Author:
D’hooghe Matthias,Vandekerckhove Stéphanie,Mollet Karen,Vervisch Karel,Dekeukeleire Stijn,Lehoucq Liesbeth,Lategan Carmen,Smith Peter J,Chibale Kelly,De Kimpe Norbert
Abstract
A variety of 2-amino-3-arylpropan-1-ols, anti-2-amino-3-aryl-3-methoxypropan-1-ols and anti-2-amino-1-arylpropan-1,3-diols were prepared selectively through elaboration of trans-4-aryl-3-chloro-β-lactams. In addition, a number of 2-(azidomethyl)aziridines was converted into novel 2-[(1,2,3-triazol-1-yl)methyl]aziridines by Cu(I)-catalyzed azide-alkyne cycloaddition, followed by microwave-assisted, regioselective ring opening by dialkylamine towards 1-(2,3-diaminopropyl)-1,2,3-triazoles. Although most of these compounds exhibited weak antiplasmodial activity, six representatives showed moderate antiplasmodial activity against both a chloroquine-sensitive and a chloroquine-resistant strain of Plasmodium falciparum with IC50-values of ≤25 μM.
Cited by
29 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献
1. An efficient microwave assisted synthesis of (E)-1-(2,4-Bis((1-Aryl-1H-1,2,3-Triazol-4-YL) Methoxy) Phenyl)-3-(2-(Pyrrolidin-1-YL) Quinolin-3-YL) Prop-2-En-1-Ones and their antimicrobial activity;Chemical Data Collections;2023-08
2. Synthesis of 4-Amino-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)one-[1,2,3]triazolebenzenesulphonamide
Bioactive Hybrids as Novel Therapeutic Agents;Asian Journal of Chemistry;2023
3. Predicting new potential antimalarial compounds by using Zagreb topological indices;AIP Advances;2022-04-01
4. Bioactive 1,2,3‐Triazoles: An Account on their Synthesis, Structural Diversity and Biological Applications;The Chemical Record;2021-02-11
5. 1,2,3-Triazoles: Lead Molecules For Promising Drugs: A Review;Asian Journal of Chemistry;2021