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用于抗HIV药物开发的杂环类药物发现与探索

Drug Discovery and Exploration of Heterocycles for the Development of Anti-HIV Agents.

作者信息

Kale Mayura A, Jain Mamata V

机构信息

Government College of Pharmacy, Karad, Maharashtra, India.

Government College of Pharmacy, Aurangabad, Maharashtra, India.

出版信息

Infect Disord Drug Targets. 2025;25(3):e18715265290911. doi: 10.2174/0118715265290911240611072422.

DOI:10.2174/0118715265290911240611072422
PMID:39185647
Abstract

It is a known fact that HIV infection remains a serious public health problem throughout the world, and the need to constantly develop new antiretroviral drugs to combat HIV emerges from the fact that repetitive mutations occurring in viral enzymes make this virus resistant to antiretroviral drugs. This resistance causes failure of treatment, and hence, for many years, extensive research has been to discover newer possibilities for fighting this disease at a molecular level, along with many long-standing and expensive clinical trials. Many scientific research programs have either been discarded or unsuccessful. However, the research has not stopped, and in the process, many heterocyclic scaffolds have been used to build up novel drug molecules to combat this disease. A literature survey reveals that many heterocycles have been explored and were found to be very useful in treating different types of viral infections. This concise and rigorous literature explains the journey and highlights the various strategies to develop new anti-HIV drug candidates.

摘要

众所周知,艾滋病毒感染在全球范围内仍然是一个严重的公共卫生问题。由于病毒酶中反复出现的突变使这种病毒对抗逆转录病毒药物产生耐药性,因此不断研发新的抗逆转录病毒药物来对抗艾滋病毒的需求应运而生。这种耐药性导致治疗失败,因此,多年来,人们进行了广泛的研究,试图在分子水平上找到对抗这种疾病的新方法,同时也进行了许多长期且昂贵的临床试验。许多科研项目要么被放弃,要么没有成功。然而,研究并未停止,在此过程中,许多杂环骨架被用于构建新型药物分子来对抗这种疾病。一项文献调查显示,许多杂环已被探索,并且发现它们在治疗不同类型的病毒感染方面非常有用。这篇简洁而严谨的文献解释了这一历程,并突出了开发新型抗艾滋病毒候选药物的各种策略。

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Discovery of diarylpyrimidine derivatives bearing piperazine sulfonyl as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.发现含哌嗪磺酰基的二芳基嘧啶衍生物作为有效的HIV-1非核苷类逆转录酶抑制剂。
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Approved HIV reverse transcriptase inhibitors in the past decade.过去十年中获批的HIV逆转录酶抑制剂。
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Update and latest advances in antiretroviral therapy.抗逆转录病毒治疗的最新进展和研究动态。
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Chemical space exploration of novel naphthyl-carboxamide-diarylpyrimidine derivatives with potent anti-HIV-1 activity.新型萘基-羧酰胺-二芳基嘧啶衍生物的化学空间探索及其强效抗 HIV-1 活性。
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Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors.新型白桦脂酸衍生物的设计、合成及构效关系分析作为有效的 HIV 抑制剂。
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Synthesis, antiviral, DFT and molecular docking studies of some novel 1,2,4-triazine nucleosides as potential bioactive compounds.合成、抗病毒、DFT 和分子对接研究新型 1,2,4-三嗪核苷作为潜在的生物活性化合物。
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