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dc.contributor.advisorLever, Susan Z., 1952-eng
dc.contributor.authorNahas, Roger I., 1978-eng
dc.date.issued2007eng
dc.date.submitted2007 Falleng
dc.descriptionThe entire dissertation/thesis text is included in the research.pdf file; the official abstract appears in the short.pdf file (which also appears in the research.pdf); a non-technical general description, or public abstract, appears in the public.pdf file.eng
dc.descriptionTitle from title screen of research.pdf file (viewed on February 26, 2008)eng
dc.descriptionIncludes bibliographical references.eng
dc.descriptionVita.eng
dc.descriptionThesis (Ph. D.) University of Missouri-Columbia 2007.eng
dc.descriptionDissertations, Academic -- University of Missouri--Columbia -- Chemistry.eng
dc.description.abstractSigma receptors are involved in several biological processes, and sigma ligands might be promising as cancer treatment agents, cocaine abuse medicines, and valuable psychiatric drugs. In an attempt to elucidate effectual structure-activity relationships, a series of N-phenylpropyl- N'-benzylpiperazine and N-phenylpropyl-4-benzylpiperidine analogs systematically substituted on both phenyl rings was synthesized. These ligands were specifically designed to have certain substituents and substitution pattern representing three physico-chemical parameters denoting size, hydrophobicity, and electronic characteristics, in order to study the effect of those properties on the biological activity. Structure-activity relationships (SAR) were evaluated qualitatively to describe the effect of the systematic benzyl substitution in comparison to the phenylpropyl substitution. High quality mathematical equations were derived to quantitatively express the statistical correlation between the biological activity and the physico-chemical parameters associated with the benzyl ring substitution. Finally, the effect of the piperidine moiety was compared to the piperazine in a systematic and coherent fashion. This SAR study will result in a better comprehension of the interaction between the sigma protein receptors and the ligands, a better understanding of the pharmacophore profile, and a more effective design for future potent sigma receptor ligands.eng
dc.identifier.merlinb62215826eng
dc.identifier.oclc210121147eng
dc.identifier.urihttps://hdl.handle.net/10355/4840
dc.identifier.urihttps://doi.org/10.32469/10355/4840eng
dc.languageEnglisheng
dc.publisherUniversity of Missouri--Columbiaeng
dc.relation.ispartofcollectionUniversity of Missouri--Columbia. Graduate School. Theses and Dissertationseng
dc.subject.lcshSigma receptorseng
dc.subject.lcshReceptor-ligand complexeseng
dc.subject.lcshLigand binding (Biochemistry)eng
dc.titleSynthesis and structure-activity relationship of a series of sigma receptor ligandseng
dc.typeThesiseng
thesis.degree.disciplineChemistry (MU)eng
thesis.degree.grantorUniversity of Missouri--Columbiaeng
thesis.degree.levelDoctoraleng
thesis.degree.namePh. D.eng


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