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Design and Synthesis of 4‐ A lkyl‐2‐amino(acetamino)‐6‐aryl‐1,3‐thiazine Derivatives as Influenza Neuraminidase Inhibitors
Author(s) -
Li Wan,
Xia Lin,
Hu Aixi,
Liu Ailin,
Peng Junmei,
Tan Weiqing
Publication year - 2013
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201300122
Subject(s) - thiazine , neuraminidase , chemistry , stereochemistry , aryl , neuraminidase inhibitor , structure–activity relationship , combinatorial chemistry , biochemistry , enzyme , in vitro , covid-19 , organic chemistry , medicine , alkyl , disease , pathology , infectious disease (medical specialty)
With a convenient and economical method, two series of 1,3‐thiazine derivatives 1 and 2 were synthesized, and their neuraminidase (NA) inhibitory activities were evaluated. The pharmacological results showed that most of the compounds have potent NA inhibitory activity. Especially, 1g exhibited the best activity against influenza virus A (H1N1) NA (IC 50 = 29.06 µg/mL), and its crystal structure was determined by single‐crystal X‐ray diffraction. The preliminary biological assay indicated that 1,3‐thiazine could be used as a core structure to design novel influenza NA inhibitors.