Bioorganic and Medicinal Chemistry Letters

, том 21 , издание 6 , страницы 1823-1826

Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors

Тип публикации: Journal Article

Дата публикации: 2011-03-01

Elsevier

Bioorganic and Medicinal Chemistry Letters

SCImago Q2

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БС2

SJR: 0.426

CiteScore: 4.5

Impact factor: 2.3

ISSN: 0960894X, 14643405

DOI: 10.1016/j.bmcl.2011.01.057

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PubMed ID: 21316237

Organic Chemistry

Drug Discovery

Biochemistry

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Pharmaceutical Science

Clinical Biochemistry

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Краткое описание

A series of 1,5-diaryl-substituted tetrazole derivatives was synthesized via conversion of readily available diaryl amides into corresponding imidoylchlorides followed by reaction with sodium azide. All compounds were evaluated by cyclooxygenase (COX) assays in vitro to determine COX-1 and COX-2 inhibitory potency and selectivity. Tetrazoles 3a-e showed IC(50) values ranging from 0.42 to 8.1 mM for COX-1 and 2.0 to 200 μM for COX-2. Most potent compound 3c (IC(50) (COX-2)=2.0 μM) was further used in molecular modeling docking studies.

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ГОСТ |

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Al Hourani B. J. et al. Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors // Bioorganic and Medicinal Chemistry Letters. 2011. Vol. 21. No. 6. pp. 1823-1826.

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Al Hourani B. J., Sharma S. K., Mane J. Y., Tuszyński J. A., Baracos V., Kniess T., Suresh M., Pietzsch J., Wuest F. R. Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors // Bioorganic and Medicinal Chemistry Letters. 2011. Vol. 21. No. 6. pp. 1823-1826.

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TY - JOUR

DO - 10.1016/j.bmcl.2011.01.057

UR - https://doi.org/10.1016/j.bmcl.2011.01.057

TI - Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors

T2 - Bioorganic and Medicinal Chemistry Letters

AU - Al Hourani, Baker Jawabrah

AU - Sharma, Sai Kiran

AU - Mane, Jonathan Y

AU - Tuszyński, J. A.

AU - Baracos, Vickie

AU - Kniess, Torsten

AU - Suresh, Mavanur

AU - Pietzsch, Jens

AU - Wuest, Frank R.

PY - 2011

DA - 2011/03/01

PB - Elsevier

SP - 1823-1826

IS - 6

VL - 21

PMID - 21316237

SN - 0960-894X

SN - 1464-3405

ER -

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@article{2011_Al Hourani,

author = {Baker Jawabrah Al Hourani and Sai Kiran Sharma and Jonathan Y Mane and J. A. Tuszyński and Vickie Baracos and Torsten Kniess and Mavanur Suresh and Jens Pietzsch and Frank R. Wuest},

title = {Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors},

journal = {Bioorganic and Medicinal Chemistry Letters},

year = {2011},

volume = {21},

publisher = {Elsevier},

month = {mar},

url = {https://doi.org/10.1016/j.bmcl.2011.01.057},

number = {6},

pages = {1823--1826},

doi = {10.1016/j.bmcl.2011.01.057}

}

MLA

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MLA Скопировать

Al Hourani, Baker Jawabrah, et al. “Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors.” Bioorganic and Medicinal Chemistry Letters, vol. 21, no. 6, Mar. 2011, pp. 1823-1826. https://doi.org/10.1016/j.bmcl.2011.01.057.

Издатель

Elsevier

Журнал

Bioorganic and Medicinal Chemistry Letters

SCImago Q2

WOS Q2

БС2

SJR

0.426

CiteScore

4.5

Impact factor