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Results: 1 to 10 of 18

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Antitrypanosomal Activity of Sterol 14α-Demethylase (CYP51) Inhibitors VNI and VFV in the Swiss Mouse Models of Chagas Disease Induced by the Trypanosoma cruzi Y Strain.
Guedes-da-Silva FH, Batista DG, Da Silva CF, De Araújo JS, Pavão BP, Simões-Silva MR, Batista MM, Demarque KC, Moreira OC, Britto C, Lepesheva GI, Soeiro MN
(2017) Antimicrob Agents Chemother 61:
MeSH Terms: 14-alpha Demethylase Inhibitors, Animals, Chagas Disease, Cyclophosphamide, Cytochrome P-450 Enzyme System, Disease Models, Animal, Drug Administration Schedule, Female, Gene Expression, Humans, Imidazoles, Immunosuppressive Agents, Male, Mice, Models, Molecular, Nitroimidazoles, Oxadiazoles, Parasite Load, Recurrence, Survival Analysis, Trypanocidal Agents, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
Different Therapeutic Outcomes of Benznidazole and VNI Treatments in Different Genders in Mouse Experimental Models of Trypanosoma cruzi Infection.
Guedes-da-Silva FH, Batista DG, da Silva CF, Meuser MB, Simões-Silva MR, de Araújo JS, Ferreira CG, Moreira OC, Britto C, Lepesheva GI, Soeiro Mde N
(2015) Antimicrob Agents Chemother 59: 7564-70
MeSH Terms: 14-alpha Demethylase Inhibitors, Animals, Chagas Disease, Cytochrome P-450 Enzyme System, Disease Models, Animal, Drug Administration Schedule, Drug Evaluation, Preclinical, Female, Gene Expression, Imidazoles, Immunosuppressive Agents, Male, Mice, Nitroimidazoles, Oxadiazoles, Parasitemia, Sex Factors, Treatment Outcome, Trypanocidal Agents, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis.
Lepesheva GI, Hargrove TY, Rachakonda G, Wawrzak Z, Pomel S, Cojean S, Nde PN, Nes WD, Locuson CW, Calcutt MW, Waterman MR, Daniels JS, Loiseau PM, Villalta F
(2015) J Infect Dis 212: 1439-48
MeSH Terms: Animals, Antiprotozoal Agents, Benzamides, Biotransformation, Chagas Disease, Cytochrome P-450 Enzyme Inhibitors, Cytochrome P-450 Enzyme System, Disease Models, Animal, Female, Humans, Imidazoles, Inhibitory Concentration 50, Leishmaniasis, Visceral, Mice, Mice, Inbred BALB C, Microsomes, Liver, Molecular Structure, Oxadiazoles, Rats, Structure-Activity Relationship, Tissue Distribution, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
The melanocortin-4 receptor is expressed in enteroendocrine L cells and regulates the release of peptide YY and glucagon-like peptide 1 in vivo.
Panaro BL, Tough IR, Engelstoft MS, Matthews RT, Digby GJ, Møller CL, Svendsen B, Gribble F, Reimann F, Holst JJ, Holst B, Schwartz TW, Cox HM, Cone RD
(2014) Cell Metab 20: 1018-29
MeSH Terms: Acids, Heterocyclic, Animals, Colon, Enteroendocrine Cells, Glucagon-Like Peptide 1, Humans, Immunohistochemistry, Mice, Mice, Inbred C57BL, Mice, Transgenic, Oxadiazoles, Peptide YY, Peptides, Cyclic, Receptor, Melanocortin, Type 4
Added January 20, 2015
0 Communities
2 Members
0 Resources
14 MeSH Terms
Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning.
Xu J, Zhu Y, Kraniotis S, He Q, Marshall JJ, Nomura T, Stauffer SR, Lindsley CW, Conn PJ, Contractor A
(2013) Learn Mem 20: 438-45
MeSH Terms: Adaptation, Psychological, Animals, Extinction, Psychological, Hippocampus, Long-Term Synaptic Depression, Male, Maze Learning, Mice, Mice, Inbred C57BL, Mice, Knockout, Oxadiazoles, Piperidines, Receptor, Metabotropic Glutamate 5
Added February 19, 2015
0 Communities
1 Members
0 Resources
13 MeSH Terms
In vitro and in vivo studies of the antiparasitic activity of sterol 14α-demethylase (CYP51) inhibitor VNI against drug-resistant strains of Trypanosoma cruzi.
Soeiro Mde N, de Souza EM, da Silva CF, Batista Dda G, Batista MM, Pavão BP, Araújo JS, Aiub CA, da Silva PB, Lionel J, Britto C, Kim K, Sulikowski G, Hargrove TY, Waterman MR, Lepesheva GI
(2013) Antimicrob Agents Chemother 57: 4151-63
MeSH Terms: 14-alpha Demethylase Inhibitors, Animals, Chagas Disease, Drug Resistance, Endoplasmic Reticulum, Golgi Apparatus, Imidazoles, Male, Mice, Microscopy, Electron, Transmission, Nitroimidazoles, Oxadiazoles, Protozoan Proteins, Sterol 14-Demethylase, Thiazoles, Triazoles, Trypanocidal Agents, Trypanosoma cruzi
Added March 7, 2014
0 Communities
2 Members
0 Resources
18 MeSH Terms
VNI cures acute and chronic experimental Chagas disease.
Villalta F, Dobish MC, Nde PN, Kleshchenko YY, Hargrove TY, Johnson CA, Waterman MR, Johnston JN, Lepesheva GI
(2013) J Infect Dis 208: 504-11
MeSH Terms: Administration, Oral, Animals, Chagas Disease, Chronic Disease, Disease Models, Animal, Enzyme Inhibitors, Female, Imidazoles, Mice, Mice, Inbred BALB C, Oxadiazoles, Survival Analysis, Treatment Outcome
Added March 7, 2014
0 Communities
2 Members
0 Resources
13 MeSH Terms
Organocatalytic, enantioselective synthesis of VNI: a robust therapeutic development platform for Chagas, a neglected tropical disease.
Dobish MC, Villalta F, Waterman MR, Lepesheva GI, Johnston JN
(2012) Org Lett 14: 6322-5
MeSH Terms: Animals, Chagas Disease, Cytochrome P-450 Enzyme Inhibitors, Cytochrome P-450 Enzyme System, Imidazoles, Mice, Molecular Structure, Neglected Diseases, Oxadiazoles, Triazoles, Tropical Medicine, Trypanosoma cruzi
Added February 12, 2015
0 Communities
2 Members
0 Resources
12 MeSH Terms
Total synthesis and biological evaluation of phidianidines A and B uncovers unique pharmacological profiles at CNS targets.
Brogan JT, Stoops SL, Lindsley CW
(2012) ACS Chem Neurosci 3: 658-64
MeSH Terms: Animals, CHO Cells, Cell Proliferation, Cell Survival, Central Nervous System Agents, Chromatography, High Pressure Liquid, Cricetinae, Cricetulus, Dopamine Plasma Membrane Transport Proteins, Gastropoda, Guanosine 5'-O-(3-Thiotriphosphate), HEK293 Cells, Humans, Indicators and Reagents, Indole Alkaloids, Ligands, Oxadiazoles, Radioligand Assay, Receptors, Opioid, mu, Serotonin Plasma Membrane Transport Proteins, Structure-Activity Relationship
Added March 7, 2014
1 Communities
1 Members
0 Resources
21 MeSH Terms
Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists.
Lamb JP, Engers DW, Niswender CM, Rodriguez AL, Venable DF, Conn PJ, Lindsley CW
(2011) Bioorg Med Chem Lett 21: 2711-4
MeSH Terms: Allosteric Regulation, Drug Discovery, Molecular Structure, Oxadiazoles, Piperidines, Protein Binding, Receptor, Metabotropic Glutamate 5, Receptors, Metabotropic Glutamate, Stereoisomerism, Structure-Activity Relationship
Added February 19, 2015
0 Communities
2 Members
0 Resources
10 MeSH Terms