title: Design, synthesis, and biological evaluation of novel tricyclic HIV-1 integrase inhibitors by modification of its pyridine ring.
abstract: This communication details both the syntheses and biological evaluation of a novel class of HIV-1 integrase inhibitors. When the quinoline moiety is replaced with the quinoxoline moiety, the antiviral activity is significantly compromised. Similarly, introduction of imidazole to replace the pyridine ring is deleterious to the potency of the compound against the enzyme. Substitution at the 3-position of the pyridine has been investigated. The presence of the pyridine ring in the tricyclic core is preferred for antiviral activity against HIV integrase.
authors.affiliation: Department of Medicinal Chemistry, Gilead Sciences, 333 Lakeside Drive, Foster City, CA 94404, USA. smetobo@gilead.com
authors.forename: Sammy E
authors.initials: SE
authors.lastname: Metobo
authors.forename: Haolun
authors.initials: H
authors.lastname: Jin
authors.forename: Manuel
authors.initials: M
authors.lastname: Tsiang
authors.forename: Choung U
authors.initials: CU
authors.lastname: Kim
mesh_terms: D015195:Drug Design; D019427:HIV Integrase / Q000187:drug effects*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects; D011725:Pyridines / Q000737:chemistry*
chemical_list: D019428:HIV Integrase Inhibitors; D011725:Pyridines; D019427:HIV Integrase; C023666:pyridine