• 1207 Citations
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1987 …2018
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Research Output 1987 2018

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2018
1 Citation (Scopus)

Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis

Tummalapalli, S. R., Bhat, R., Chojnowski, A., Prorok, M., Kreiss, T., Goldberg, R., Canan, S., Hawryluk, N., Mortensen, D., Khetani, V., Zeldis, J., Siekierka, J. & Rotella, D., 8 Mar 2018, In : ACS Medicinal Chemistry Letters. 9, 3, p. 210-214 5 p.

Research output: Contribution to journalArticle

Filarial Elephantiasis
Structure-Activity Relationship
Protein Kinase Inhibitors
Heat-Shock Proteins
Protein Kinases
1 Citation (Scopus)

Expression, purification, and inhibition profile of dihydrofolate reductase from the filarial nematode Wuchereria bancrofti

Tobias, A. M., Toska, D., Lange, K., Eck, T., Bhat, R., Janson, C. A., Rotella, D. P., Gubler, U. & Goodey, N. M., May 2018, In : PLoS ONE. 13, 5, e0197173.

Research output: Contribution to journalArticle

Wuchereria bancrofti
Aminopterin
dihydrofolate reductase
Folic Acid Antagonists
Tetrahydrofolate Dehydrogenase
2017
4 Citations (Scopus)

Mechanism of inhibition of botulinum neurotoxin type A light chain by two quinolinol compounds

Minnow, Y. V. T., Goldberg, R., Tummalapalli, S. R., Rotella, D. P. & Goodey, N. M., 15 Mar 2017, In : Archives of Biochemistry and Biophysics. 618, p. 15-22 8 p.

Research output: Contribution to journalArticle

Hydroxyquinolines
Type A Botulinum Toxins
Light
Tetanus Toxin
Structure-Activity Relationship

Synthesis and computational analysis of conformationally restricted [3.2.2]- and [3.2.1]-3-azabicyclic diamines

Tummalapalli, S. R., Bhat, R., Waitt, C., Eshuis, H. & Rotella, D. P., 1 Jan 2017, In : Tetrahedron Letters. 58, 43, p. 4087-4089 3 p.

Research output: Contribution to journalArticle

Organic Chemistry
Diamines
Pharmaceutical Chemistry
Scaffolds
Computer Simulation
2014
9 Citations (Scopus)

Structure-activity studies of (-)-epigallocatechin gallate derivatives as HCV entry inhibitors

Bhat, R., Adam, A. T., Lee, J. J., Deloison, G., Rouillé, Y., Séron, K. & Rotella, D. P., 1 Sep 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 17, p. 4162-4165 4 p.

Research output: Contribution to journalArticle

Virus Internalization
Viruses
Hepacivirus
Derivatives
Pharmaceutical Preparations
8 Citations (Scopus)

Towards the discovery of drug-like epigallocatechin gallate analogs as Hsp90 inhibitors

Bhat, R., Adam, A. T., Lee, J. J., Gasiewicz, T. A., Henry, E. C. & Rotella, D. P., 15 May 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 10, p. 2263-2266 4 p.

Research output: Contribution to journalArticle

Drug Discovery
Esters
Pharmaceutical Preparations
Hydroxyl Radical
Stereochemistry
2013
13 Citations (Scopus)

The spectral properties of (-)-epigallocatechin 3-O-gallate (EGCG) fluorescence in different solvents: Dependence on solvent polarity

Snitsarev, V., Young, M. N., Miller, R. M. S. & Rotella, D. P., 22 Nov 2013, In : PLoS ONE. 8, 11, e79834.

Research output: Contribution to journalArticle

epigallocatechin
Fluorescence
fluorescence
dimethyl sulfoxide
Dimethyl Sulfoxide
2010
12 Citations (Scopus)

Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia

Yan, Y., Zhou, P., Rotella, D. P., Feenstra, R., Kruse, C. G., Reinders, J. H., Neut, M. V. D., Lai, M., Zhang, J., Kowal, D. M., Carrick, T., Marquis, K. L., Pausch, M. H. & Robichaud, A. J., 1 May 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 9, p. 2983-2986 4 p.

Research output: Contribution to journalArticle

Serotonin Uptake Inhibitors
Dopamine
Schizophrenia
Amines
Ligands
12 Citations (Scopus)

WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol- 2(3H)-one]: A novel dopamine D2 receptor partial agonist/serotonin reuptake inhibitor with preclinical antipsychotic-like and antidepressant-like activity

Brennan, J. A., Graf, R., Grauer, S. M., Navarra, R. L., Pulicicchio, C. M., Hughes, Z. A., Lin, Q., Wantuch, C., Rosenzweig-Lipson, S., Pruthi, F., Lai, M., Smith, D., Goutier, W., Van De Neut, M., Robichaud, A. J., Rotella, D., Feenstra, R. W., Kruse, C., Broqua, P., Beyer, C. E. & 3 others, McCreary, A. C., Pausch, M. H. & Marquis, K. L., 1 Jan 2010, In : Journal of Pharmacology and Experimental Therapeutics. 332, 1, p. 190-201 12 p.

Research output: Contribution to journalArticle

Dopamine D2 Receptors
Serotonin Uptake Inhibitors
Antidepressive Agents
Antipsychotic Agents
Serotonin Plasma Membrane Transport Proteins
2009

American chemical society - 238th national meeting & exposition. Novel small molecule therapeutics

Rotella, D., 1 Oct 2009, In : IDrugs. 12, 10, p. 612-613 2 p.

Research output: Contribution to journalArticle

Purinergic P1 Receptor Agonists
PAR-2 Receptor
Purinergic P1 Receptor Antagonists
Anti-Inflammatory Agents
Therapeutics
14 Citations (Scopus)

Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia

Rotella, D. P., McFarlane, G. R., Greenfield, A., Grosanu, C., Robichaud, A. J., Denny, R. A., Feenstra, R. W., Núñez-García, S., Reinders, J. H., Neut, M. V. D., McCreary, A., Kruse, C. G., Sullivan, K., Pruthi, F., Lai, M., Zhang, J., Kowal, D. M., Carrick, T., Grauer, S. M., Navarra, R. L. & 4 others, Graf, R., Brennan, J., Marquis, K. L. & Pausch, M. H., 1 Oct 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 19, p. 5552-5555 4 p.

Research output: Contribution to journalArticle

Serotonin Uptake Inhibitors
Dopamine
Schizophrenia
Dopamine D2 Receptors
Assays
2008

American Chemical Society - 235th national meeting: Part 3

Rotella, D., 1 Jun 2008, In : IDrugs. 11, 6, p. 394-396 3 p.

Research output: Contribution to journalArticle

Proto-Oncogene Proteins c-bcl-2
Antidiarrheals
Cystic Fibrosis Transmembrane Conductance Regulator
Urokinase-Type Plasminogen Activator
Drug Industry

American Chemical Society - 236th National Meeting & Exposition. Drug development for tuberculosis and cancer

Rotella, D., 1 Oct 2008, In : IDrugs. 11, 10, p. 699-701 3 p.

Research output: Contribution to journalArticle

Proto-Oncogene Proteins c-met
Vinca Alkaloids
Antitubercular Agents
Kinesin
Preclinical Drug Evaluations

American Chemical Society - 236th National Meeting & Exposition. New Frontiers in Drug Delivery

Rotella, D., 1 Oct 2008, In : IDrugs. 11, 10, p. 702-704 3 p.

Research output: Contribution to journalArticle

Peritoneal Diseases
Drug-Eluting Stents
Eye Diseases
Drug Delivery Systems
RNA Interference

Medicinal Chemistry - XXth International Symposium. Lead finding strategies and kinase selectivity

Rotella, D., 1 Nov 2008, In : IDrugs. 11, 11, p. 774-778 5 p.

Research output: Contribution to journalArticle

Preclinical Drug Evaluations
Pharmaceutical Chemistry
Drug Design
Enzyme Inhibitors
Antineoplastic Agents

Medicinal Chemistry - XXth International Symposium. Natural products and neurodegenerative diseases

Rotella, D., 1 Nov 2008, In : IDrugs. 11, 11, p. 779-782 4 p.

Research output: Contribution to journalArticle

Glycogen Synthase
Pharmaceutical Chemistry
Enzyme Inhibitors
Medicinal Plants
Biological Products
2007

American Chemical Society - 233rd national meeting. CNS, cancer and cardiovascular targets

Rotella, D., 1 May 2007, In : IDrugs. 10, 5, p. 310-312 3 p.

Research output: Contribution to journalArticle

CD18 Antigens
CD11b Antigens
Piperazines
Lobeline
Vesicular Monoamine Transport Proteins

American Chemical Society - 234th National meeting - Syntheses of novel compounds and data on novel therapeutics

Rotella, D., 1 Oct 2007, In : IDrugs. 10, 10, p. 681-685 5 p.

Research output: Contribution to journalArticle

Adrenergic Uptake Inhibitors
Janus Kinase 3
HSP90 Heat-Shock Proteins
Thiazoles
PPAR alpha
23 Citations (Scopus)

Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors

Simpkins, L. M., Bolton, S., Pi, Z., Sutton, J. C., Kwon, C., Zhao, G., Magnin, D. R., Augeri, D. J., Gungor, T., Rotella, D. P., Sun, Z., Liu, Y., Slusarchyk, W. S., Marcinkeviciene, J., Robertson, J. G., Wang, A., Robl, J. A., Atwal, K. S., Zahler, R. L., Parker, R. A. & 2 others, Kirby, M. S. & Hamann, L. G., 1 Dec 2007, In : Bioorganic and Medicinal Chemistry Letters. 17, 23, p. 6476-6480 5 p.

Research output: Contribution to journalArticle

Dipeptidyl-Peptidase IV Inhibitors
Structure-Activity Relationship
Scaffolds
Nitrogen
Amino Acids
2006
Biological Models
PPAR gamma
Opioid Receptors
G-Protein-Coupled Receptors
Gene Library
Pharmaceutical Chemistry
1 Citation (Scopus)
Aspartic Acid Endopeptidases
Endopeptidases
Amyloid Precursor Protein Secretases
Preclinical Drug Evaluations
Enzyme Inhibitors

American chemical society 232nd national meeting. 10-14 September 2006, San Francisco, CA, USA

Rotella, D., 1 Nov 2006, In : IDrugs. 9, 11, p. 745-747 3 p.

Research output: Contribution to journalArticle

Aminoquinolines
Potassium Channel Blockers
Benzimidazoles
Investigational Drugs
MAP Kinase Kinase Kinases
1 Citation (Scopus)

COMP-Structure-Based Design and Development of Estrogen Receptor Modulators. 10-14 September 2006, San Francisco, CA, USA

Rotella, D., 1 Nov 2006, In : IDrugs. 9, 11, p. 748-750 3 p.

Research output: Contribution to journalArticle

Oxazoles
Investigational Drugs
Selective Estrogen Receptor Modulators
Estrogen Receptor beta
Molecular Models
2005

American Chemical Society - 229th National Meeting. Bench to pilot plant: 13-17 March 2005, San Diego, CA, USA

Rotella, D., 1 May 2005, In : IDrugs. 8, 5, p. 390-391 2 p.

Research output: Contribution to journalArticle

3',5'-Cyclic-AMP Phosphodiesterases
Pharmaceutical Technology
Phosphodiesterase Inhibitors
Pharmaceutical Chemistry
Chronic Obstructive Pulmonary Disease

American Chemical Society - 229th National Meeting. Carbohydrate vaccines: 13-17 March 2005, San Diego, CA, USA

Rotella, D., 1 May 2005, In : IDrugs. 8, 5, p. 387-389 3 p.

Research output: Contribution to journalArticle

AIDS Vaccines
Cancer Vaccines
Synthetic Vaccines
Vaccines
Carbohydrates

American Chemical Society - 230th National Meeting Medicinal chemistry. 28 August - 1 September 2005, Washington, DC, USA

Rotella, D., 1 Nov 2005, In : IDrugs. 8, 11, p. 871-875 5 p.

Research output: Contribution to journalArticle

Viral Nonstructural Proteins
Prostaglandin E Receptors
Protein Tyrosine Phosphatases
Pharmaceutical Chemistry
Drug Design
42 Citations (Scopus)

Discovery and structure-activity relationships of 2-benzylpyrrolidine- substituted aryloxypropanols as calcium-sensing receptor antagonists

Yang, W., Wang, Y., Roberge, J. Y., Ma, Z., Liu, Y., Lawrence, R. M., Rotella, D., Seethala, R., Feyen, J. H. M. & Dickson, J. K., 15 Feb 2005, In : Bioorganic and Medicinal Chemistry Letters. 15, 4, p. 1225-1228 4 p.

Research output: Contribution to journalArticle

Calcium-Sensing Receptors
Structure-Activity Relationship
Ether
Amines
Genes

Proteins, peptides, amino acids and enzyme inhibitors. 28 August - 1 September 2005, Washington, DC, USA

Rotella, D., 1 Nov 2005, In : IDrugs. 8, 11, p. 878-879 2 p.

Research output: Contribution to journalArticle

Amino Acids, Peptides, and Proteins
Depsipeptides
Protein Folding
Enzyme Inhibitors
Amino Acids

Technical achievements in organic chemistry. 28 August - 1 September 2005, Washington, DC, USA

Rotella, D., 1 Nov 2005, In : IDrugs. 8, 11, p. 876-877 2 p.

Research output: Contribution to journalArticle

Integrin alphaVbeta3
Organic Chemistry
HIV Protease Inhibitors
Enzyme Inhibitors
Caspases
2004
Molecular Mimicry
Phosphotyrosine
Hydrogels
Hypoglycemic Agents
Blood Glucose
Carbazoles
Antiparkinson Agents
Indoles
Prodrugs
Neuroprotective Agents
Memantine
Excitatory Amino Acid Antagonists
Drug Design
Drug Industry
N-Methyl-D-Aspartate Receptors

American Chemical Society - 228th National meeting. Technical achievements in organic synthesis

Rotella, D., 1 Oct 2004, In : IDrugs. 7, 10, p. 889-892 4 p.

Research output: Contribution to journalArticle

Organic Chemistry
Organic Chemicals
Synthetic Chemistry Techniques
Pharmaceutical Preparations

Wolfrom/Isbell New Investigator Award Symposium

Rotella, D. P., 1 Oct 2004, In : IDrugs. 7, 10, p. 893-894 2 p.

Research output: Contribution to journalArticle

AIDS Vaccines
Nucleosides
Oligonucleotides
Carbohydrates
Research Personnel
2002
Osteoporosis

American Chemical Society - 223rd National Meeting: New Clinical Candidates: 7-11 April 2002, Orlando, FL, USA

Rotella, D., 1 Dec 2002, In : IDrugs. 5, 5, p. 430-432 3 p.

Research output: Contribution to journalArticle

2000

A cholesterol ester transfer protein inhibitor attenuates atherosclerosis in rabbits

Rotella, D., 22 Nov 2000, In : Chemtracts. 13, 9, p. 630-632 3 p.

Research output: Contribution to journalArticle

Cholesterol Ester Transfer Proteins
2 Citations (Scopus)
Amyloid Precursor Protein Secretases
Amyloid beta-Peptides
Sulfonamides
Brain
Molecules
53 Citations (Scopus)

N-3-substituted imidazoquinazolinones: Potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction

Rotella, D., Sun, Z., Zhu, Y., Krupinski, J., Pongrac, R., Seliger, L., Normandin, D. & Macor, J. E., 6 Apr 2000, In : Journal of Medicinal Chemistry. 43, 7, p. 1257-1263 7 p.

Research output: Contribution to journalArticle

Phosphodiesterase 5 Inhibitors
Erectile Dysfunction
Isoenzymes
Incidence
Sildenafil Citrate
34 Citations (Scopus)

Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors

Rotella, D. P., Sun, Z., Zhu, Y., Krupinski, J., Pongrac, R., Seliger, L., Normandin, D. & Macor, J. E., 28 Dec 2000, In : Journal of Medicinal Chemistry. 43, 26, p. 5037-5043 7 p.

Research output: Contribution to journalArticle

Phosphodiesterase 5 Inhibitors
Sulfonamides
Structure-Activity Relationship
Pharmacokinetics
Enzymes
1999
44 Citations (Scopus)

Rank-order of potencies for inhibition of the secretion of Aβ40 and Aβ42 suggests that both are generated by a single γ-secretase

Durkin, J. T., Murthy, S., Husten, E. J., Trusko, S. P., Savage, M. J., Rotella, D., Greenberg, B. D. & Siman, R., 16 Jul 1999, In : Journal of Biological Chemistry. 274, 29, p. 20499-20504 6 p.

Research output: Contribution to journalArticle

Amyloid Precursor Protein Secretases
Amyloid beta-Protein Precursor
Cells
Derivatives
Immunosorbents
1998
1 Citation (Scopus)

Novel biologically active nonpeptidic inhibitors of myristoyl-CoA:protein N-myristoyltransferase

Rotella, D. P., 1 Aug 1998, In : Chemtracts. 11, 9, p. 667-670 4 p.

Research output: Contribution to journalArticle

glycylpeptide N-tetradecanoyltransferase
1997
1 Citation (Scopus)

Antibacterial agents that inhibit lipid A biosynthesis

Rotella, D. P., 1 Dec 1997, In : Chemtracts. 10, 9, p. 665-668 4 p.

Research output: Contribution to journalArticle

Lipid A
Biosynthesis
Anti-Bacterial Agents
1 Citation (Scopus)
Neuraminidase
N-Acetylneuraminic Acid
Structural analysis
Enzymes
Leukotriene A4
Hydrolases
Neutrophils
Enzymes
116 Citations (Scopus)

Neurotrophic 3,9-bis[(alkylthio)methyl]-and-bis(alkoxymethyl)-K-252a derivatives

Kaneko, M., Saito, Y., Saito, H., Matsumoto, T., Matsuda, Y., Vaught, J. L., Dionne, C. A., Angeles, T. S., Glicksman, M. A., Neff, N. T., Rotella, D. P., Kauer, J. C., Mallamo, J. P., Hudkins, R. L. & Murakata, C., 6 Jun 1997, In : Journal of Medicinal Chemistry. 40, 12, p. 1863-1869 7 p.

Research output: Contribution to journalArticle

Phosphotransferases
Motor Neurons
Neurological Models
Basal Nucleus of Meynert
Myosin-Light-Chain Kinase

Phosphinate inhibitors of the D-glutamic acid-adding enzyme of peptidoglycan biosynthesis

Rotella, D., 1 Dec 1997, In : Chemtracts. 10, 4, p. 325-327 3 p.

Research output: Contribution to journalArticle

Peptidoglycan
Biosynthesis
UDP-N-acetylmuramoylalanine-D-glutamate ligase

The carboxy termini of β-amyloid peptides I-40 and I-42 are generated by distinct γ-secretase activities

Rotella, D., 1 Dec 1997, In : Chemtracts. 10, 9, p. 669-672 4 p.

Research output: Contribution to journalArticle

Amyloid Precursor Protein Secretases
Amyloid beta-Peptides
1996
7 Citations (Scopus)

Facile Lewis Acid-Mediated Ring Opening of 4-Hydroxypyrrolidin-2-ones by Amino Acid Esters

Rotella, D., 1 Jan 1996, In : Synlett. 1996, 5, p. 479-480 2 p.

Research output: Contribution to journalArticle

Lewis Acids
Dipeptides
Esters
Amino Acids
hydroxyethylene