Synthesis, biological activity and structure activity relationship studies of novel conazole analogues via conventional, microwave and ultrasound mediated techniques

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Atıf İçin Kopyala

MERMER A., DEMİRBAŞ N., DEMİRBAŞ A., ÇOLAK N., AYAZ F. A., Alagumuthu M., ...Daha Fazla

BIOORGANIC CHEMISTRY, cilt.81, ss.55-70, 2018 (SCI-Expanded)

• Yayın Türü: Makale / Tam Makale
• Cilt numarası: 81
• Basım Tarihi: 2018
• Doi Numarası: 10.1016/j.bioorg.2018.07.036
• Dergi Adı: BIOORGANIC CHEMISTRY
• Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
• Sayfa Sayıları: ss.55-70
• Anahtar Kelimeler: alpha-Glucosidase activity, Antimicrobial, Antioxidants, Conazole, Microwave irradiation, Molecular docking, Ultrasound sonication, Urease activity, GLUCOSIDASE INHIBITION, ANTIMICROBIAL ACTIVITY, ASSISTED SYNTHESIS, MOLECULAR DOCKING, ORGANIC-SYNTHESIS, HYBRID MOLECULES, DRUG-RESISTANCE, SOLVENT-FREE, DERIVATIVES, DISCOVERY
• Karadeniz Teknik Üniversitesi Adresli: Evet

Özet

1,2,4-Triazole derivatives containing a piperazine nucleus (4a-d and 10) were prepared starting from 1-(2-methoxyphenyl)piperazine or ethyl 4-(4-amino-2-fluorophenyepiperazine-1-carboxylate via several steps. The synthesis of fifteen compounds (7a-1 and 13a-c), which can be considered as new analogues of azole class antifungals was performed starting from 1,2,4-triazoles (4a-d and 10) via three steps containing the condensation with 2-bromo-1-(4-chlorophenyl)ethanone, reduction of carbonyl group to alcohol and alkylation of OH group, respectively. All the reactions were examined under conventional, ultrasound and microwave irradiation conditions as green chemistry techniques, and optimum conditions were defined. The newly synthesized compounds were screened for their biological potentials including antimicrobial, antioxidant, antiurease and anti a-glucosidase activities and promising results were obtained. The enzyme inhibitory potentials of these compounds were further validated through molecular docking.