Research output: Contribution to journal › Article › peer-review
New class of hantaan virus inhibitors based on conjugation of the isoindole fragment to (+)-camphor or (−)-fenchone hydrazonesv. / Yarovaya, Olga I.; Kovaleva, Kseniya S.; Zaykovskaya, Anna A. et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 40, 127926, 15.05.2021.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - New class of hantaan virus inhibitors based on conjugation of the isoindole fragment to (+)-camphor or (−)-fenchone hydrazonesv
AU - Yarovaya, Olga I.
AU - Kovaleva, Kseniya S.
AU - Zaykovskaya, Anna A.
AU - Yashina, Liudmila N.
AU - Scherbakova, Nadezda S.
AU - Scherbakov, Dmitry N.
AU - Borisevich, Sophia S.
AU - Zubkov, Fedor I.
AU - Antonova, Alexandra S.
AU - Peshkov, Roman Yu
AU - Eltsov, Ilia V.
AU - Pyankov, Oleg V.
AU - Maksyutov, Rinat A.
AU - Salakhutdinov, Nariman F.
N1 - Publisher Copyright: © 2021 Elsevier Ltd Copyright: Copyright 2021 Elsevier B.V., All rights reserved.
PY - 2021/5/15
Y1 - 2021/5/15
N2 - This work presents the design and synthesis of camphor, fenchone, and norcamphor N-acylhydrazone derivatives as a new class of inhibitors of the Hantaan virus, which causes haemorrhagic fever with renal syndrome (HFRS). A cytopathic model was developed for testing chemotherapeutics against the Hantaan virus, strain 76–118. In addition, a study of the antiviral activity was carried out using a pseudoviral system. It was found that the hit compound possesses significant activity (IC50 = 7.6 ± 2 µM) along with low toxicity (CC50 > 1000 µM). Using molecular docking procedures, the binding with Hantavirus nucleoprotein was evaluated and the correlation between the structure of the synthesised compounds and the antiviral activity was established.
AB - This work presents the design and synthesis of camphor, fenchone, and norcamphor N-acylhydrazone derivatives as a new class of inhibitors of the Hantaan virus, which causes haemorrhagic fever with renal syndrome (HFRS). A cytopathic model was developed for testing chemotherapeutics against the Hantaan virus, strain 76–118. In addition, a study of the antiviral activity was carried out using a pseudoviral system. It was found that the hit compound possesses significant activity (IC50 = 7.6 ± 2 µM) along with low toxicity (CC50 > 1000 µM). Using molecular docking procedures, the binding with Hantavirus nucleoprotein was evaluated and the correlation between the structure of the synthesised compounds and the antiviral activity was established.
KW - Antiviral
KW - Hantavirus
KW - HFRS
KW - Isoindole
KW - Terpene
UR - http://www.scopus.com/inward/record.url?scp=85102584920&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2021.127926
DO - 10.1016/j.bmcl.2021.127926
M3 - Article
C2 - 33705902
AN - SCOPUS:85102584920
VL - 40
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
M1 - 127926
ER -
ID: 28079230