자료유형  

 학위논문

Control Number  

0016933306

International Standard Book Number  

9798379779207

Dewey Decimal Classification Number  

540

Main Entry-Personal Name  

Hill, Sarah J.

Publication, Distribution, etc. (Imprint  

[S.l.] : The Scripps Research Institute., 2024

Publication, Distribution, etc. (Imprint  

Ann Arbor : ProQuest Dissertations & Theses, 2024

Physical Description  

1 online resource(375 p.)

General Note  

Source: Dissertations Abstracts International, Volume: 85-01, Section: B.

General Note  

Advisor: Shenvi, Ryan A.

Dissertation Note  

Thesis (Ph.D.)--The Scripps Research Institute, 2024.

Restrictions on Access Note  

This item must not be sold to any third party vendors.

Summary, Etc.  

요약The salvinorins serve as templates for next generation analgesics, antipruritics and dissociative hallucinogens via selective and potent agonism of the kappa-opioid receptor (KOR). In contrast to most opioids, the salvinorins lack basic amines and bind with high affinity and selectivity via complex polyoxygenated scaffolds that have frustrated deep-seated modification by synthesis. Here we describe a short asymmetric synthesis that relies on a sterically-confined organocatalyst to dissociate acidity from reactivity and effect Robinson annulation of an unactivated nucleophile / unstable electrophile pair. Combined with a cobalt-catalyzed polarized diene-alkyne cycloaddition, the route allows divergent access to a focused library of salvinorins. We appraise the synthesis by its generation of multiple analogs that exceed the potency, selectivity, stability and functional bias of salvinorin A itself.  

Subject Added Entry-Topical Term  

Chemistry.

Subject Added Entry-Topical Term  

Pharmaceutical sciences.

Index Term-Uncontrolled  

Chemistry

Index Term-Uncontrolled  

Organic chemistry

Index Term-Uncontrolled  

Salvinorins

Index Term-Uncontrolled  

Antipruritics

Index Term-Uncontrolled  

Kappa-opioid receptor

Index Term-Uncontrolled  

Analgesics

Added Entry-Corporate Name  

The Scripps Research Institute Chemistry

Host Item Entry  

Dissertations Abstracts International. 85-01B.

Host Item Entry  

Dissertation Abstract International

Electronic Location and Access  

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Control Number  

joongbu:643068