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Open AccessCommunication

Synthesis and Identification of Pentathiepin-Based Inhibitors of Sporothrix brasiliensis

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
*
Author to whom correspondence should be addressed.
Antibiotics 2019, 8(4), 249; https://doi.org/10.3390/antibiotics8040249
Received: 13 November 2019 / Revised: 25 November 2019 / Accepted: 30 November 2019 / Published: 3 December 2019
(This article belongs to the Special Issue Fungal Pathogens: Resistance and Novel Therapeutics)
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. View Full-Text
Keywords: sporotrichosis; 1,2,3,4,5-pentathiepin; varacin; anti-fungal; sulfur heterocycle sporotrichosis; 1,2,3,4,5-pentathiepin; varacin; anti-fungal; sulfur heterocycle
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MDPI and ACS Style

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, 8, 249.

AMA Style

Asquith CRM, Machado ACS, de Miranda LHM, Konstantinova LS, Almeida-Paes R, Rakitin OA, Pereira SA. Synthesis and Identification of Pentathiepin-Based Inhibitors of Sporothrix brasiliensis. Antibiotics. 2019; 8(4):249.

Chicago/Turabian Style

Asquith, Christopher R.M.; Machado, Ana C.S.; de Miranda, Luisa H.M.; Konstantinova, Lidia S.; Almeida-Paes, Rodrigo; Rakitin, Oleg A.; Pereira, Sandro A. 2019. "Synthesis and Identification of Pentathiepin-Based Inhibitors of Sporothrix brasiliensis" Antibiotics 8, no. 4: 249.

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