Synthesis and antifungal activity of new hybrids pyrimido[4,5-d]pyridazinone-N-acylhydrazones |
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| Affiliation: | 1. Laboratory of Applied Chemistry and Environment (LCAE), Department of Chemistry, Faculty of Sciences, Mohammed I University, Oujda, Morocco;2. Laboratory of Analytical Chemistry and Bromatology, Faculty of Medicine and Pharmacy, Mohammed V University, Rabat, Morocco;3. Department of Physics, Faculty of Arts and Sciences, OndokuzMayıs University, 55139 Samsun, Turkey;4. Institute of Nursing Professions and Health Techniques Fez, EL Ghassani Hospital, Fez30000, Morocco;5. Cátedra de Química General, Instituto de QuímicaInorgánica, Facultad de Bioquímica, Química y Farmacia, Universidad Nacional de Tucumán, Ayacucho 471, 4000 Tucumán, Argentina |
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| Abstract: | Paracoccidioidomycosis is an endemic mycosis in Latin America for which there is a high mortality rate and limited treatment options. There are no specific drugs to treat the systemic disease. Thus, there is a need for further studies focused on the development of specific drugs. In this work we synthesized new hybrids pyrimido[4,5-d]pyridazinone-N-acylhydrazone (5a-p) by simple methodologies with good yields. The antifungal activity of compounds was evaluated against P. brasiliensis (Pb18) and Candida spp. Compounds 5a, 5f, 5i, 5 k, 5m and 5n showed significant inhibition against Pb18 with MIC of 0.125 to 64 µg mL−1. Compound 5a is the most promising, showing potent fungicidal profile with MFC of 0.5 µg mL−1, synergic effect with amphotericin B, besides showing no toxicity against HeLa and Vero cells. |
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| Keywords: | Paracoccidioidomycosis Fungicidal Neglected disease Antifungal |
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