title: Design, synthesis and antiviral activity of novel pyridazines.
abstract: A series of pyridazines were prepared and evaluated for their anti-HIV activity. The new synthetic route involving a novel rearrangement reaction provided a practical method for the preparation of 5-hydroxypyridazines. The primary bioassay results indicated that most of the pyridazines possess anti-HIV activity. It ought to been mentioned that the rearranged compounds 35 and 39 exhibited relatively higher HIV inhibitory effect. Most of the synthesized compounds were also found to possess good anti-TMV activity, of which compound 9 showed similar in vivo anti-TMV activity to commercial plant virucide Ribavirin. This work provides a new and efficient approach to evolve novel multi-functional antiviral agents by rational integration and optimization of previously reported antiviral agents.
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, Nankai University, 94 Weijing Street, Tianjin 300071, People's Republic of China.
authors.forename: Ziwen
authors.initials: Z
authors.lastname: Wang
authors.forename: Mingxiao
authors.initials: M
authors.lastname: Wang
authors.forename: Xue
authors.initials: X
authors.lastname: Yao
authors.forename: Yue
authors.initials: Y
authors.lastname: Li
authors.forename: Juan
authors.initials: J
authors.lastname: Tan
authors.forename: Lizhong
authors.initials: L
authors.lastname: Wang
authors.forename: Wentao
authors.initials: W
authors.lastname: Qiao
authors.forename: Yunqi
authors.initials: Y
authors.lastname: Geng
authors.forename: Yuxiu
authors.initials: Y
authors.lastname: Liu
authors.forename: Qingmin
authors.initials: Q
authors.lastname: Wang
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D015497:HIV-1 / Q000187:drug effects; D011724:Pyridazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D013329:Structure-Activity Relationship; D014027:Tobacco Mosaic Virus / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D011724:Pyridazines