Bioorganic and Medicinal Chemistry Letters

, том 27 , издание 15 , страницы 3529-3533

Synthesis and structure–activity relationship study of novel quinazolinone-based inhibitors of MurA

Тип публикации: Journal Article

Дата публикации: 2017-08-01

Elsevier

Bioorganic and Medicinal Chemistry Letters

scimago Q2

wos Q2

БС2

SJR: 0.472

CiteScore: 5.1

Impact factor: 2.2

ISSN: 0960894X, 14643405

DOI: 10.1016/j.bmcl.2017.05.064

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PubMed ID: 28579123

Organic Chemistry

Drug Discovery

Biochemistry

Molecular Biology

Pharmaceutical Science

Clinical Biochemistry

Molecular Medicine

Краткое описание

MurA is an intracellular bacterial enzyme that is essential for peptidoglycan biosynthesis, and is therefore an important target for antibacterial drug discovery. We report the synthesis, in silico studies and extensive structure-activity relationships of a series of quinazolinone-based inhibitors of MurA from Escherichia coli. 3-Benzyloxyphenylquinazolinones showed promising inhibitory potencies against MurA, in the low micromolar range, with an IC50 of 8µM for the most potent derivative (58). Furthermore, furan-substituted quinazolinones (38, 46) showed promising antibacterial activities, with MICs from 1µg/mL to 8µg/mL, concomitant with their MurA inhibitory potencies. These data represent an important step towards the development of novel antimicrobial agents to combat increasing bacterial resistance.

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European Journal of Medicinal Chemistry	European Journal of Medicinal Chemistry, 5, 9.09% European Journal of Medicinal Chemistry 5 публикаций, 9.09%
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Hrast M. et al. Synthesis and structure–activity relationship study of novel quinazolinone-based inhibitors of MurA // Bioorganic and Medicinal Chemistry Letters. 2017. Vol. 27. No. 15. pp. 3529-3533.

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Hrast M., Rozman K., Jukic M., Patin D., Gobec S., Sova M. Synthesis and structure–activity relationship study of novel quinazolinone-based inhibitors of MurA // Bioorganic and Medicinal Chemistry Letters. 2017. Vol. 27. No. 15. pp. 3529-3533.

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TY - JOUR

DO - 10.1016/j.bmcl.2017.05.064

UR - https://doi.org/10.1016/j.bmcl.2017.05.064

TI - Synthesis and structure–activity relationship study of novel quinazolinone-based inhibitors of MurA

T2 - Bioorganic and Medicinal Chemistry Letters

AU - Hrast, Martina

AU - Rozman, Kaja

AU - Jukic, Marko

AU - Patin, Delphine

AU - Gobec, Stanislav

AU - Sova, Matej

PY - 2017

DA - 2017/08/01

PB - Elsevier

SP - 3529-3533

IS - 15

VL - 27

PMID - 28579123

SN - 0960-894X

SN - 1464-3405

ER -

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@article{2017_Hrast,

author = {Martina Hrast and Kaja Rozman and Marko Jukic and Delphine Patin and Stanislav Gobec and Matej Sova},

title = {Synthesis and structure–activity relationship study of novel quinazolinone-based inhibitors of MurA},

journal = {Bioorganic and Medicinal Chemistry Letters},

year = {2017},

volume = {27},

publisher = {Elsevier},

month = {aug},

url = {https://doi.org/10.1016/j.bmcl.2017.05.064},

number = {15},

pages = {3529--3533},

doi = {10.1016/j.bmcl.2017.05.064}

}

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MLA Скопировать

Hrast, Martina, et al. “Synthesis and structure–activity relationship study of novel quinazolinone-based inhibitors of MurA.” Bioorganic and Medicinal Chemistry Letters, vol. 27, no. 15, Aug. 2017, pp. 3529-3533. https://doi.org/10.1016/j.bmcl.2017.05.064.

Издатель

Elsevier

Журнал

Bioorganic and Medicinal Chemistry Letters

scimago Q2

wos Q2

БС2

SJR

0.472

CiteScore

5.1

Impact factor

2.2

ISSN

0960894X (Print)

14643405 (Electronic)