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异恶唑啉-碳环核苷的合成及其抗病毒评估：标准方案

Syntheses of isoxazoline-carbocyclic nucleosides and their antiviral evaluation: a standard protocol.

作者信息

Quadrelli Paolo, Vazquez Martinez Naiara, Scrocchi Roberto, Corsaro Antonino, Pistarà Venerando

机构信息

Dipartimento di Chimica, Università degli Studi di Pavia, Viale Taramelli 12, 27100 Pavia, Italy.

Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, Viale A. Doria 8, 95125 Catania, Italy.

出版信息

ScientificWorldJournal. 2014;2014:492178. doi: 10.1155/2014/492178. Epub 2014 Oct 30.

DOI:10.1155/2014/492178
PMID:25544956
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4230217/
Abstract

The current synthesis of racemic purine and pyrimidine isoxazoline-carbocyclic nucleosides is reported, detailing the key-steps for standard and reliable preparations. Improved yields were obtained by the proper tuning of the single synthetic steps, opening the way for the preparation of a variety of novel compounds. Some of the obtained compounds were also evaluated against a wide variety of DNA and RNA viruses including HIV. No specific antiviral activity was observed in the cases at hand. Novel compounds were prepared for future biological tests.

摘要

报道了外消旋嘌呤和嘧啶异恶唑啉-碳环核苷的当前合成方法，详细介绍了标准且可靠制备方法的关键步骤。通过对单个合成步骤进行适当调整，提高了产率，为制备各种新型化合物开辟了道路。还针对包括HIV在内的多种DNA和RNA病毒对部分所得化合物进行了评估。在目前的案例中未观察到特定的抗病毒活性。制备了新型化合物用于未来的生物学测试。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/fa4a1c2551ae/TSWJ2014-492178.sch.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/37272f6da627/TSWJ2014-492178.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/cf947d4cf5b9/TSWJ2014-492178.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/b73a5543eeb7/TSWJ2014-492178.sch.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/d675ba106c05/TSWJ2014-492178.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/722d923c1d8e/TSWJ2014-492178.sch.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/fa4a1c2551ae/TSWJ2014-492178.sch.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/37272f6da627/TSWJ2014-492178.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/cf947d4cf5b9/TSWJ2014-492178.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/b73a5543eeb7/TSWJ2014-492178.sch.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/d675ba106c05/TSWJ2014-492178.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/722d923c1d8e/TSWJ2014-492178.sch.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b3f2/4230217/fa4a1c2551ae/TSWJ2014-492178.sch.004.jpg

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