Department of Pharmaceutical Sciences and Natural Products, School of Basic and Applied Sciences, Central University of Punjab, Bathinda, 151001, India.
Department of Human Genetics and Molecular Medicine, School of Health Sciences, Central University of Punjab, Bathinda, 151001, India.
Mini Rev Med Chem. 2019;19(6):510-526. doi: 10.2174/1389557518666181018163448.
After restricting the proliferation of CD4+T cells, Human Immunodeficiency Virus (HIV), infection persists at a very fast rate causing Acquired Immunodeficiency Syndrome (AIDS). This demands the vigorous need of suitable anti-HIV agents, as existing medicines do not provide a complete cure and exhibit drawbacks like toxicities, drug resistance, side-effects, etc. Even the introduction of Highly Active Antiretroviral Therapy (HAART) failed to combat HIV/AIDS completely. The major breakthrough in anti-HIV discovery was marked with the discovery of raltegravir in 2007, the first integrase (IN) inhibitor. Thereafter, the discovery of elvitegravir, a quinolone derivative emerged as the potent HIV-IN inhibitor. Though many more classes of different drugs that act as anti-HIV have been identified, some of which are under clinical trials, but the recent serious focus is still laid on quinoline and its analogues. In this review, we have covered all the quinoline-based derivatives that inhibit various targets and are potential anti-HIV agents in various phases of the drug discovery.
抑制 CD4+T 细胞增殖后,人类免疫缺陷病毒 (HIV) 仍以极快的速度持续感染,导致获得性免疫缺陷综合征 (AIDS)。这就迫切需要合适的抗 HIV 药物,因为现有药物不能完全治愈 HIV,而且还存在毒性、耐药性、副作用等缺点。即使引入高效抗逆转录病毒疗法 (HAART),也未能完全对抗 HIV/AIDS。2007 年发现拉替拉韦是抗 HIV 发现的重大突破,这是第一种整合酶 (IN) 抑制剂。此后,发现了埃替拉韦,一种喹诺酮衍生物,成为有效的 HIV-IN 抑制剂。虽然已经鉴定出更多类别的不同作用于抗 HIV 的药物,其中一些正在临床试验中,但最近的重点仍然是喹啉及其类似物。在这篇综述中,我们涵盖了所有基于喹啉的衍生物,它们抑制各种靶标,是药物发现各个阶段有潜力的抗 HIV 药物。