Research Interests: Organic Chemistry, DNA, Humans, Melanocortin receptor, Chronic myeloid leukemia, and 11 moreAmides, DNA binding, Benzoic Acid, Molecular Conformation, Alkylation, Bioorganic and medicinal Chemistry, Structure activity Relationship, Antineoplastic Agents, Anticancer Drug, Piperidines, and Binding affinity
Research Interests:
Research Interests:
Research Interests:
Research Interests:
Research Interests:
Piperazinebenzylamines bearing a small N-(1-methoxy-2-propyl) side chain were found to be potent and selective antagonists of the human melanocortin-4 (MC4) receptor. Compound 7b, having K(i) values of 6.9 and 2800 nM at the human MC4 and... more
Piperazinebenzylamines bearing a small N-(1-methoxy-2-propyl) side chain were found to be potent and selective antagonists of the human melanocortin-4 (MC4) receptor. Compound 7b, having K(i) values of 6.9 and 2800 nM at the human MC4 and MC3 receptors, respectively, has moderate oral bioavailability in mice, which is improved relative to the arylethyl analogues.
Research Interests:
Research Interests:
Research Interests: Organic Chemistry, Macromolecular X-Ray Crystallography, Dogs, Humans, Mice, and 15 moreAnimals, Male, Food intake, Melanocortin receptor, Caco-2 cells, Rats, Time Factors, Cachexia, Amino Acid Profile, Molecular Conformation, Bioorganic and medicinal Chemistry, Structure activity Relationship, Caco 2 Cell, Weight Gain, and Binding affinity
Research Interests:
... Wanlong Jianga, Joseph Pontilloa, Dragan Marinkovica, Nicole S. Whitea, Melissa Arellanoa, Beth A. Fleckb, Jenny Wenc, John Saundersa, Alan C. Fosterd ... administration [3]. While 1a displays relatively good in vitro metabolic... more
... Wanlong Jianga, Joseph Pontilloa, Dragan Marinkovica, Nicole S. Whitea, Melissa Arellanoa, Beth A. Fleckb, Jenny Wenc, John Saundersa, Alan C. Fosterd ... administration [3]. While 1a displays relatively good in vitro metabolic stability in human liver microsomes (CLint = 23 mL ...
Research Interests:
A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain... more
A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain penetration in mice.
Research Interests:
Research Interests:
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the alpha-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu... more
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the alpha-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or beta-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.
Research Interests:
Research Interests:
A potent and selective antagonist of the melanocortin-4 receptor, 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-6-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine (10d), was identified from a series... more
A potent and selective antagonist of the melanocortin-4 receptor, 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-6-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine (10d), was identified from a series piperazinebenzylamine attached with a N,N-dimethyl-beta-alanine side chain. This compound possessed high water solubility and exhibited good metabolic profiles. In animals, 10d showed moderate to good oral bioavailability and promoted food intake in tumor-bearing mice after oral administration.
Research Interests:
Research Interests:
Research Interests:
Research Interests: Organic Chemistry, Treatment, Pharmacokinetics, In Vitro, Humans, and 17 moreMice, Animals, Body Composition, Male, Animal Model, Bioavailability, In Vivo, Melanocortin receptor, Cachexia, Body Weight, Bioorganic and medicinal Chemistry, Affinity, Structure activity Relationship, Biological Availability, Chemical Synthesis, Molecular Structure, and Selectivity
Research Interests: Organic Chemistry, Immunology, Rheumatoid Arthritis, Immunology of the Gut, Cell line, and 17 moreHumans, Mice, Chronic Disease, Female, Animals, Urea, The, Feeding Behavior, Food intake, Neutrophils, Melanocortin receptor, Lipopolysaccharides, Bioorganic and medicinal Chemistry, Rabbits, Recombinant Proteins, Interleukin, and Acute Disease
Research Interests:
Research Interests: Organic Chemistry, DNA, Humans, Melanocortin receptor, Chronic myeloid leukemia, and 11 moreAmides, DNA binding, Benzoic Acid, Molecular Conformation, Alkylation, Bioorganic and medicinal Chemistry, Structure activity Relationship, Antineoplastic Agents, Anticancer Drug, Piperidines, and Binding affinity
Research Interests:
Research Interests:
Research Interests:
Research Interests:
Research Interests:
Piperazinebenzylamines bearing a small N-(1-methoxy-2-propyl) side chain were found to be potent and selective antagonists of the human melanocortin-4 (MC4) receptor. Compound 7b, having K(i) values of 6.9 and 2800 nM at the human MC4 and... more
Piperazinebenzylamines bearing a small N-(1-methoxy-2-propyl) side chain were found to be potent and selective antagonists of the human melanocortin-4 (MC4) receptor. Compound 7b, having K(i) values of 6.9 and 2800 nM at the human MC4 and MC3 receptors, respectively, has moderate oral bioavailability in mice, which is improved relative to the arylethyl analogues.
Research Interests:
Research Interests:
Research Interests: Organic Chemistry, Macromolecular X-Ray Crystallography, Dogs, Humans, Mice, and 15 moreAnimals, Male, Food intake, Melanocortin receptor, Caco-2 cells, Rats, Time Factors, Cachexia, Amino Acid Profile, Molecular Conformation, Bioorganic and medicinal Chemistry, Structure activity Relationship, Caco 2 Cell, Weight Gain, and Binding affinity
Research Interests:
... Wanlong Jianga, Joseph Pontilloa, Dragan Marinkovica, Nicole S. Whitea, Melissa Arellanoa, Beth A. Fleckb, Jenny Wenc, John Saundersa, Alan C. Fosterd ... administration [3]. While 1a displays relatively good in vitro metabolic... more
... Wanlong Jianga, Joseph Pontilloa, Dragan Marinkovica, Nicole S. Whitea, Melissa Arellanoa, Beth A. Fleckb, Jenny Wenc, John Saundersa, Alan C. Fosterd ... administration [3]. While 1a displays relatively good in vitro metabolic stability in human liver microsomes (CLint = 23 mL ...
Research Interests:
A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain... more
A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain penetration in mice.
Research Interests:
Research Interests:
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the alpha-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu... more
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the alpha-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or beta-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.
Research Interests:
Research Interests:
A potent and selective antagonist of the melanocortin-4 receptor, 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-6-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine (10d), was identified from a series... more
A potent and selective antagonist of the melanocortin-4 receptor, 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-6-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine (10d), was identified from a series piperazinebenzylamine attached with a N,N-dimethyl-beta-alanine side chain. This compound possessed high water solubility and exhibited good metabolic profiles. In animals, 10d showed moderate to good oral bioavailability and promoted food intake in tumor-bearing mice after oral administration.