Tweet
Arch Pharm (Weinheim). 2013 Aug 7. doi: 10.1002/ardp.201300122. [Epub ahead of print]
Design and Synthesis of 4-Alkyl-2-amino(acetamino)-6-aryl-1,3-thiazine Derivatives as Influenza Neuraminidase Inhibitors.
Li W, Xia L, Hu A, Liu A, Peng J, Tan W.
Source
College of Chemistry and Chemical Engineering, Hunan University, Changsha, China.
Abstract
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 (IC50 = 29.06 ?g/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.
? 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
KEYWORDS:
1,3-Thiazine, Crystal structure, Neuraminidase inhibitor, Synthesis
PMID:
23926081
[PubMed - as supplied by publisher]
Design and Synthesis of 4-Alkyl-2-amino(acetamino)-6-aryl-1,3-thiazine Derivatives as Influenza Neuraminidase Inhibitors.
Li W, Xia L, Hu A, Liu A, Peng J, Tan W.
Source
College of Chemistry and Chemical Engineering, Hunan University, Changsha, China.
Abstract
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 (IC50 = 29.06 ?g/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.
? 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
KEYWORDS:
1,3-Thiazine, Crystal structure, Neuraminidase inhibitor, Synthesis
PMID:
23926081
[PubMed - as supplied by publisher]
