Abstract:
:Histoplasmosis is a severe infection that affects millions of patients worldwide and is endemic in the Americas. Amphotericin B (AMB) and itraconazole are highly effective for the treatment of severe and milder forms of the disease, but AMB is toxic, and the bioavailability of itraconazole is erratic. Therefore, it is important to investigate new classes of drugs for histoplasmosis treatment. In this study, a series of nine isoniazid hydrazone derivatives were synthesized and evaluated for their antifungal activities in vitro against the dimorphic fungus Histoplasma capsulatum var. capsulatum. The drugs were tested by microdilution in accordance with CLSI guidelines. The compound N'-(1-phenylethylidene)isonicotinohydrazide had the lowest MIC range of all the compounds for the yeast and filamentous forms of H. capsulatum. The in vitro synergy of this compound with AMB against the planktonic and biofilm forms of H. capsulatum cells was assessed by the checkerboard method. The effects of this hydrazone on cellular ergosterol content and membrane integrity were also investigated. The study showed that the compound alone is able to reduce the ergosterol content of planktonic cells and can alter the membrane permeability of the fungus. Furthermore, the compound alone or in combination with AMB showed inhibitory effects against mature biofilms of H. capsulatum. N'-(1-Phenylethylidene)isonicotinohydrazide alone or combined with AMB might be of interest in the management of histoplasmosis.
journal_name
Antimicrob Agents Chemotherjournal_title
Antimicrobial agents and chemotherapyauthors
de Aguiar Cordeiro R,de Farias Marques FJ,de Aguiar Cordeiro R,da Silva MR,Donato Maia Malaquias A,Silva de Melo CV,Mafezoli J,Ferreira de Oliveira Mda C,Nogueira Brilhante RS,Gadelha Rocha MF,Pinheiro Gomes Bandeira Tde J,Costa Sidoi
10.1128/AAC.01654-13subject
Has Abstractpub_date
2014-05-01 00:00:00pages
2504-11issue
5eissn
0066-4804issn
1098-6596pii
AAC.01654-13journal_volume
58pub_type
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