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Synthesis, biological activity and structure activity relationship studies of novel conazole analogues via conventional, microwave and ultrasound mediated techniques.
- Source :
-
Bioorganic chemistry [Bioorg Chem] 2018 Dec; Vol. 81, pp. 55-70. Date of Electronic Publication: 2018 Aug 01. - Publication Year :
- 2018
-
Abstract
- 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-fluorophenyl)piperazine-1-carboxylate via several steps. The synthesis of fifteen compounds (7a-l 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 α-glucosidase activities and promising results were obtained. The enzyme inhibitory potentials of these compounds were further validated through molecular docking.<br /> (Copyright © 2018 Elsevier Inc. All rights reserved.)
- Subjects :
- Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Antifungal Agents chemical synthesis
Antifungal Agents chemistry
Antioxidants chemical synthesis
Antioxidants chemistry
Azoles chemical synthesis
Azoles chemistry
Bacteria drug effects
Canavalia enzymology
Dose-Response Relationship, Drug
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Fungi drug effects
Microbial Sensitivity Tests
Molecular Docking Simulation
Molecular Structure
Structure-Activity Relationship
Urease antagonists & inhibitors
Urease metabolism
alpha-Glucosidases metabolism
Anti-Bacterial Agents pharmacology
Antifungal Agents pharmacology
Antioxidants pharmacology
Azoles pharmacology
Enzyme Inhibitors pharmacology
Microwaves
Ultrasonic Waves
Subjects
Details
- Language :
- English
- ISSN :
- 1090-2120
- Volume :
- 81
- Database :
- MEDLINE
- Journal :
- Bioorganic chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 30118986
- Full Text :
- https://doi.org/10.1016/j.bioorg.2018.07.036