Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
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.
в: European Journal of Medicinal Chemistry, Том 97, 7886, 07.05.2015, стр. 225-234.Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
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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