羟基-15-阿扎甾醇的合成。

IF 4.3 3区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY

ACS Omega Pub Date : 2025-01-31 eCollection Date: 2025-02-11 DOI:10.1021/acsomega.4c09907

Caleb A H Jones, Bruce J Melancon, Craig W Lindsley

{"title":"羟基-15-阿扎甾醇的合成。","authors":"Caleb A H Jones, Bruce J Melancon, Craig W Lindsley","doi":"10.1021/acsomega.4c09907","DOIUrl":null,"url":null,"abstract":"Niemann-Pick type C (NPC) is a lysosomal storage disorder that will cause eventual brain damage with limited treatment options available. Though clinical trials are undergoing with repurposed pharmaceuticals, no novel chemotype exists purely for the treatment of NPC. In 2021, an azasterol was found to bind to both NPC1 and NPC2 proteins and is considered as a cholesterol mimic. A convergent synthesis to obtain a hydroxy-15-azasterol was completed in 12 steps, from 2-oxepanone.","PeriodicalId":22,"journal":{"name":"ACS Omega","volume":"10 5","pages":"4784-4791"},"PeriodicalIF":4.3000,"publicationDate":"2025-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11822486/pdf/","citationCount":"0","resultStr":"{\"title\":\"Synthesis of a Hydroxy-15-Azasterol.\",\"authors\":\"Caleb A H Jones, Bruce J Melancon, Craig W Lindsley\",\"doi\":\"10.1021/acsomega.4c09907\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Niemann-Pick type C (NPC) is a lysosomal storage disorder that will cause eventual brain damage with limited treatment options available. Though clinical trials are undergoing with repurposed pharmaceuticals, no novel chemotype exists purely for the treatment of NPC. In 2021, an azasterol was found to bind to both NPC1 and NPC2 proteins and is considered as a cholesterol mimic. A convergent synthesis to obtain a hydroxy-15-azasterol was completed in 12 steps, from 2-oxepanone.\",\"PeriodicalId\":22,\"journal\":{\"name\":\"ACS Omega\",\"volume\":\"10 5\",\"pages\":\"4784-4791\"},\"PeriodicalIF\":4.3000,\"publicationDate\":\"2025-01-31\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11822486/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ACS Omega\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1021/acsomega.4c09907\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/2/11 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ACS Omega","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1021/acsomega.4c09907","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/2/11 0:00:00","PubModel":"eCollection","JCR":"Q2","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}

引用次数: 0

摘要

尼曼-皮克C型（NPC）是一种溶酶体贮积性疾病，最终会导致脑损伤，治疗方案有限。虽然临床试验正在进行重新利用的药物，没有新的化学类型存在，纯粹用于治疗鼻咽癌。2021年，一种阿沙甾醇被发现与NPC1和NPC2蛋白结合，被认为是一种胆固醇模拟物。以2-奥西酮为原料，经12步聚合合成羟基-15-阿扎甾醇。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Synthesis of a Hydroxy-15-Azasterol.

查看原文本刊更多论文

Synthesis of a Hydroxy-15-Azasterol.

Niemann-Pick type C (NPC) is a lysosomal storage disorder that will cause eventual brain damage with limited treatment options available. Though clinical trials are undergoing with repurposed pharmaceuticals, no novel chemotype exists purely for the treatment of NPC. In 2021, an azasterol was found to bind to both NPC1 and NPC2 proteins and is considered as a cholesterol mimic. A convergent synthesis to obtain a hydroxy-15-azasterol was completed in 12 steps, from 2-oxepanone.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

ACS Omega Chemical Engineering-General Chemical Engineering

CiteScore

6.60

自引率

4.90%

发文量

3945

审稿时长

2.4 months

期刊介绍： ACS Omega is an open-access global publication for scientific articles that describe new findings in chemistry and interfacing areas of science, without any perceived evaluation of immediate impact.