Highly active antiretroviral therapy currently used for HIV/AIDS has significantly increased the life expectancy of HIV-infected individuals. It has also improved the quality of life, reduced mortality, and decreased the incidence of AIDS and HIV-related conditions. Currently, however, affected individuals are typically on a lifetime course of several therapeutic drugs, all with the potential for associated toxicity and emergence of resistance. This calls for development of novel, potent, and broad anti-HIV agents able to stop the spread of HIV/AIDS. Significant progress has been made toward identification of anti-HIV-1 broadly neutralizing antibodies (bNAbs). However, antibody-based drugs are costly to produce and store. Administration (by injection only) and other obstacles limit clinical use. In recent years, several highly promising small-molecule HIV-1 entry inhibitors targeting the epitopes of bNAbs have been developed. These newly developed compounds are the focus of the present article.

目前用于 HIV/AIDS 的高效抗逆转录病毒疗法显着延长了 HIV 感染者的预期寿命。它还提高了生活质量，降低了死亡率，并降低了艾滋病和艾滋病毒相关疾病的发病率。然而，目前，受影响的个体通常在终生使用几种治疗药物，所有这些药物都可能产生相关的毒性和耐药性的出现。这就要求开发能够阻止 HIV/AIDS 传播的新型、有效和广泛的抗 HIV 药物。在鉴定抗 HIV-1 广泛中和抗体 (bNAb) 方面取得了重大进展。然而，基于抗体的药物的生产和储存成本很高。给药（仅通过注射）和其他障碍限制了临床使用。最近几年，已经开发了几种针对 bNAb 表位的非常有前景的小分子 HIV-1 进入抑制剂。这些新开发的化合物是本文的重点。