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SYNTHESIS AND IDENTIFICATION OF PENTATHIEPIN-BASED INHIBITORS OF SPOROTHRIX BRASILIENSIS
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University of North Carolina at Chapel Hill. School of Medicine. Department of Pharmacology. Chapel Hill, NC, USA.
Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Laboratório de Pesquisa Clínica em Dermatozoonoses em Animais Domésticos. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Laboratório de Pesquisa Clínica em Dermatozoonoses em Animais Domésticos. Rio de Janeiro, RJ, Brasil.
Russian Academy of Sciences. Zelinsky Institute of Organic Chemistry. Moscow, Russia / South Ural State University. Nanotechnology Education and Research Center. Chelyabinsk, Russia.
Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Laboratório de Micologia. Rio de Janeiro, RJ, Brasil.
Russian Academy of Sciences. Zelinsky Institute of Organic Chemistry. Moscow, Russia / South Ural State University. Nanotechnology Education and Research Center. Chelyabinsk, Russia.
Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Laboratório de Pesquisa Clínica em Dermatozoonoses em Animais Domésticos. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Laboratório de Pesquisa Clínica em Dermatozoonoses em Animais Domésticos. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Laboratório de Pesquisa Clínica em Dermatozoonoses em Animais Domésticos. Rio de Janeiro, RJ, Brasil.
Russian Academy of Sciences. Zelinsky Institute of Organic Chemistry. Moscow, Russia / South Ural State University. Nanotechnology Education and Research Center. Chelyabinsk, Russia.
Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Laboratório de Micologia. Rio de Janeiro, RJ, Brasil.
Russian Academy of Sciences. Zelinsky Institute of Organic Chemistry. Moscow, Russia / South Ural State University. Nanotechnology Education and Research Center. Chelyabinsk, Russia.
Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Laboratório de Pesquisa Clínica em Dermatozoonoses em Animais Domésticos. Rio de Janeiro, RJ, Brasil.
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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