Bioorganic and Medicinal Chemistry

, volume 24 , issue 16 , pages 3771-3780

Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines

Egor V. Verbitskiy ^{1, 2}

Svetlana A Baskakova ³

Marionella A. Kravchenko ⁴

Sergey N. Skornyakov ⁴

Gennady L. Rusinov ^{1, 2}

O. N. Chupakhin ^{1, 2}

Valery Charushin ^{1, 2}

Hide authors affiliations Show authors affiliations: 4 affiliations

Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, S. Kovalevskoy Str, 22, Ekaterinburg 620990, Russia |

Ural Federal University, Mira St. 19, Ekaterinburg 620002, Russia |

Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, S. Kovalevskoy Str., 22, Ekaterinburg 620990, Russia. |

⁴

Ural Research Institute for Phthisiopulmonology, 22 Parts’ezda St., 50, Ekaterinburg 620039, Russia |

Publication type: Journal Article

Publication date: 2016-08-01

Elsevier

Bioorganic and Medicinal Chemistry

scimago Q2

wos Q1

SJR: 0.608

CiteScore: 6.7

Impact factor: 3.0

ISSN: 09680896, 14643391

DOI: 10.1016/j.bmc.2016.06.020

Copy DOI

PubMed ID: 27338658

Organic Chemistry

Drug Discovery

Biochemistry

Molecular Biology

Pharmaceutical Science

Clinical Biochemistry

Molecular Medicine

Abstract

Various 5-(fluoroaryl)-4-(hetero)aryl substituted pyrimidines have been synthesized based on the Suzuki cross-coupling and nucleophilic aromatic substitution of hydrogen (SN(H)) reactions starting from commercially available 5-bromopyrimidine and their antitubercular activity against Mycobacterium tuberculosis H37Rv has been explored. The outcome of the study disclose that, some of the compounds have showed promising activity in micromolar concentration against Mycobacterium tuberculosis H37Rv, Mycobacterium avium, Mycobacterium terrae, and multidrug-resistant strains isolated from tuberculosis patients in Ural region (Russia). The data concerning the 'structure-activity' relationship for fluorinated compounds have been discussed.

Found

1 citation

Makarov Vadim

🥼 🤝

DSc in Chemistry

177 publications, 4 647 citations, 7 reviews

h-index: 36

Federal Research Centre “Fundamentals of Biotechnology” of the Russian Academy of Sciences

Research interests

Early drug discovery

Medicinal Chemistry

1 citation

F. Ekaterina

50 publications, 426 citations

h-index: 13

Postovsky Institute of Organic Synthesis of the Ural Branch of the Russian Academy of Sciences

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GOST Copy

Verbitskiy E. V. et al. Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines // Bioorganic and Medicinal Chemistry. 2016. Vol. 24. No. 16. pp. 3771-3780.

GOST all authors (up to 50) Copy

Verbitskiy E. V., Baskakova S. A., Kravchenko M. A., Skornyakov S. N., Rusinov G. L., Chupakhin O. N., Charushin V. Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines // Bioorganic and Medicinal Chemistry. 2016. Vol. 24. No. 16. pp. 3771-3780.

RIS |

Cite this

RIS Copy

TY - JOUR

DO - 10.1016/j.bmc.2016.06.020

UR - https://linkinghub.elsevier.com/retrieve/pii/S0968089616304436

TI - Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines

T2 - Bioorganic and Medicinal Chemistry

AU - Verbitskiy, Egor V.

AU - Baskakova, Svetlana A

AU - Kravchenko, Marionella A.

AU - Skornyakov, Sergey N.

AU - Rusinov, Gennady L.

AU - Chupakhin, O. N.

AU - Charushin, Valery

PY - 2016

DA - 2016/08/01

PB - Elsevier

SP - 3771-3780

IS - 16

VL - 24

PMID - 27338658

SN - 0968-0896

SN - 1464-3391

ER -

BibTex |

Cite this

BibTex (up to 50 authors) Copy

@article{2016_Verbitskiy,

author = {Egor V. Verbitskiy and Svetlana A Baskakova and Marionella A. Kravchenko and Sergey N. Skornyakov and Gennady L. Rusinov and O. N. Chupakhin and Valery Charushin},

title = {Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines},

journal = {Bioorganic and Medicinal Chemistry},

year = {2016},

volume = {24},

publisher = {Elsevier},

month = {aug},

url = {https://linkinghub.elsevier.com/retrieve/pii/S0968089616304436},

number = {16},

pages = {3771--3780},

doi = {10.1016/j.bmc.2016.06.020}

}

MLA

Cite this

MLA Copy

Verbitskiy, Egor V., et al. “Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines.” Bioorganic and Medicinal Chemistry, vol. 24, no. 16, Aug. 2016, pp. 3771-3780. https://linkinghub.elsevier.com/retrieve/pii/S0968089616304436.

Publisher

Elsevier

Journal

Bioorganic and Medicinal Chemistry

scimago Q2

wos Q1

SJR

0.608

CiteScore

6.7

Impact factor

3.0

ISSN

09680896 (Print)

14643391 (Electronic)