2-Substituted benzoxazinone analogues as anti-human coronavirus (anti-HCoV) and ICAM-1 expression inhibition agents.
A series of 2-substituted benzoxazinones were synthesized and subjected to anti-human coronavirus and ICAM-1 expression inhibition assays. Among them, compounds 1, 3, 4, 5, 6, and 7 exhibited significant anti-HCoV activities, and the IC(50) value of these compounds are 6.08, 5.06, 6.83, 1.92, 7.59, and 5.79 microg/mL, respectively. Furthermore, compounds 1 and 6 showed significant inhibitory effect on ICAM-1 expression, the ED(50) values of 1 and 6 are 1.00 and 0.50 microg/mL, respectively.
Hsieh
Pei-Wen
PW
Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
Chang
Fang-Rong
FR
Chang
Cheng-Hsien
CH
Cheng
Pei-Wen
PW
Chiang
Lien-Chai
LC
Zeng
Fu-Long
FL
Lin
Kuei-Hsiang
KH
Wu
Yang-Chang
YC
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001555:Benzene Derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D017934:Coronavirus / Q000187:drug effects*; D003864:Depression, Chemical; D006801:Humans; D018799:Intercellular Adhesion Molecule-1 / Q000096:biosynthesis* / Q000235:genetics; D010078:Oxazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D001555:Benzene Derivatives; D010078:Oxazines; D018799:Intercellular Adhesion Molecule-1