ChemInform Abstract: Synthesis and Biological Activity of N-Alkyl Derivatives of Ibotenic Acid.

Today 3,7,10-trioxo-2,4,6,8,9,11-hexaaaza[3.3.3]propellane (THAP) has not yet received widespread re-search attention due to the complexity of the synthesis. This work is devoted to the development of a method for the THAP derivatives synthesis, as well as to the study of their biological activity in comparison with al-kyl-substituted glycolurils (subject of comparison). ТНАРwas N-alkylated to furnish novel hexaalkyl deriva-tives of ТНАРwith methyl, ethyl and propyl substituents. The conditionsfor obtaining the maximum yield of the target productwere optimizedon the base of methyl derivative. The reaction proceeded in DMSO/КОНat 75–80ºC for 13hours in a moderate yield of 56%. The ethyl and propyl derivatives of ТНАРwere synthe-sized under the same conditions. The biological activity of the obtained ТНАРalkyl derivatives and glycoluril alkyl derivatives was evaluated against Sporosarcina ureae, Bacillus pumilus, Salmonella typhimurium and Staphylococcus aureus bacteria and influenza A virus. All the samples were found to exhib-it antibacterial activity against Staphylococcus aureus.It was shown that 2,4,6,8,9,11-hexapropyl-ТНАР, di-tert-butyl-diphenyl-, di-tert-butyl-dibenzyl-, di-tert-butyl-dimethyl-and di-isopropyl-dibenzylglycoluril, have exhibited also toxicity to living cells besides antiviral activity

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The synthesis and prediction of biological activity in silico for new alkyl derivatives of 4-r-3-(morfolinometylen)-4H-1,2,4-triazole-5-thioles

Ukraïns’kij bìofarmacevtičnij žurnal ◽

10.24959/ubphj.16.36 ◽

2016 ◽

Vol 0 (3(44)) ◽

pp. 34-38

Author(s):

R. O. Shcherbyna

Keyword(s):

Biological Activity ◽

In Silico ◽

Alkyl Derivatives ◽

Derivatives Of

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Synthesis and Biological Activity of 1H-benzotriazole and 1H-benzimidazole Analogues — Inhibitors of the NTPase/Helicase of HCV and of Some Related Flaviviridae

Antiviral Chemistry and Chemotherapy ◽

10.1177/095632020501600504 ◽

2005 ◽

Vol 16 (5) ◽

pp. 315-326 ◽

Cited By ~ 25

Author(s):

Maria Bretner ◽

Andrea Baier ◽

Katarzyna Kopańska ◽

Andżelika Najda ◽

Anna Schoof ◽

...

Keyword(s):

Biological Activity ◽

Hepatitis C Virus ◽

Hepatitis C ◽

Inhibitory Activity ◽

Alkylating Agents ◽

Alkyl Halides ◽

Helicase Activity ◽

Alkyl Derivatives ◽

Flash Column Chromatography ◽

Derivatives Of

To improve anti-helical activity of analogues of 1 H-benzotriazole and 1 H-benzimidazole their N-alkyl derivatives were synthesized and tested for anti-helicase activity against enzymes of selected Flaviviridae including hepatitis C virus (HCV), West Nile virus (WNV), Dengue virus (DENV) and Japanese encephalitis virus (JEV). 1- and 2-alkyl derivatives of 4,5,6,7-tetrabromo-1 H-benzotriazole were obtained by direct alkylation of 4,5,6,7-tetrabromo-1 H-benzotriazole with the use of respective alkyl halides in the presence of KOH in methanol, to give a mixture of 1- and 2- isomers, which was separated by flash column chromatography in good yield. The proportion of isomers strongly depended on the reaction time and temperature. 1- and 2-hydroxyethyl and 1- and 2-chloroethyl derivatives of the tetrabromobenzo-triazole were synthesized with the use of 2-bromoethanol and 1-bromo-2-chloroethane respectively as alkylating agents. N-alkylation of this benzotriazole compound enhanced inhibitory activity and selectivity towards the helicase activity of HCV NTPase/helicase. The most active were the 2-methyl, 2-ethyl and 2-propyl derivatives (IC50∼6.5 μM in the presence of DNA as a substrate). Derivatives of the benzotriazole in which hydroxyethyl or chloroethyl replaced the alkyl substituents lost their inhibitory activity. Brominated or methylated benzotriazole N(1) ribosides also did not exert helicase inhibitory activity. Although a number of N(1) and N(2) alkyl derivatives exerted good HCV and WNV helicase inhibitory activity when DNA was used as substrate, the activity was strongly decreased or even disappeared when RNA was used as substrate. The cytotoxicity tests in Vero and HeLa Tat cells showed a substantial decrease of cytotoxicity of N-alkyl derivatives as compared to the parent benzotriazole.

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Synthesis and Biological Activity of Novel O-Alkyl Derivatives of Naringenin and Their Oximes

Molecules ◽

10.3390/molecules22091485 ◽

2017 ◽

Vol 22 (9) ◽

pp. 1485 ◽

Cited By ~ 14

Author(s):

Joanna Kozłowska ◽

Bartłomiej Potaniec ◽

Barbara Żarowska ◽

Mirosław Anioł

Keyword(s):

Biological Activity ◽

Alkyl Derivatives ◽

Derivatives Of

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Synthesis and biological activity of N-alkyl derivatives of 2,3,4,5-tetrahydro-1h-1,5-benzodiazepin-2-one

Pharmaceutical Chemistry Journal ◽

10.1007/bf00763661 ◽

1988 ◽

Vol 22 (9) ◽

pp. 679-683

Author(s):

B. A. Puodzhyunaite ◽

R. A. Yanchene ◽

A. S. Zaks ◽

Yu. M. Rabotnikov ◽

E. A. Usachev

Keyword(s):

Biological Activity ◽

Alkyl Derivatives ◽

Derivatives Of

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Study of the Biological Activity of Alkyl Derivatives of Tetrahydroisoquinolines

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i46b32938 ◽

2021 ◽

pp. 238-246

Author(s):

Umida Khamidova ◽

Ekaterina Terenteva ◽

Mukaddas Umarova ◽

Jaloliddin Abdurakhmanov ◽

Sabirdjan Sasmakov ◽

...

Keyword(s):

Antimicrobial Activity ◽

Biological Activity ◽

Cancer Cells ◽

Cytotoxic Effect ◽

Normal Cells ◽

Alkyl Derivatives ◽

Antifungal Effects ◽

Low Toxicity ◽

Antibacterial And Antifungal ◽

Derivatives Of

A row of 1-alkyne (C6-C17) derivatives against tetrahydroisoquinoline have been synthesized. 1-alkyne (C6-C17) derivatives cytotoxicity against three lines of cancer cells and two lines of normal cells was studied. It was found that 1-tridecyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline exhibits a high cytotoxic effect with low toxicity to healthy cells. Antimicrobial activity of 1-alkyne (C6-C17) derivatives against 5 strains of bacteria and fungus was studied. It has been found that 1-nonyl-6,7-dimethoxy-1,3,4-tetrahydroisoquinoline exhibits strong antibacterial and antifungal effects.

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Synthesis, Characterization and Evaluation of the Biological Activity of Azetidin -2-carbonyl Derivatives of Thymine Nitrogenous Base

International Journal of Pharmaceutical Research ◽

10.31838/ijpr/2020.12.02.0146 ◽

2020 ◽

Vol 12 (02) ◽

Keyword(s):

Biological Activity ◽

Carbonyl Derivatives ◽

Nitrogenous Base ◽

Derivatives Of

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Synthesis and Biological Potentials of Quinoline Analogues: A Review of Literature

Mini-Reviews in Organic Chemistry ◽

10.2174/1570193x16666190213105146 ◽

2019 ◽

Vol 16 (7) ◽

pp. 653-688 ◽

Cited By ~ 6

Author(s):

Leena Kumari ◽

Salahuddin ◽

Avijit Mazumder ◽

Daman Pandey ◽

Mohammad Shahar Yar ◽

...

Keyword(s):

Biological Activity ◽

Heterocyclic Compounds ◽

Building Blocks ◽

Vital Role ◽

Review Of Literature ◽

Drug Discovery Process ◽

Active Compounds ◽

Lead Compounds ◽

Synthetic Approaches ◽

Derivatives Of

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.

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