Conventional and microwave irradiated synthesis, biological activity evaluation of highly substituted indole-triazole hybrids

Cebeci Y. U., Ceylan S., Karaoglu S. A.

JOURNAL OF MOLECULAR STRUCTURE, cilt.1250, 2022 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 1250
  • Basım Tarihi: 2022
  • Doi Numarası: 10.1016/j.molstruc.2021.131799
  • Dergi Adı: JOURNAL OF MOLECULAR STRUCTURE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Chemical Abstracts Core, INSPEC
  • Anahtar Kelimeler: 1,2,4-triazole, Fluoroquinolone, Conazole, Antimicrobial activity, ANTIMICROBIAL ACTIVITY EVALUATION, DERIVATIVES, ANTIOXIDANT, ENVIRONMENT, INHIBITORS, DISCOVERY, ANALOGS, MANNICH, DESIGN, AGENTS
  • Recep Tayyip Erdoğan Üniversitesi Adresli: Evet

Özet

In the present study, a series of new indole-3-carbaldehyde embedded triazole derivatives have been synthesized. 4-{[(1E)-1H-indol-3-ylmethylidene]amino}-5-methyl-2,4-dihydro-3H-1,2,4-triazol-3-one (2) were converted to the corresponding Mannich bases containing flouroquinolone core via a one-pot, three-component reaction. The synthesis of conazole analogues was carried out starting from triazoles by three steps. Reactions were carried out under conventional and microwave-mediated conditions. Various catalysts and solvents were tested to see how they affected conventional and microwave (MW)-induced reactions. The antibacterial characteristics of all the newly synthesized compounds were tested, and the majority of them showed good to moderate activity. The most significant result of our investigation is the high activity of fluoroquinolone derivative compounds that we synthesized as hybrid molecules. (C) 2021 Elsevier B.V. All rights reserved.