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Molecules 2013, 18(3), 3479-3501; https://doi.org/10.3390/molecules18033479

Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents

1
Pharmacognosy Department, Faculty of Biochemical and Pharmaceutical Sciences, National University of Rosario, Suipacha 531, 2000 Rosario, Argentine
2
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, CIETUS-IBSAL, University of Salamanca, Campus Miguel de Unamuno, 37007 Salamanca, Spain
3
Faculty of Chemistry, Biochemistry and Pharmacy, National University of San Luis (UNSL), Chacabuco 917, 5700 San Luis, Argentine
4
IMIBIO-CONICET, Universidad Nacional de San Luis, Chacabuco 915, 5700 San Luis, Argentina
*
Author to whom correspondence should be addressed.
Received: 14 January 2013 / Revised: 31 January 2013 / Accepted: 14 March 2013 / Published: 18 March 2013
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Twenty-five polysubstituted phthalazinone derivatives were synthesized and tested for their antifungal activity against a panel of pathogenic and clinically important yeasts and filamentous fungi. Among them, the compound 4-(4-chlorobenzyl)-2-methylphthalazin-1(2H)-one (5) exhibited a remarkable antifungal activity against standardised strains of dermatophytes and Cryptococcus neoformans, as well as against some clinical isolates. A physicochemical study performed on compound 5 revealed its conformational and electronic characteristics, providing us with useful data for the future design of novel related antifungal analogues. View Full-Text
Keywords: benzylphthalazinones; antifungal; Cryptococcus neoformans; dermatophytes structure–activity relationships; conformational study benzylphthalazinones; antifungal; Cryptococcus neoformans; dermatophytes structure–activity relationships; conformational study
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Derita, M.; del Olmo, E.; Barboza, B.; García-Cadenas, A.E.; López-Pérez, J.L.; Andújar, S.; Enriz, D.; Zacchino, S.; San Feliciano, A. Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents. Molecules 2013, 18, 3479-3501.

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