Synthesis and biological evaluation of a new series of N-acyldiamines as potential antibacterial and antifungal agents |
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| Affiliation: | 1. Departamento de Química, ICE, Universidade Federal de Juiz de Fora, 36036-330 Juiz de Fora, MG, Brazil;2. Departamento de Parasitologia, Microbiologia e Imunologia, ICB, Universidade Federal de Juiz de Fora, 36036-330 Juiz de Fora, MG, Brazil;1. Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi ‘Aldo Moro’ di Bari, Via Orabona 4, 70126 Bari, Italy;2. Università degli Studi di Firenze, Dipartimento di Chimica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy;3. Università degli Studi di Firenze, Neurofarba Dept., Section of Pharmaceutical and Nutriceutical Sciences, Via U. Schiff 6, 50019 Sesto Fiorentino (Firenze), Italy;1. Key Laboratory of Nondestructive Testing Ministry of Education, School of the Testing and Photoelectric Engineering, Nanchang Hangkong University, Nanchang 330063, China;2. Key Laboratory of Novel Thin-Film Solar Cells, Division of Solar Energy Materials and Engineering, Institute of Plasma Physics, Chinese Academy of Sciences, Hefei, Anhui 230031, China;3. State Key Laboratory of Alternate Electrical Power System with Renewable Energy Sources, North China Electric Power University, Beijing 102206, China;1. School of Physical and Molecular Sciences (Chemistry), Al-Falah University, Dhauj, Faridabad, Haryana, 121004, India;2. Departamento de Química Fundamental, Universidade da Coruña, Campus da Zapateira s/n, 15008, ACoruña, Spain;3. Advanced Material Research Group, CNT Lab, ABV-Indian Institute of Information Technology and Management, Gwalior, 474015, India;4. Department of Bioscience, Jamia Millia Islamia, New Delhi, 110025, India |
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| Abstract: | In continuation of our efforts to find new antimicrobial compounds, series of fatty N-acyldiamines were prepared from fatty methyl esters and 1,2-ethylenediamine, 1,3-propanediamine or 1,4-butanediamine. The synthesized compounds were screened for their antibacterial activity against Gram-positive bacteria (Staphylococcus aureus, Staphylococcus epidermidis), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and for their antifungal activity against four species of Candida (C. albicans, C. tropicalis, C. glabrata and C. parapsilosis). Compounds 5a (N-(2-aminoethyl)dodecanamide), 5b (N-(2-aminoethyl)tetracanamide) and 6d (N-(3-aminopropyl)oleamide) were the most active against Gram-positive bacteria, with MIC values ranging from 1 to 16 μg/mL and were evaluated for their activity against 21 clinical isolates of methicillin-resistant S. aureus. All the compounds exhibited good to moderate antifungal activity. Compared to chloramphenicol, compound 6b displayed a similar activity (MIC50 = 16 μg/mL). A positive correlation could be established between lipophilicity and biological activity. |
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| Keywords: | Antibacterial Antifungal MRSA Lipophilicity |
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