title: [Pyrido(3,2-e)(1,4)diazepines--synthesis and testing of anti-HIV-1 activity].
abstract: Starting from the commercially available 6-methyl-2-pyridylamine (1) the pyrido[3,2-e][1,4]diazepine 14a was synthesized in 12 steps with 7% total yield. 14a, the N-methyl derivative 14b, the thiolactam 15a, the amidine 16, and the 1,2,4-triazole 17 were tested for anti-HIV-1-activity. None of the compounds tested possesses antiviral activity comparable to that of zidovudine (3'-azido-3'-desoxythymidine = AZT).
authors.affiliation: Institut für Pharmazeutische Chemie, Technischen Universität Braunschweig.
authors.forename: K
authors.initials: K
authors.lastname: Görlitzer
authors.forename: C
authors.initials: C
authors.lastname: Wilpert
authors.forename: H
authors.initials: H
authors.lastname: Rübsamen-Waigmann
authors.forename: H
authors.initials: H
authors.lastname: Suhartono
authors.forename: L
authors.initials: L
authors.lastname: Wang
authors.forename: A
authors.initials: A
authors.lastname: Immelmann
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001381:Azepines / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D015215:Zidovudine / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D001381:Azepines; D011725:Pyridines; D015215:Zidovudine
vernacular_title: Pyrido[3,2-e][1,4]diazepine-Synthese und Prüfung auf Anti-HIV-1-Wirkung.