Literature DB >> 34766232

Design of new imidazole derivatives with anti-HCMV activity: QSAR modeling, synthesis and biological testing.

Vasyl Kovalishyn1, Volodymyr Zyabrev2, Maryna Kachaeva2, Kostiantyn Ziabrev3,4, Kathy Keith5, Emma Harden5, Caroll Hartline5, Scott H James5, Volodymyr Brovarets2.   

Abstract

The problem of designing new antiviral drugs against Human Cytomegalovirus (HCMV) was addressed using the Online Chemical Modeling Environment (OCHEM). Data on compound antiviral activity to human organisms were collected from the literature and uploaded in the OCHEM database. The predictive ability of the regression models was tested through cross-validation, giving coefficient of determination q2 = 0.71-0.76. The validation of the models using an external test set proved that the models can be used to predict the activity of newly designed compounds with reasonable accuracy within the applicability domain (q2 = 0.70-0.74). The models were applied to screen a virtual chemical library of imidazole derivatives, which was designed to have antiviral activity. The six most promising compounds were identified, synthesized and their antiviral activities against HCMV were evaluated in vitro. However, only two of them showed some activity against the HCMV AD169 strain.
© 2021. The Author(s), under exclusive licence to Springer Nature Switzerland AG.

Entities:  

Keywords:  Antiviral activity; Human cytomegalovirus (HCMV); Imidazole derivatives; Machine learning; OCHEM

Mesh:

Substances:

Year:  2021        PMID: 34766232     DOI: 10.1007/s10822-021-00428-z

Source DB:  PubMed          Journal:  J Comput Aided Mol Des        ISSN: 0920-654X            Impact factor:   3.686


  5 in total

1.  Rational design of isonicotinic acid hydrazide derivatives with antitubercular activity: Machine learning, molecular docking, synthesis and biological testing.

Authors:  Vasyl Kovalishyn; Julie Grouleff; Ivan Semenyuta; Vitaliy O Sinenko; Sergiy R Slivchuk; Diana Hodyna; Volodymyr Brovarets; Volodymyr Blagodatny; Gennady Poda; Igor V Tetko; Larysa Metelytsia
Journal:  Chem Biol Drug Des       Date:  2018-05-06       Impact factor: 2.817

2.  Recommendations for diagnosis of shiga toxin--producing Escherichia coli infections by clinical laboratories.

Authors:  L Hannah Gould; Cheryl Bopp; Nancy Strockbine; Robyn Atkinson; Vickie Baselski; Barbara Body; Roberta Carey; Claudia Crandall; Sharon Hurd; Ray Kaplan; Marguerite Neill; Shari Shea; Patricia Somsel; Melissa Tobin-D'Angelo; Patricia M Griffin; Peter Gerner-Smidt
Journal:  MMWR Recomm Rep       Date:  2009-10-16

3.  ToxAlerts: a Web server of structural alerts for toxic chemicals and compounds with potential adverse reactions.

Authors:  Iurii Sushko; Elena Salmina; Vladimir A Potemkin; Gennadiy Poda; Igor V Tetko
Journal:  J Chem Inf Model       Date:  2012-08-10       Impact factor: 4.956

4.  Online chemical modeling environment (OCHEM): web platform for data storage, model development and publishing of chemical information.

Authors:  Iurii Sushko; Sergii Novotarskyi; Robert Körner; Anil Kumar Pandey; Matthias Rupp; Wolfram Teetz; Stefan Brandmaier; Ahmed Abdelaziz; Volodymyr V Prokopenko; Vsevolod Y Tanchuk; Roberto Todeschini; Alexandre Varnek; Gilles Marcou; Peter Ertl; Vladimir Potemkin; Maria Grishina; Johann Gasteiger; Christof Schwab; Igor I Baskin; Vladimir A Palyulin; Eugene V Radchenko; William J Welsh; Vladyslav Kholodovych; Dmitriy Chekmarev; Artem Cherkasov; Joao Aires-de-Sousa; Qing-You Zhang; Andreas Bender; Florian Nigsch; Luc Patiny; Antony Williams; Valery Tkachenko; Igor V Tetko
Journal:  J Comput Aided Mol Des       Date:  2011-06-10       Impact factor: 3.686

5.  Prediction-driven matched molecular pairs to interpret QSARs and aid the molecular optimization process.

Authors:  Yurii Sushko; Sergii Novotarskyi; Robert Körner; Joachim Vogt; Ahmed Abdelaziz; Igor V Tetko
Journal:  J Cheminform       Date:  2014-12-11       Impact factor: 5.514

  5 in total

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