)-Epigallocatechin 3-O-gallate (EGCG) a molecule found in green tea and known for plethora of bioactive properties is an inhibitor heat shock protein 90 (HSP90), interest as target cancer neuroprotection. Determination the spectral EGCG fluorescence environments similar to those binding sites proteins provides important tool directly study protein-EGCG interactions. The goal this examine aqueous buffer (AB) at pH=7.0, acetonitrile (AN) (a polar aprotic solvent), dimethylsulfoxide (DMSO)...
Malaria, toxoplasmosis, and cryptosporidiosis are caused by apicomplexan parasites Plasmodium spp., Toxoplasma gondii, Cryptosporidium parvum, respectively, pose major health challenges. Their therapies inadequate, ineffective or threatened drug resistance. The development of novel drugs against them requires innovative resource-efficient strategies. We exploited the kinome conservation these to determine cellular targets effects two falciparum inhibitors in T. gondii C. parvum. imidazoles,...
PDE11A is a little-studied phosphodiesterase family that breaks down cAMP and cGMP, with the PDE11A4 isoform enriched in memory-related hippocampus. Age-related increases hippocampal expression occur human rodents, causing age-related cognitive decline of social memories. Interestingly, this increase triggers liquid-liquid phase separation (LLPS), enzyme to accumulate brain filamentous structures termed ghost axons. Here we sought identify molecular mechanisms regulating LLPS therapeutic...
ADVERTISEMENT RETURN TO ISSUEPREVCommunicationNEXTSolid Phase Synthesis of Olefin and Hydroxyethylene PeptidomimeticsDavid P. RotellaView Author Information Department Chemistry, Cephalon, Inc. 145 Brandywine Parkway, West Chester, Pennsylvania 19380 Cite this: J. Am. Chem. Soc. 1996, 118, 48, 12246–12247Publication Date (Web):December 4, 1996Publication History Received5 July 1996Published online4 December inissue 1 January...
ADVERTISEMENT RETURN TO ISSUEPerspectiveNEXTNovel "Second-Generation" Approaches for the Control of Type 2 DiabetesDavid P. RotellaView Author Information Lexicon Pharmaceuticals, 350 Carter Road, Princeton, New Jersey 08540 Cite this: J. Med. Chem. 2004, 47, 17, 4111–4112Publication Date (Web):July 20, 2004Publication History Received24 December 2003Published online20 July 2004Published inissue 1 August...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTTotal synthesis of (.+-.)-dactylol and related studiesKen S. Feldman, Ming Jung Wu, David P. RotellaCite this: J. Am. Chem. Soc. 1990, 112, 23, 8490–8496Publication Date (Print):November 1, 1990Publication History Published online1 May 2002Published inissue 1 November 1990https://pubs.acs.org/doi/10.1021/ja00179a038https://doi.org/10.1021/ja00179a038research-articleACS PublicationsRequest reuse permissionsArticle Views529Altmetric-Citations40LEARN...
Phosphodiesterase type 5 (PDE5) inhibitors with improved PDE isozyme selectivity relative to sildenafil may result in agents for the treatment of male erectile dysfunction (MED) a lower incidence PDE-associated adverse effects. This paper describes discovery 14, PDE5 inhibitor potency and vitro compared sildenafil. compound shows activity functional assay function comparable that
Boceprevir was the first direct acting agent developed for treatment of hepatitis C virus infection. functions by targeting NS3 protease, a viral enzyme essential replication. This peptidomimetic molecule optimized from peptide lead to provide potent, selective and orally bioavailable drug that can be combined with ribavirin peg interferon achieve sustained response (undetectable HCV RNA levels 24 weeks after completion therapy) in patients infected Genotype 1 virus.This article provides...
Small molecules remain the backbone for modern drug discovery. They are conceived and synthesized by medicinal chemists, many of whom were originally trained as organic chemists. Support from government industry to provide training personnel continued development this critical skill set has been declining years. This Viewpoint highlights value chemistry chemists in complex journey discovery a reminder that basic science support must be restored.
The Alzheimer's disease amyloid peptide Aβ has a heterogeneous COOH terminus, as variants 40 and 42 residues long are found in neuritic plaques secreted constitutively by cultured cells. proteolytic activity that liberates the terminus from β-amyloid precursor protein is called γ-secretase. It could be one protease with dual specificity or two distinct enzymes. By using enzyme-linked immunosorbent assays selective for Aβ40 Aβ42, we have measured secretion HeLa cell line, examined dose...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTMechanistic and preparative studies of the intramolecular photocyclization methylated 2-(4-pentenyl)troponesKen S. Feldman, Jon H. Come, Benedict J. Kosmider, Pamela M. Smith, David P. Rotella, Ming Jung WuCite this: Org. Chem. 1989, 54, 3, 592–601Publication Date (Print):February 1, 1989Publication History Published online1 May 2002Published inissue 1 February...