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Structure, Synthesis and Inhibition Mechanism of Nucleoside Analogues as HIV‐1 Reverse Transcriptase Inhibitors (NRTIs)
ChemMedChem ( IF 3.4 ) Pub Date : 2020-11-23 , DOI: 10.1002/cmdc.202000695
Yuki Yoshida 1 , Masakazu Honma 2 , Yasuaki Kimura 1 , Hiroshi Abe 1, 3, 4, 5
Affiliation  

Acquired immunodeficiency syndrome (AIDS) is caused by infection with the human immunodeficiency virus (HIV). Although treatments against HIV infection are available, AIDS remains a serious disease that causes many deaths annually. Although a variety of anti‐HIV drugs have been synthesized and marketed to treat HIV‐infected patients, nucleoside analogue reverse transcriptase inhibitors (NRTIs), which mimic nucleosides, are used extensively and remain a subject of interest to medicinal chemists. However, HIV has acquired drug resistance against NRTIs, and thus the struggle to find novel therapies continues. In this review, we trace the trajectory of NRTIs, focusing on the synthesis, mechanisms of action and applications of NRTIs that have been developed.

中文翻译:

作为 HIV-1 逆转录酶抑制剂 (NRTI) 的核苷类似物的结构、合成和抑制机制

获得性免疫缺陷综合征 (AIDS) 是由人类免疫缺陷病毒 (HIV) 感染引起的。尽管有针对 HIV 感染的治疗方法,但 AIDS 仍然是一种严重的疾病,每年都会导致许多人死亡。尽管已经合成并销售了多种抗 HIV 药物来治疗 HIV 感染患者,但模拟核苷的核苷类似物逆转录酶抑制剂 (NRTI) 被广泛使用并且仍然是药物化学家感兴趣的主题。然而,HIV 已经获得了对 NRTIs 的耐药性,因此寻找新疗法的斗争仍在继续。在这篇综述中,我们追踪了 NRTIs 的发展轨迹,重点关注已开发的 NRTIs 的合成、作用机制和应用。
更新日期:2020-11-23
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