title: HIV-1 integrase inhibitors: a review of their chemical development.
abstract: Highly active antiretroviral therapy (HAART) significantly decreases plasma viral load, increases CD4+ T-cell counts in HIV-1-infected patients and has reduced progression to AIDS in developed countries. However, adverse side effects, and emergence of drug resistance, mean there is still a demand for new anti-HIV agents. The HIV integrase (IN) is a target that has been the focus of rational drug design over the past decade. In 2007, raltegravir was the first IN inhibitor approved by the US Food and Drug Administration for antiretroviral combination therapy, while another IN inhibitor, elvitegravir, is currently in Phase III clinical trials. This article reviews the development and resistance profiling of small molecule HIV-1 IN inhibitors.
authors.affiliation: Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of Pharmacy, Kolhapur, India. kundan.i@rediffmail.com
authors.forename: Kundan B
authors.initials: KB
authors.lastname: Ingale
authors.forename: Manish S
authors.initials: MS
authors.lastname: Bhatia
mesh_terms: D055808:Drug Discovery; D024882:Drug Resistance, Viral / Q000187:drug effects; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans
chemical_list: D019428:HIV Integrase Inhibitors; D019427:HIV Integrase