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Start Over Author "McComas CC" Publisher elsevier science ltd
5 results on '"McComas CC"'

1. Structure-activity relationships of norepinephrine reuptake inhibitors with benzothiadiazine dioxide or dihydrosulfostyril cores.

Author

Fensome A, Goldberg J, McComas CC, Trybulski EJ, Woodworth RP, Deecher DC, Whiteside GT, and Zhang P

Subjects
Adrenergic Uptake Inhibitors chemical synthesis, Adrenergic Uptake Inhibitors pharmacology, Animals, Biological Transport, Cyclic S-Oxides chemical synthesis, Cyclic S-Oxides pharmacology, Humans, Microsomes, Liver metabolism, Models, Animal, Norepinephrine Plasma Membrane Transport Proteins metabolism, Rats, Structure-Activity Relationship, Thiazines chemical synthesis, Thiazines pharmacology, Adrenergic Uptake Inhibitors chemistry, Benzothiadiazines chemistry, Cyclic S-Oxides chemistry, Norepinephrine metabolism, Norepinephrine Plasma Membrane Transport Proteins chemistry, Thiazines chemistry
Abstract

Two related series of selective norepinephrine reuptake inhibitors were synthesized based on 3,4-dihydro-1H-2,1,3-benzothiadiazine 2,2-dioxide or 3,4-dihydrosulfostyril cores, and screened for monoamine reuptake inhibition. Structure-activity relationships were determined for the series' in vitro potency and selectivity versus serotonin or dopamine transporter inhibition, and analogs based on both cores were identified as potent and selective NRIs. The 3,4-dihydrosulfostyril series was further tested for microsome stability, and compound 16j, which was optimized for both potency and stability, showed efficacy in an in vivo model of thermoregulatory dysfunction., (Copyright 2010 Elsevier Ltd. All rights reserved.)

Published
2010
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2. Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.

Author

Zhang P, Terefenko EA, McComas CC, Mahaney PE, Vu A, Trybulski E, Koury E, Johnston G, Bray J, and Deecher D

Subjects
Benzimidazoles chemistry, Combinatorial Chemistry Techniques, Drug Design, Humans, Molecular Structure, Neurotransmitter Uptake Inhibitors chemistry, Norepinephrine metabolism, Stereoisomerism, Benzimidazoles chemical synthesis, Benzimidazoles pharmacology, Neurotransmitter Uptake Inhibitors chemical synthesis, Neurotransmitter Uptake Inhibitors pharmacology, Norepinephrine antagonists & inhibitors
Abstract

A series of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors was discovered. Several compounds such as 15 and 20 showed good hNET potency. Compounds 15 and 20 also displayed excellent selectivity at hNET that appeared superior to those of reboxetine and atomoxetine (4 and 5).

Published
2008
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3. Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.

Author

McComas CC, Vu AT, Mahaney PE, Cohn ST, Fensome A, Marella MA, Nogle L, Trybulski EJ, Ye F, Zhang P, Alfinito P, Bray J, Johnston G, Koury E, and Deecher DC

Subjects
Humans, Indoles chemistry, Molecular Structure, Neurotransmitter Uptake Inhibitors chemistry, Stereoisomerism, Structure-Activity Relationship, Indoles chemical synthesis, Indoles pharmacology, Neurotransmitter Uptake Inhibitors chemical synthesis, Neurotransmitter Uptake Inhibitors pharmacology, Norepinephrine antagonists & inhibitors
Abstract

Norepinephrine and serotonin play an important role in a wide variety of biological processes and are implicated in a number of neurological disorders. A novel class of 1-(3-amino-1-phenylpropyl)indolin-2-ones was designed and synthesized that displays potent norepinephrine reuptake inhibition while maintaining high selectivity (>100-fold) against the human serotonin and dopamine transporters.

Published
2008
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4. Synthesis and evaluation of methyl ether derivatives of the vancomycin, teicoplanin, and ristocetin aglycon methyl esters.

Author

McComas CC, Crowley BM, Hwang I, and Boger DL

Subjects
Enterococcus faecalis drug effects, Methyl Ethers chemical synthesis, Methyl Ethers pharmacology, Microbial Sensitivity Tests, Ristocetin chemical synthesis, Ristocetin pharmacology, Staphylococcus aureus drug effects, Structure-Activity Relationship, Teicoplanin chemical synthesis, Teicoplanin pharmacology, Vancomycin chemical synthesis, Vancomycin pharmacology, Vancomycin Resistance, Anti-Infective Agents chemical synthesis, Anti-Infective Agents pharmacology, Ristocetin analogs & derivatives, Teicoplanin analogs & derivatives, Vancomycin analogs & derivatives
Abstract

A series of methyl ether derivatives of the vancomycin, teicoplanin, and ristocetin aglycon methyl esters was synthesized and their antimicrobial activity was established. These derivatives exhibit increased activity against VanB resistant strains of bacteria equipotent with that observed with sensitive bacteria.

Published
2003
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5. A new and improved method for deglycosidation of glycopeptide antibiotics exemplified with vancomycin, ristocetin, and ramoplanin.

Author

Wanner J, Tang D, McComas CC, Crowley BM, Jiang W, Moss J, and Boger DL

Subjects
Chromatography, High Pressure Liquid, Hydrofluoric Acid, Indicators and Reagents, Pyridines chemistry, Solvents, Anti-Bacterial Agents chemistry, Depsipeptides, Peptides, Cyclic chemistry, Ristocetin chemistry, Vancomycin chemistry
Abstract

A general method for the deglycosidation of glycopeptide antibiotics has been developed. Treatment of vancomycin, ristocetin, and ramoplanin with anhydrous HF results in efficient cleavage of the sugars to provide the corresponding aglycons in high yield.

Published
2003
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