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与抗病毒药物化学公式共舞:全景图(第二部分)。

Dancing with chemical formulae of antivirals: A panoramic view (Part 2).

机构信息

Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium.

出版信息

Biochem Pharmacol. 2013 Nov 15;86(10):1397-410. doi: 10.1016/j.bcp.2013.09.010. Epub 2013 Sep 23.

Abstract

In this second part of "Dancing with antivirals as chemical formulae" I will focus on a number of chemical compounds that in the last few years have elicited more than common attraction from a commercial viewpoint: (i) favipiravir (T-705), as it is active against influenza, but also several other RNA viruses; (ii) neuraminidase inhibitors such as zanamivir and oseltamivir; (iii) peramivir and laninamivir octanoate, which might be effective against influenza virus following a single (intravenous or inhalation) administration; (iv) sofosbuvir, the (anticipated) cornerstone for the interferon-free therapy of HCV infections; (v) combinations of DAAs (direct antiviral agents) to achieve, in no time, a sustained virus response (SVR) against HCV infection; (vi) HIV protease inhibitors, the latest and most promising being darunavir; (vii) the integrase inhibitors (INIs) (raltegravir, elvitegravir, dolutegravir), representing a new dimension in the anti-HIV armamentarium; (viii), a new class of helicase primase inhibitors (HPIs) that may exceed acyclovir and the other anti-herpes compounds in both potency and safety; (ix) CMX-001, as the latest of Dr. Antonín Holý's legacy for its activity against poxviruses and CMV infections, and (x) noroviruses for which the ideal antiviral compounds are still awaited for.

摘要

在“与抗病毒药物共舞——化学公式篇”的第二部分,我将集中讨论近年来从商业角度引起更多关注的一些化学化合物:(i) 法匹拉韦(T-705),因其对流感以及其他几种 RNA 病毒具有活性;(ii) 神经氨酸酶抑制剂,如扎那米韦和奥司他韦;(iii) 帕拉米韦和拉尼米韦辛酸酯,可能对流感病毒具有单次(静脉或吸入)给药的有效性;(iv) 索非布韦,有望成为 HCV 感染无干扰素治疗的基石;(v) DAA 联合治疗(直接抗病毒药物),以实现 HCV 感染的持续病毒应答(SVR);(vi) HIV 蛋白酶抑制剂,最新、最有前途的是达芦那韦;(vii) 整合酶抑制剂(INIs)(拉替拉韦、艾维雷韦、多替拉韦),为抗 HIV 武器库增添了新维度;(viii) 一类新的解旋酶-引物酶抑制剂(HPIs),在效力和安全性方面可能超过阿昔洛韦和其他抗疱疹化合物;(ix) CMX-001,作为 Antonín Holý 博士的最新遗产,因其对痘病毒和 CMV 感染的活性;(x) 诺如病毒,目前仍在寻找理想的抗病毒化合物。

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