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New chalcone derivatives as effective against SARS-CoV-2 agent.
Duran, Nizami; Polat, M Fatih; Aktas, Derya Anil; Alagoz, M Abdullah; Ay, Emrah; Cimen, Funda; Tek, Erhan; Anil, Baris; Burmaoglu, Serdar; Algul, Oztekin.
  • Duran N; Department of Medical Microbiology, Medical Faculty, Mustafa Kemal University, Antakya, Turkey.
  • Polat MF; Department of Pharmaceutical Basic Sciences, Faculty of Pharmacy, Erzincan Binali Yildirim University, Erzincan, Turkey.
  • Aktas DA; Department of Chemistry and Chemical Process Technologies, Erzurum Vocational High School, Atatürk University, Erzurum, Turkey.
  • Alagoz MA; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Inonu University, Malatya, Turkey.
  • Ay E; Department of Medical Microbiology, Medical Faculty, Mustafa Kemal University, Antakya, Turkey.
  • Cimen F; Department of Medical Microbiology, Medical Faculty, Mustafa Kemal University, Antakya, Turkey.
  • Tek E; Department of Medical Microbiology, Medical Faculty, Mustafa Kemal University, Antakya, Turkey.
  • Anil B; Department of Chemistry, Faculty of Science, Atatürk University, Erzurum, Turkey.
  • Burmaoglu S; Department of Chemistry, Faculty of Science, Atatürk University, Erzurum, Turkey.
  • Algul O; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin, Turkey.
Int J Clin Pract ; 75(12): e14846, 2021 Dec.
Article in English | MEDLINE | ID: covidwho-1555354
ABSTRACT

AIMS:

Flavonoids and related compounds, such as quercetin-based antiviral drug Gene-Eden-VIR/Novirin, inhibit the protease of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The alkylated chalcones isolated from Angelica keiskei inhibit SARS-CoV proteases. In this study, we aimed to compare the anti-SARS CoV-2 activities of both newly synthesized chalcone derivatives and these two drugs.

METHODS:

Determination of the potent antiviral activity of newly synthesized chalcone derivatives against SARS-CoV-2 by calculating the RT-PCR cycling threshold (Ct ) values.

RESULTS:

Antiviral activities of the compounds varied because of being dose dependent. Compound 6, 7, 9, and 16 were highly effective against SARS-CoV-2 at the concentration of 1.60 µg/mL. Structure-based virtual screening was carried out against the most important druggable SARS-CoV-2 targets, viral RNA-dependent RNA polymerase, to identify putative inhibitors that could facilitate the development of potential anti-coronavirus disease-2019 drug candidates.

CONCLUSIONS:

Computational analyses identified eight compounds inhibiting each target, with binding affinity scores ranging from -4.370 to -2.748 kcal/mol along with their toxicological, ADME, and drug-like properties.
Subject(s)

Full text: Available Collection: International databases Database: MEDLINE Main subject: Chalcone / Chalcones / COVID-19 Type of study: Experimental Studies / Prognostic study Limits: Humans Language: English Journal: Int J Clin Pract Journal subject: Medicine Year: 2021 Document Type: Article Affiliation country: Ijcp.14846

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Chalcone / Chalcones / COVID-19 Type of study: Experimental Studies / Prognostic study Limits: Humans Language: English Journal: Int J Clin Pract Journal subject: Medicine Year: 2021 Document Type: Article Affiliation country: Ijcp.14846