斯坦吡啶是一种具有强效抗HIV活性的新型核苷类逆转录酶抑制剂。

Stampidine as a novel nucleoside reverse transcriptase inhibit with potent anti-HIV activity.

作者信息

Uckun Fatih M

机构信息

Parker Hughes Institute, Roseville, Minnesota, USA.

出版信息

Arzneimittelforschung. 2006 Feb;56(2A):121-35. doi: 10.1055/s-0031-1296800.

DOI:10.1055/s-0031-1296800

PMID:16570821

Abstract

Stavudine (STV, d4T, 2',3'-didehydro-3'-deoxythymidine, CAS 3056-17-5) is a standard anti-HIV drug. Stampidine (STAMP, DDE-113, HI-113, N-[p-(4-bromophenyl)-2',3'-didehydro-3'-deoxy-5'-thymidylyl]-L-alanine methyl ester, CAS 217178-62-6) is a novel aryl phosphate derivative of stavudine with more potent anti-HIV activity and more favorable pharmacodynamic features. The remarkable potency of stampidine against clinical HIV-1 isolates with NRTI- or NNRTI-resistance (NRTI, nucleoside reverse transcriptase inhibitor; NNRTI, non-nucleoside reverse transcriptase inhibitor) warrants the further development of this new anti-HIV agent.

摘要

司他夫定（STV，d4T，2'，3'-二脱氢-3'-脱氧胸苷，CAS 3056-17-5）是一种标准的抗HIV药物。司他莫定（STAMP，DDE-113，HI-113，N-[对-(4-溴苯基)-2'，3'-二脱氢-3'-脱氧-5'-胸苷酰基]-L-丙氨酸甲酯，CAS 217178-62-6）是司他夫定的一种新型芳基磷酸酯衍生物，具有更强的抗HIV活性和更有利的药效学特性。司他莫定对具有核苷类逆转录酶抑制剂（NRTI）或非核苷类逆转录酶抑制剂（NNRTI）耐药性的临床HIV-1分离株具有显著的效力，这使得这种新型抗HIV药物值得进一步开发。