Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
Design of 4-Substituted Sulfonamidobenzoic Acid Derivatives Targeting Coxsackievirus B3. / Шетнев, А.А.; Волобуева, А. С.; Панова, Валерия; Зарубаев, Владимир Викторович; Байков, Сергей Валентинович.
в: Life, Том 12, № 11, 1832, 09.11.2022.Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
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TY - JOUR
T1 - Design of 4-Substituted Sulfonamidobenzoic Acid Derivatives Targeting Coxsackievirus B3
AU - Шетнев, А.А.
AU - Волобуева, А. С.
AU - Панова, Валерия
AU - Зарубаев, Владимир Викторович
AU - Байков, Сергей Валентинович
N1 - Publisher Copyright: © 2022 by the authors.
PY - 2022/11/9
Y1 - 2022/11/9
N2 - A series of novel 4-substituted sulfonamidobenzoic acid derivatives was synthesized as the structural evolution of 4-(4-(1,3-dioxoisoindolin-2-yl)phenylsulfonamido)benzoic acid, which is the known inhibitor of the enterovirus life cycle. Antiviral properties of prepared compounds were evaluated in vitro using phenotypic screening and viral yield reduction assay. Their capsid binding properties were verified in thermostability assay. We identified two new hit-compounds (4 and 7a) with high activity against the coxsackievirus B3 (Nancy, CVB3) strain with potencies (IC50 values of 4.29 and 4.22 μM, respectively) which are slightly superior to the reference compound 2a (IC50 5.54 μM). Both hits changed the heat inactivation of CVB3 in vitro to higher temperatures, suggesting that they are capsid binders, as 2a is. The results obtained can serve as a basis for further development of the lead compounds for novel drug design to combat enterovirus infection.
AB - A series of novel 4-substituted sulfonamidobenzoic acid derivatives was synthesized as the structural evolution of 4-(4-(1,3-dioxoisoindolin-2-yl)phenylsulfonamido)benzoic acid, which is the known inhibitor of the enterovirus life cycle. Antiviral properties of prepared compounds were evaluated in vitro using phenotypic screening and viral yield reduction assay. Their capsid binding properties were verified in thermostability assay. We identified two new hit-compounds (4 and 7a) with high activity against the coxsackievirus B3 (Nancy, CVB3) strain with potencies (IC50 values of 4.29 and 4.22 μM, respectively) which are slightly superior to the reference compound 2a (IC50 5.54 μM). Both hits changed the heat inactivation of CVB3 in vitro to higher temperatures, suggesting that they are capsid binders, as 2a is. The results obtained can serve as a basis for further development of the lead compounds for novel drug design to combat enterovirus infection.
KW - aminobenzoic acid
KW - capsid binders
KW - enteroviruses
KW - heterocycles
KW - imide
KW - screening
UR - https://www.mdpi.com/2075-1729/12/11/1832
UR - https://www.mendeley.com/catalogue/ec03762e-11e0-3692-b8f3-632445c18ba6/
UR - http://www.scopus.com/inward/record.url?scp=85141726728&partnerID=8YFLogxK
U2 - 10.3390/life12111832
DO - 10.3390/life12111832
M3 - Article
VL - 12
JO - Life
JF - Life
SN - 0024-3019
IS - 11
M1 - 1832
ER -
ID: 100039083