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

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

1
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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.
Keywords: benzylphthalazinones; antifungal; Cryptococcus neoformans; dermatophytes structure–activity relationships; conformational study benzylphthalazinones; antifungal; Cryptococcus neoformans; dermatophytes structure–activity relationships; conformational study
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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