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Synthesis and Identification of Pentathiepin-Based Inhibitors of . | LitMetric

Synthesis and Identification of Pentathiepin-Based Inhibitors of .

Antibiotics (Basel)

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.

Published: December 2019

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 and . These compounds were more potent than itraconazole which is the current standard of care for sporotrichosis.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6963766PMC
http://dx.doi.org/10.3390/antibiotics8040249DOI Listing

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