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Sulfonamide-1,2,4-thiadiazole Derivatives as Antifungal and Antibacterial Agents: Synthesis, Biological Evaluation, Lipophilicity, and Conformational Studies

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Sulfonamide-1,2,4-thiadiazole Derivatives as Antifungal and Antibacterial Agents: Synthesis, Biological Evaluation, Lipophilicity, and Conformational Studies
Camoutsis, Charalabos
Ciric, Ana
Geronikaki, Athina
Sokovic, Marina
Ζουμπουλάκης, Παναγιώτης
Ζερβού, Μαρία
Άρθρο σε επιστημονικό περιοδικό
2010-02
Tokyo
A series of thirteen new thiadiazole compounds were synthesized and evaluated for in vitro antifungal and antibacterial activity. All compound tested showed significant antifungal activity against all the micromycetes, compared to the commercial fungicide bifonazole. Differences in their activity depend on the substitution of different reactive groups. More specifically, best antifungal activity was shown for the synthetic analogue with methylpiperazine reactive group. Furthermore, it is apparent that different compounds reacted on different ways against bacteria. An effort was made to correlate the above mentioned differences in activity with lipophilicity studies. Furthermore, NMR and molecular modelling were used to obtain the main conformational features of a potent analogue, for future in silica studies.
Χημεία (Γενικά) (EL)
Φαρμακευτική (EL)
Pharmacy and materia medica (EN)
Chemistry (General) (EN)
antifungal
thiadiazole
ketoconazole
antibacterial
Chemistry, Medicinal
Chemistry, Multidisciplinary
bifonazole
English
Pharmaceutical Society Japan
Chemical & Pharmaceutical Bulletin
© PHARMACEUTICAL SOC JAPAN
© PHARMACEUTICAL SOC JAPAN (EN)
National Hellenic Research Foundation (NHRF)
Helios - Repository of the National Hellenic Research Foundation (NHRF)



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