Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine. 2000

A P Tamiz, and M P Smith, and A P Kozikowski
Drug Discovery Program, Institute of Cognitive and Comuputational Science, Georgetown University Medical Center, Washington, DC 20007-2197, USA.

The synthesis and biological activity of a series of azatricyclodecane analogues of cocaine are described. All compounds studied in this series exhibit nanomolar potency and good selectivity for the serotonin transporter versus the dopamine transporter.

UI MeSH Term Description Entries
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D003042 Cocaine An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. Cocaine HCl,Cocaine Hydrochloride,HCl, Cocaine,Hydrochloride, Cocaine
D006575 Heterocyclic Compounds, 3-Ring A class of heterocyclic compounds that include a three-ring fused structure. Both aromatic or non-aromatic ring structures are included in this category. Fused Heterocyclic Compounds, Three-Ring,Heterocyclic Cpds, 3 Ring,Three Ring Heterocyclic Compounds,3-Ring Heterocyclic Compounds,Fused Heterocyclic Compounds, Three Ring,Heterocyclic Compounds, 3 Ring
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular

Related Publications

A P Tamiz, and M P Smith, and A P Kozikowski
March 2017, International journal of molecular sciences,
A P Tamiz, and M P Smith, and A P Kozikowski
June 2013, Yao xue xue bao = Acta pharmaceutica Sinica,
A P Tamiz, and M P Smith, and A P Kozikowski
May 2008, Bioorganic & medicinal chemistry,
A P Tamiz, and M P Smith, and A P Kozikowski
February 2009, Journal of medicinal chemistry,
A P Tamiz, and M P Smith, and A P Kozikowski
September 2011, ChemMedChem,
A P Tamiz, and M P Smith, and A P Kozikowski
November 2004, Journal of medicinal chemistry,
A P Tamiz, and M P Smith, and A P Kozikowski
February 2009, European journal of medicinal chemistry,
A P Tamiz, and M P Smith, and A P Kozikowski
December 2008, Organic & biomolecular chemistry,
A P Tamiz, and M P Smith, and A P Kozikowski
January 2008, ChemMedChem,
A P Tamiz, and M P Smith, and A P Kozikowski
April 2005, Chemistry & biodiversity,
Copied contents to your clipboard!