title: Design, synthesis and antiviral activity of 2-(3-amino-4-piperazinylphenyl)chromone derivatives.
abstract: Previously, we have confirmed that the antiviral activities of the chromone derivatives were controlled by the type as well as the position of the substituents attached to the chromone core structure. In the course of our ongoing efforts to optimize the antiviral activity of the chromone derivatives, we have been attempting to derivatize the chromone scaffold via introduction of various substituents. In this proof-of-concept study, we introduced a 3-amino-4-piperazinylphenyl functionality to the chromone scaffold and evaluated the antiviral activities of the resulting chromone derivatives. The synthesized 2-(3-amino-4-piperazinylphenyl)-chromones showed severe acute respiratory syndrome-corona virus (SARS-CoV)-specific antiviral activity. In particular, the 2-pyridinylpiperazinylphenyl substituents provided the resulting chromone derivatives with selective antiviral activity. Taken together, this result indicates the possible pharmacophoric role of the 2-pyridinylpiperazine functionality attached to the chromone scaffold, which warrants further in-depth structure-activity relationship study.
authors.affiliation: Department of Bioscience and Biotechnology, Bio/Molecular Informatics Center, Konkuk University, Hwayangdong, Gwangjin-gu, Seoul, Korea.
authors.forename: Mi Kyoung
authors.initials: MK
authors.lastname: Kim
authors.forename: Hyunjun
authors.initials: H
authors.lastname: Yoon
authors.forename: Dale Lynn
authors.initials: DL
authors.lastname: Barnard
authors.forename: Youhoon
authors.initials: Y
authors.lastname: Chong
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002867:Chromones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D016174:Hepacivirus / Q000187:drug effects; D006801:Humans; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry*; D045473:Severe acute respiratory syndrome-related coronavirus / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D002867:Chromones; D010879:Piperazines; D000077489:Piperazine