Peptide deformylase inhibitors of Mycobacterium tuberculosis: Synthesis, structural investigations, and biological results
Тип публикации: Journal Article
Дата публикации: 2008-12-01
scimago Q2
wos Q2
БС2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
19008098
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
Bacterial peptide deformylase (PDF) belongs to a subfamily of metalloproteases catalyzing the removal of the N-terminal formyl group from newly synthesized proteins. We report the synthesis and biological activity of highly potent inhibitors of Mycobacterium tuberculosis (Mtb) PDF enzyme as well as the first X-ray crystal structure of Mtb PDF. Structure-activity relationship and crystallographic data clarified the structural requirements for high enzyme potency and cell based potency. Activities against single and multi-drug-resistant Mtb strains are also reported.
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Pichota A. et al. Peptide deformylase inhibitors of Mycobacterium tuberculosis: Synthesis, structural investigations, and biological results // Bioorganic and Medicinal Chemistry Letters. 2008. Vol. 18. No. 24. pp. 6568-6572.
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Pichota A., Duraiswamy J., Yin Z., Keller T. M., Alam J., Liung S., Lee G., Ding M., Wang G., Chan W. L. M., Schreiber M., Ma I., Beer D. G., Ngew X., Mukherjee K., Nanjundappa M., Teo J. W. P., Thayalan P., Yap A., Dick T. E., Meng W., Xu M., Koehn J., Pan S., CLARK K., Xie X., Shoen C., Cynamon M. H. Peptide deformylase inhibitors of Mycobacterium tuberculosis: Synthesis, structural investigations, and biological results // Bioorganic and Medicinal Chemistry Letters. 2008. Vol. 18. No. 24. pp. 6568-6572.
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TY - JOUR
DO - 10.1016/j.bmcl.2008.10.040
UR - https://doi.org/10.1016/j.bmcl.2008.10.040
TI - Peptide deformylase inhibitors of Mycobacterium tuberculosis: Synthesis, structural investigations, and biological results
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Pichota, Arkadius
AU - Duraiswamy, Jeyaraj
AU - Yin, Zheng
AU - Keller, Thomas M.
AU - Alam, Jenefer
AU - Liung, Sarah
AU - Lee, Gladys
AU - Ding, M.
AU - Wang, Gang
AU - Chan, Wai Leong Mickey
AU - Schreiber, Mark
AU - Ma, Ida
AU - Beer, David G.
AU - Ngew, Xinyi
AU - Mukherjee, Kakoli
AU - Nanjundappa, Mahesh
AU - Teo, Jeanette W. P.
AU - Thayalan, Pamela
AU - Yap, Amelia
AU - Dick, T E
AU - Meng, Wuyi
AU - Xu, Mei
AU - Koehn, James
AU - Pan, Shi-hao
AU - CLARK, Kirk
AU - Xie, Xiaoling
AU - Shoen, Carolyn
AU - Cynamon, M. H.
PY - 2008
DA - 2008/12/01
PB - Elsevier
SP - 6568-6572
IS - 24
VL - 18
PMID - 19008098
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2008_Pichota,
author = {Arkadius Pichota and Jeyaraj Duraiswamy and Zheng Yin and Thomas M. Keller and Jenefer Alam and Sarah Liung and Gladys Lee and M. Ding and Gang Wang and Wai Leong Mickey Chan and Mark Schreiber and Ida Ma and David G. Beer and Xinyi Ngew and Kakoli Mukherjee and Mahesh Nanjundappa and Jeanette W. P. Teo and Pamela Thayalan and Amelia Yap and T E Dick and Wuyi Meng and Mei Xu and James Koehn and Shi-hao Pan and Kirk CLARK and Xiaoling Xie and Carolyn Shoen and M. H. Cynamon},
title = {Peptide deformylase inhibitors of Mycobacterium tuberculosis: Synthesis, structural investigations, and biological results},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2008},
volume = {18},
publisher = {Elsevier},
month = {dec},
url = {https://doi.org/10.1016/j.bmcl.2008.10.040},
number = {24},
pages = {6568--6572},
doi = {10.1016/j.bmcl.2008.10.040}
}
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MLA
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Pichota, Arkadius, et al. “Peptide deformylase inhibitors of Mycobacterium tuberculosis: Synthesis, structural investigations, and biological results.” Bioorganic and Medicinal Chemistry Letters, vol. 18, no. 24, Dec. 2008, pp. 6568-6572. https://doi.org/10.1016/j.bmcl.2008.10.040.