Bianco Maria da Conceição Avelino Dias, Marinho Debora Inacio Leite Firmino, Hoelz Lucas Villas Boas, Bastos Monica Macedo, Boechat Nubia
Laboratório de Sintese de Farmacos-LASFAR, Instituto de Tecnologia em Farmacos-Farmanguinhos, FIOCRUZ, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, RJ, Brazil.
Centro de Ciencias da Saude-CCS, Programa de Pos-graduação em Farmacologia e Quimica Medicinal do Instituto de Ciencias Biomedicas-ICB-UFRJ, Bloco J, Ilha do Fundao, Rio de Janeiro 21941-902, RJ, Brazil.
Pharmaceuticals (Basel). 2021 Sep 2;14(9):893. doi: 10.3390/ph14090893.
Acquired immunodeficiency syndrome (AIDS) is caused by human immunodeficiency virus (HIV) and remains a global health problem four decades after the report of its first case. Despite success in viral load suppression and the increase in patient survival due to combined antiretroviral therapy (cART), the development of new drugs has become imperative due to strains that have become resistant to antiretrovirals. In this context, there has been a continuous search for new anti-HIV agents based on several chemical scaffolds, including nitrogenated heterocyclic pyrrole rings, which have been included in several compounds with antiretroviral activity. Thus, this review aims to describe pyrrole-based compounds with anti-HIV activity as a new potential treatment against AIDS, covering the period between 2015 and 2020. Our research allowed us to conclude that pyrrole derivatives are still worth exploring, as they may provide highly active compounds targeting different steps of the HIV-1 replication cycle and act with an innovative mechanism.
获得性免疫缺陷综合征(艾滋病)由人类免疫缺陷病毒(HIV)引起,自首例病例报告以来的四十年间,它一直是一个全球性的健康问题。尽管联合抗逆转录病毒疗法(cART)在抑制病毒载量以及提高患者生存率方面取得了成功,但由于出现了对抗逆转录病毒药物耐药的毒株,开发新药已变得势在必行。在此背景下,人们一直在基于多种化学骨架不断寻找新的抗HIV药物,包括含氮杂环吡咯环,它已被纳入多种具有抗逆转录病毒活性的化合物中。因此,本综述旨在描述2015年至2020年期间具有抗HIV活性的吡咯类化合物,作为一种治疗艾滋病的新的潜在疗法。我们的研究使我们得出结论,吡咯衍生物仍值得探索,因为它们可能提供针对HIV-1复制周期不同步骤的高活性化合物,并以创新机制发挥作用。