title: Structure-activity relationship of indoloquinoline analogs anti-MRSA.
abstract: Indolo[3,2-b]quinoline analogs (3a-3s), 4-(acridin-9-ylamino) phenol hydrochloride (4), benzofuro[3,2-b]quinoline (3t), indeno[1,2-b]quinolines (3u and 3v) have been synthesized. Those compounds were found to exhibit anti-bacterial activity towards Methicillin-resistant Staphylococcus aureus (anti-MRSA activity). Structure-activity relationship studies were conducted that indoloquinoline ring, benzofuroquinoline ring and 4-aminophenol group are essential structure for anti-MRSA activity.
authors.affiliation: Faculty of Pharmaceutical Sciences, Okayama University, Kitaku-Tsushima-naka 1-1-1, Okayama 700-8530, Japan.
authors.forename: Min
authors.initials: M
authors.lastname: Zhao
authors.affiliation: Faculty of Pharmaceutical Sciences, Okayama University, Kitaku-Tsushima-naka 1-1-1, Okayama 700-8530, Japan.
authors.forename: Tomonori
authors.initials: T
authors.lastname: Kamada
authors.affiliation: Faculty of Pharmaceutical Sciences, Okayama University, Kitaku-Tsushima-naka 1-1-1, Okayama 700-8530, Japan.
authors.forename: Aya
authors.initials: A
authors.lastname: Takeuchi
authors.affiliation: Faculty of Pharmaceutical Sciences, Okayama University, Kitaku-Tsushima-naka 1-1-1, Okayama 700-8530, Japan.
authors.forename: Hiromi
authors.initials: H
authors.lastname: Nishioka
authors.affiliation: Faculty of Pharmaceutical Sciences, Okayama University, Kitaku-Tsushima-naka 1-1-1, Okayama 700-8530, Japan.
authors.forename: Teruo
authors.initials: T
authors.lastname: Kuroda
authors.affiliation: Faculty of Pharmaceutical Sciences, Okayama University, Kitaku-Tsushima-naka 1-1-1, Okayama 700-8530, Japan. Electronic address: take@pharm.okayama-u.ac.jp.
authors.forename: Yasuo
authors.initials: Y
authors.lastname: Takeuchi
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D024881:Drug Resistance, Bacterial / Q000187:drug effects; D007211:Indoles / Q000737:chemistry*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D007211:Indoles; D011804:Quinolines; C037219:quinoline
keywords: Anti-MRSA; Benzofuroquinoline; Indenoquinoline; Indoloquinoline; Structure–activity