Primary screening of the biological activity of heterocyclic aminoderivatives of 2,3-dichloro-1,4-naphtoquinone

Authors

DOI:

https://doi.org/10.15587/2519-4852.2019.188127

Keywords:

aminopyrazole 2, 3-dichloro-1, 4-naphthoquinone derivatives, primary biological screening, GUSAR program

Abstract

The aim. Check the antimicrobial and fungicidal activity of 2,3-dichloro-1,4-naphthoquinone aminopyrazole derivatives and predict their severity of toxicity to rats.

Materials and methods of the research. The antimicrobial activity of heterocyclic amino derivatives of naphthoquinone 3a-d was studied by diffusion of the substance into agar on solid nutrient medium and by serial dilution. Acute rodent toxicity was determined by the QSAR simulation method implemented in GUSAR software.

Results. In the work, the antimicrobial and fungicidal activities of new heterocyclic amino derivatives of naphthoquinone were studied, as well as the in silico determination of their acute toxicity for rats was carried out using four types of substance administration.

Conclusions. The study of aminopyrazole derivatives of naphthoquinone revealed the compounds exhibiting high antimicrobial activity against the Candida tenuis test culture, namely: 2-chloro-3-((1-methyl-1H-pyrazol-4-yl) amino) naphthalene-1,4-dione (3a) and 2-chloro-3 - ((1-methyl-1H-pyrazol-3-yl) amino) naphthalene-1,4-dione (3b). All the synthesized compounds were found to exhibit selective bacterio- and fungistatic activity. QSAR determined the non-toxic compound 3c in the intraperitoneal route of administration, as well as the non-toxic compound 3d in the subcutaneous route of administration

Supporting Agency

  • Національний університет "Львівська політехніка"

Author Biographies

Nataliia Polish, Lviv Polytechnic National University St. Bandery str., 12, Lviv, Ukraine, 79013

Postgraduate Student

Department of Technology Biologically Compounds, Pharmacy and Biotechnology

Olha Voitsakhivska, Lviv Polytechnic National University St. Bandery str., 12, Lviv, Ukraine, 79013

Department of Technology Biologically Compounds, Pharmacy and Biotechnology

Nataliia Marintsova, Lviv Polytechnic National University St. Bandery str., 12, Lviv, Ukraine, 79013

PhD, Associate Professor

Department of Technology Biologically Compounds, Pharmacy and Biotechnology

Lesya Zhurakhivska, Lviv Polytechnic National University St. Bandery str., 12, Lviv, Ukraine, 79013

PhD, Associate Professor

Department of Technology Biologically Compounds, Pharmacy and Biotechnology

Volodymyr Novikov, Lviv Polytechnic National University St. Bandery str., 12, Lviv, Ukraine, 79013

Doctor of Chemical Sciences, Professor

Department of Technology Biologically Compounds, Pharmacy and Biotechnology

Serhii Bohza, Institute of Organic Chemistry of the National Academy of Sciences of Ukraine Murmanska str., 5, Kyiv, Ukraine, 02660

Doctor of Chemical Sciences, Senior Researcher

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Published

2019-12-30

How to Cite

Polish, N., Voitsakhivska, O., Marintsova, N., Zhurakhivska, L., Novikov, V., & Bohza, S. (2019). Primary screening of the biological activity of heterocyclic aminoderivatives of 2,3-dichloro-1,4-naphtoquinone. ScienceRise: Pharmaceutical Science, (6 (22), 37–42. https://doi.org/10.15587/2519-4852.2019.188127

Issue

No. 6 (22) (2019)

Section

Pharmaceutical Science

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Copyright (c) 2019 Nataliia Polish, Olha Voytsakhivska, Nataliia Marintsova, Lesya Zhurakhivska, Volodymyr Novikov, Serhii Bohza

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