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Your search keyword '"Stefan Menzler"' showing total 4 results
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4 results on '"Stefan Menzler"'

1. Synthesis of a non-peptide analogue of omega-conotoxin MVIIA

Author

Stefan Menzler, David Christopher Horwell, and Jack A Bikker

Subjects
chemistry.chemical_classification, biology, Voltage-dependent calcium channel, Peptidomimetic, Stereochemistry, Organic Chemistry, Conus magus, Ether, Cone shell, biology.organism_classification, Biochemistry, Combinatorial chemistry, Non peptide, Amino acid, chemistry.chemical_compound, Omega-conotoxin MVIIA, chemistry, Drug Discovery
Abstract

An efficient synthesis of an alkylphenyl ether based peptidomimetic is described. The compound mimics three key amino acids of omega-conotoxin MVIIA from the cone shell Conus magus and may provide an entry to the design of low molecular weight antagonists of N-type neuronal calcium channels.

Published
1998
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2. ChemInform Abstract: Synthesis of a Non-Peptide Analogue of Omega-Conotoxin MVIIA

Author

Jack A Bikker, David Christopher Horwell, and Stefan Menzler

Subjects
chemistry.chemical_classification, biology, Voltage-dependent calcium channel, Stereochemistry, Peptidomimetic, Conus magus, Ether, General Medicine, Cone shell, biology.organism_classification, Non peptide, Amino acid, chemistry.chemical_compound, Omega-conotoxin MVIIA, chemistry
Abstract

An efficient synthesis of an alkylphenyl ether based peptidomimetic is described. The compound mimics three key amino acids of omega-conotoxin MVIIA from the cone shell Conus magus and may provide an entry to the design of low molecular weight antagonists of N-type neuronal calcium channels.

Published
2010
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3. ChemInform Abstract: Design and Biological Evaluation of Non-Peptide Analogues of Omega-Conotoxin MVIIA

Author

Jack A Bikker, N. Suman-Chauhan, Stefan Menzler, and David Christopher Horwell

Subjects
chemistry.chemical_classification, Chemistry, Stereochemistry, Toxin, Antagonist, Ether, General Medicine, medicine.disease_cause, Non peptide, Amino acid, chemistry.chemical_compound, Omega-conotoxin MVIIA, Ic50 values, medicine, Biological evaluation
Abstract

Omega-conotoxin MVIIA, a highly potent antagonist of the N-type voltage sensitive calcium channel, has shown utility in several models of pain and ischemia. We report a series of three alkylphenyl ether based analogues which mimic three key amino acids of the toxin. Two of the compounds have been found to exhibit IC50 values of 2.7 and 3.3 μM at the human N-type voltage sensitive calcium channel.

Published
2010
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4. Design and biological evaluation of non-peptide analogues of omega-conotoxin MVIIA

Author

N. Suman-Chauhan, David Christopher Horwell, Stefan Menzler, and Jack A Bikker

Subjects
Models, Molecular, Calcium Channels, L-Type, Stereochemistry, Clinical Biochemistry, Snails, Pharmaceutical Science, chemistry.chemical_element, Mollusk Venoms, Ether, Calcium, Biochemistry, Chemical synthesis, omega-Conotoxins, Amidine, chemistry.chemical_compound, Inhibitory Concentration 50, Structure-Activity Relationship, Calcium Channels, N-Type, Drug Discovery, Animals, Molecular Biology, chemistry.chemical_classification, Phenyl Ethers, Organic Chemistry, Antagonist, Biological activity, Muscle, Smooth, Rats, Inbred Strains, Calcium Channel Blockers, In vitro, Amino acid, Rats, chemistry, Molecular Medicine, Drug Evaluation
Abstract

Omega-conotoxin MVIIA, a highly potent antagonist of the N-type voltage sensitive calcium channel, has shown utility in several models of pain and ischemia. We report a series of three alkylphenyl ether based analogues which mimic three key amino acids of the toxin. Two of the compounds have been found to exhibit IC50 values of 2.7 and 3.3 μM at the human N-type voltage sensitive calcium channel.

Published
2000

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