Algul Oztekin, Kaessler Andre, Apcin Yagmur, Yilmaz Akin, Jose Joachim
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin 33169, Turkey.
Molecules. 2008 Mar 27;13(4):736-48. doi: 10.3390/molecules13040736.
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 microM. The most potent compound was 2-(4-hydroxyphenyl)-3-phenylindole (12) with an IC(50) value of 107 microM at both pH 7 and 3.5.
我们使用微波辐射和传统加热方法合成了十二种2-取代苯并咪唑、苯并噻唑和吲哚衍生物。观察到微波方法更具优势，因为它能使产率从3%提高到113%，并将时间缩短95%至98%。所有化合物均在pH 7下通过全染色试验以及在pH 3.5下通过摩根-埃尔森试验进行测试，以检测其在100微摩尔浓度下的透明质酸酶抑制活性。最有效的化合物是2-(4-羟基苯基)-3-苯基吲哚(12)，在pH 7和3.5时的IC(50)值均为107微摩尔。
