Molecules p. 736 - 748 (2008)
Update date:2022-08-05
Topics: Synthesis Characterization Selectivity Optimization Improved Yields Reaction Conditions Efficiency Yield and Purity Conventional Synthesis Microwave Synthesis Reproducibility
Algul, Oztekin
Kaessler, Andre
Apcin, Yagmur
Yilmaz, Akin
Jose, Joachim
We have synthesized twelve 2-substituted benzimidazole, benzothiazole and indole derivatives using on both microwave irradiation and conventional heating methods. The microwave method was observed to be more beneficial as it provides an increase of yield from 3% to 113% and a 95 to 98 % reduction in time. All compounds were tested by a stains-all assay at pH 7 and by a Morgan-Elson assay at pH 3.5 for hyaluronidase inhibitory activity at a concentration of 100 μM. The most potent compound was 2-(4-hydroxyphenyl)-3-phenylindole (12) with an IC50 value of 107 μM at both pH 7 and 3.5.
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