Standard

Synthesis, and structure-activity relationship for C(4) and/or C(5) thienyl substituted pyrimidines, as a new family of antimycobacterial compounds. / Verbitskiy, Egor V.; Cheprakova, Ekaterina M.; Slepukhin, Pavel A.; Kravchenko, Marionella A.; Skornyakov, Sergey N.; Rusinov, Gennady L.; Chupakhin, Oleg N.; Charushin, Valery N.

In: European Journal of Medicinal Chemistry, Vol. 97, 7886, 07.05.2015, p. 225-234.

Research output: Contribution to journal › Article › peer-review

Harvard

Verbitskiy, EV, Cheprakova, EM, Slepukhin, PA, Kravchenko, MA, Skornyakov, SN, Rusinov, GL, Chupakhin, ON & Charushin, VN 2015, 'Synthesis, and structure-activity relationship for C(4) and/or C(5) thienyl substituted pyrimidines, as a new family of antimycobacterial compounds', European Journal of Medicinal Chemistry, vol. 97, 7886, pp. 225-234. https://doi.org/10.1016/j.ejmech.2015.05.007

APA

Verbitskiy, E. V., Cheprakova, E. M., Slepukhin, P. A., Kravchenko, M. A., Skornyakov, S. N., Rusinov, G. L., Chupakhin, O. N., & Charushin, V. N. (2015). Synthesis, and structure-activity relationship for C(4) and/or C(5) thienyl substituted pyrimidines, as a new family of antimycobacterial compounds. European Journal of Medicinal Chemistry, 97, 225-234. [7886]. https://doi.org/10.1016/j.ejmech.2015.05.007

Vancouver

Verbitskiy EV, Cheprakova EM, Slepukhin PA, Kravchenko MA, Skornyakov SN, Rusinov GL et al. Synthesis, and structure-activity relationship for C(4) and/or C(5) thienyl substituted pyrimidines, as a new family of antimycobacterial compounds. European Journal of Medicinal Chemistry. 2015 May 7;97:225-234. 7886. https://doi.org/10.1016/j.ejmech.2015.05.007

Author

Verbitskiy, Egor V. ; Cheprakova, Ekaterina M. ; Slepukhin, Pavel A. ; Kravchenko, Marionella A. ; Skornyakov, Sergey N. ; Rusinov, Gennady L. ; Chupakhin, Oleg N. ; Charushin, Valery N. / Synthesis, and structure-activity relationship for C(4) and/or C(5) thienyl substituted pyrimidines, as a new family of antimycobacterial compounds. In: European Journal of Medicinal Chemistry. 2015 ; Vol. 97. pp. 225-234.

BibTeX

@article{212bedb55c5042d6809280d3ed7eb8e9,
title = "Synthesis, and structure-activity relationship for C(4) and/or C(5) thienyl substituted pyrimidines, as a new family of antimycobacterial compounds",
abstract = "Abstract Combination of the Suzuki cross-coupling and nucleophilic aromatic substitution of hydrogen (SNH) reactions proved to be a convenient method for the synthesis of C(4) and/or C(5) mono(thienyl) and di(thienyl) substituted pyrimidines from commercially available 5-bromopyrimidine. All new pyrimidines were found to be active in micromolar concentrations in vitro against H37Rv, avium, terrae, rifampicin and isoniazid-resistance strains of Mycobacterium tuberculosis. The data for acute in vivo toxicity in mice have been obtained for these compounds which appear to be promising antitubercular agents. A series of C-4 and/or C-5 thienyl substituted pyrimidines were synthesized.All compounds were evaluated for their antimycobacterial activities.",
keywords = "Antimicobacterial, Cross-coupling, Nucleophilic aromatic substitution of hydrogen, Pyrimidine, Tuberculosis",
author = "Verbitskiy, {Egor V.} and Cheprakova, {Ekaterina M.} and Slepukhin, {Pavel A.} and Kravchenko, {Marionella A.} and Skornyakov, {Sergey N.} and Rusinov, {Gennady L.} and Chupakhin, {Oleg N.} and Charushin, {Valery N.}",
year = "2015",
month = may,
day = "7",
doi = "10.1016/j.ejmech.2015.05.007",
language = "English",
volume = "97",
pages = "225--234",
journal = "European Journal of Medicinal Chemistry",
issn = "0223-5234",
publisher = "Elsevier",

}

RIS

TY - JOUR

T1 - Synthesis, and structure-activity relationship for C(4) and/or C(5) thienyl substituted pyrimidines, as a new family of antimycobacterial compounds

AU - Verbitskiy, Egor V.

AU - Cheprakova, Ekaterina M.

AU - Slepukhin, Pavel A.

AU - Kravchenko, Marionella A.

AU - Skornyakov, Sergey N.

AU - Rusinov, Gennady L.

AU - Chupakhin, Oleg N.

AU - Charushin, Valery N.

PY - 2015/5/7

Y1 - 2015/5/7

N2 - Abstract Combination of the Suzuki cross-coupling and nucleophilic aromatic substitution of hydrogen (SNH) reactions proved to be a convenient method for the synthesis of C(4) and/or C(5) mono(thienyl) and di(thienyl) substituted pyrimidines from commercially available 5-bromopyrimidine. All new pyrimidines were found to be active in micromolar concentrations in vitro against H37Rv, avium, terrae, rifampicin and isoniazid-resistance strains of Mycobacterium tuberculosis. The data for acute in vivo toxicity in mice have been obtained for these compounds which appear to be promising antitubercular agents. A series of C-4 and/or C-5 thienyl substituted pyrimidines were synthesized.All compounds were evaluated for their antimycobacterial activities.

AB - Abstract Combination of the Suzuki cross-coupling and nucleophilic aromatic substitution of hydrogen (SNH) reactions proved to be a convenient method for the synthesis of C(4) and/or C(5) mono(thienyl) and di(thienyl) substituted pyrimidines from commercially available 5-bromopyrimidine. All new pyrimidines were found to be active in micromolar concentrations in vitro against H37Rv, avium, terrae, rifampicin and isoniazid-resistance strains of Mycobacterium tuberculosis. The data for acute in vivo toxicity in mice have been obtained for these compounds which appear to be promising antitubercular agents. A series of C-4 and/or C-5 thienyl substituted pyrimidines were synthesized.All compounds were evaluated for their antimycobacterial activities.

KW - Antimicobacterial

KW - Cross-coupling

KW - Nucleophilic aromatic substitution of hydrogen

KW - Pyrimidine

KW - Tuberculosis

UR - http://www.scopus.com/inward/record.url?scp=84929311532&partnerID=8YFLogxK

U2 - 10.1016/j.ejmech.2015.05.007

DO - 10.1016/j.ejmech.2015.05.007

M3 - Article

C2 - 25982331

AN - SCOPUS:84929311532

VL - 97

SP - 225

EP - 234

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

SN - 0223-5234

M1 - 7886

ER -

ID: 39450485