Discovery of a new class of antiviral compounds: Camphor imine derivatives

作者：Sokolova Anastasiya S; Yarovaya Olga I^*; Shernyukov Andrey V; Gatilov Yuriy V; Razumova Yuliya V; Zarubaev Vladimir V; Tretiak Tatiana S; Pokrovsky Andrey G; Kiselev Oleg I; Salakhutdinov Nariman F

来源：European Journal of Medicinal Chemistry, 2015, 105: 263-273.

DOI：10.1016/j.ejmech.2015.10.010

• Influenza
• Camphor derivatives
• Antiviral
• Cage compounds

A new class of compounds featuring a camphor moiety has been discovered that exhibits potent inhibitory activity against influenza A(H1N1)pdm09 and A(H5N1) viruses. The synthesized compounds were characterized by spectroscopic analysis; in addition the structures of compound 2 and 14 were elucidated by the X-ray diffraction technique. Structure activity relationship studies have been conducted to identify the 1,7,7-trimethylbicyclo[2.2.1]heptanes2-ylidene group as the key functional group responsible for the observed antiviral activity. The most potent antiviral compound is imine 2 with therapeutic index more than 500.

• 出版日期2015-11-13