吡唑相关核苷5. 4-碘-1-β-D-呋喃核糖基-3-羧甲基吡唑（IPCAR）的2'-脱氧-2',3'-二脱氧和无环类似物的合成及生物活性

Pyrazole related nucleosides 5. Synthesis and biological activity of 2'-deoxy-2',3'-dideoxy- and acyclo-analogues of 4-iodo-1-beta-D-ribofuranosyl-3-carboxymethyl pyrazole (IPCAR).

作者信息

Manfredini S, Baraldi P G, Bazzanini R, Durini E, Vertuani S, Pani A, Marceddu T, Demontis F, Vargiu L, La Colla P

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2000 Apr;19(4):705-22. doi: 10.1080/15257770008035019.

DOI:10.1080/15257770008035019

PMID:10960030

Abstract

Continuing our studies on the structure-activity relationships (SAR) of 4-iodo-1-beta-D-ribofuranosyl-3-carboxymethyl pyrazole (IPCAR), the ribofuranosyl moiety has been substituted with acyclic chains, namely 1-[(2-hydroxyethoxy)methyl]- and 1-[(1,3-dihydroxy-2-propoxy)methyl]-pyrazole derivatives (4, 5 and 8, 9 respectively), with the 2'-deoxy-beta-D-ribofuranosyl group (12 and 13) and finally with the 2',3'-dideoxy-D-glycero-pentofuranosyl-moiety (16 and 17). None of the new compounds display any interesting biological activity.

摘要

在继续我们关于4-碘-1-β-D-呋喃核糖基-3-羧甲基吡唑（IPCAR）结构-活性关系（SAR）的研究中，呋喃核糖基部分已被无环链取代，即1-[(2-羟基乙氧基)甲基]-和1-[(1,3-二羟基-2-丙氧基)甲基]-吡唑衍生物（分别为4、5和8、9），2'-脱氧-β-D-呋喃核糖基（12和13），最后是2',3'-二脱氧-D-甘油-戊呋喃糖基部分（16和17）。这些新化合物均未表现出任何有趣的生物活性。