4.3 Article

Syntheses of 2-Deoxy-2,3-didehydro-N-acetylneuraminic Acid Analogues Modified by α-Acylaminoamido Groups at the C-4 Position Using Isocyanide-Based Four-Component Coupling and Biological Evaluation as Inhibitors of Human Parainfluenza Virus Type 1

期刊

CHEMICAL & PHARMACEUTICAL BULLETIN
卷 61, 期 1, 页码 69-74

出版社

PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c12-00834

关键词

human parainfluenza virus type 1; sialidase inhibitor; sialic acid; 4-isocyano Neu5Ac2en derivative; isocyanide-based four-component coupling

资金

  1. Ministry of Education, Culture, Sports, Science and Technology of Japan [21590117]
  2. Uehara Memorial Foundation
  3. Grants-in-Aid for Scientific Research [21590117, 23590549] Funding Source: KAKEN

向作者/读者索取更多资源

Novel sialidase inhibitors 11 having an alpha-acylaminoamido group at the C-4 position of Neu5Ac2en 1 against human parainfluenza virus type 1 (hPIV-1) were synthesized using one-pot isocyanide-based four-component condensation, and their inhibitory activities against hPIV-1 sialidase were studied. Compound 11b showed inhibitory activity (IC50=5.1mM) against hPIV-1 sialidase. The degree of inhibition of 11b was much weaker than that of 1 (IC50=0.3 mM).

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