Synthesis and Identification of Pentathiepin-Based Inhibitors of Sporothrix brasiliensis

Synthesis and Identification of Pentathiepin-Based Inhibitors of Sporothrix brasiliensis Full article

Journal

Antibiotics-Basel
ISSN: 2079-6382

Output data

Year: 2019, Volume: 8, Number: 4, Article number : 249, Pages count : DOI: 10.3390/antibiotics8040249

Authors

Asquith Christopher R.M. ¹ , Machado Ana C.S. ² , de Miranda Luisa H.M. ² , Konstantinova Lidia S. ^3,4 , Almeida-Paes Rodrigo ⁵ , Rakitin Oleg A. ^3,4 , Pereira Sandro A. ²

Affiliations

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
3	Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow 119991, Russia
4	Nanotechnology Education and Research Center, South Ural State University, Lenina Ave. 76, Chelyabinsk 454080, Russia
5	Mycology Laboratory, INI, Fiocruz, Rio de Janeiro 21040-360, Brazil

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.

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-Basel. 2019. V.8. N4. 249 . DOI: 10.3390/antibiotics8040249 WOS Scopus OpenAlex

Web of science:	WOS:000506678800093
Scopus:	2-s2.0-85076337862
OpenAlex:	W2994146012

DB	Citing
OpenAlex	9
Scopus	11
Web of science	9