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Open access
Antibiotics, volume 8, issue 4, pages 249

Synthesis and identification of pentathiepin-based inhibitors of sporothrix brasiliensis

Machado Ana C. S. 2
De Miranda Luisa H M 2
Rakitin Oleg A. 3, 4
Pereira Sandro A 2
1
 
Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
2
 
Laboratory of Clinical Research in Dermatozoonoses on Domestic Animals (LAPCLIN-DERMZOO), Evandro Chagas National Institute of Infectious Diseases (INI), Oswaldo Cruz Foundation (Fiocruz), Rio de Janeiro 21040-360, Brazil
5
 
Mycology Laboratory, INI, Fiocruz, Rio de Janeiro 21040-360, Brazil
Publication typeJournal Article
Publication date2019-12-03
Journal: Antibiotics
Quartile SCImago
Q1
Quartile WOS
Q1
Impact factor4.8
ISSN20796382
Biochemistry
Microbiology (medical)
Microbiology
Infectious Diseases
Pharmacology (medical)
General Pharmacology, Toxicology and Pharmaceutics
Abstract

Sporothrix brasiliensis is the causative agent of zoonotic sporotrichosis in Brazil and is currently referred to as the most virulent species among those of clinical importance within the genus. Sporotrichosis is an emergent disease that has come to the forefront over two decades with a recent hot spot of sporotrichosis infection emerging in the state of Rio de Janeiro. The source of these infections is now at epidemic proportions with more than 4000 cases reported in Rio de Janeiro, Brazil, alone since 1998. We developed a focused library of a rare pentathiepin ring system and identified a potent substitution pattern that yielded compounds 21 and 22. These compounds were more potent than itraconazole which is the current standard of care for sporotrichosis.

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GOST |
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GOST Copy
Asquith C. R. M. et al. Synthesis and identification of pentathiepin-based inhibitors of sporothrix brasiliensis // Antibiotics. 2019. Vol. 8. No. 4. p. 249.
GOST all authors (up to 50) Copy
Asquith C. R. M., Machado A. C. S., De Miranda L. H. M., Konstantinova L. S., Almeida-Paes R., Rakitin O. A., Pereira S. A. Synthesis and identification of pentathiepin-based inhibitors of sporothrix brasiliensis // Antibiotics. 2019. Vol. 8. No. 4. p. 249.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.3390/antibiotics8040249
UR - https://doi.org/10.3390%2Fantibiotics8040249
TI - Synthesis and identification of pentathiepin-based inhibitors of sporothrix brasiliensis
T2 - Antibiotics
AU - Machado, Ana C. S.
AU - De Miranda, Luisa H M
AU - Konstantinova, Lidia S.
AU - Pereira, Sandro A
AU - Asquith, Christopher R M
AU - Almeida-Paes, Rodrigo
AU - Rakitin, Oleg A.
PY - 2019
DA - 2019/12/03 00:00:00
PB - Multidisciplinary Digital Publishing Institute (MDPI)
SP - 249
IS - 4
VL - 8
PMID - 31816950
SN - 2079-6382
ER -
BibTex |
Cite this
BibTex Copy
@article{2019_Asquith
author = {Ana C. S. Machado and Luisa H M De Miranda and Lidia S. Konstantinova and Sandro A Pereira and Christopher R M Asquith and Rodrigo Almeida-Paes and Oleg A. Rakitin},
title = {Synthesis and identification of pentathiepin-based inhibitors of sporothrix brasiliensis},
journal = {Antibiotics},
year = {2019},
volume = {8},
publisher = {Multidisciplinary Digital Publishing Institute (MDPI)},
month = {dec},
url = {https://doi.org/10.3390%2Fantibiotics8040249},
number = {4},
pages = {249},
doi = {10.3390/antibiotics8040249}
}
MLA
Cite this
MLA Copy
Asquith, Christopher R. M., et al. “Synthesis and identification of pentathiepin-based inhibitors of sporothrix brasiliensis.” Antibiotics, vol. 8, no. 4, Dec. 2019, p. 249. https://doi.org/10.3390%2Fantibiotics8040249.
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