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Literature DB >> 32435415

Synthesis and Selective Functionalization of Thiadiazine 1,1-Dioxides with Efficacy in a Model of Huntington's Disease.

Leila Terrab¹, Christopher J Rosenker¹, Lisa Johnstone¹, Linh K Ngo¹, Li Zhang¹, Nathaniel F Ware¹, Bettina Miller¹, Andrea Z Topacio¹, Sara Sannino², Jeffrey L Brodsky², Peter Wipf¹.

Abstract

The scope of the acid-mediated 3-component synthesis of thiadiazines was investigated. A selective functionalization of the six-membered heterocyclic core structure was accomplished by sequential alkylations, saponifications, and coupling reactions. Several new analogs of a dihydropyrimidinone Hsp70 chaperone agonist, MAL1-271, showed promising activity in a cell based model of Huntington's disease.

Entities: Chemical Disease Gene

Year: 2020 PMID： 32435415 PMCID： PMC7236266 DOI： 10.1021/acsmedchemlett.0c00018

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

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