Burmaoglu Serdar, Yilmaz Ali Osman, Polat M Fatih, Kaya Rüya, Gulcin İlhami, Algul Oztekin
Tercan Vocational High School, Erzincan Binali Yildirim University, Erzincan, Turkey.
Department of Chemistry, Faculty of Science, Atatürk University, Erzurum, Turkey.
Arch Physiol Biochem. 2021 Apr;127(2):153-161. doi: 10.1080/13813455.2019.1623265. Epub 2019 Jun 7.
In this study, we report the synthesis of novel tris-chalcones and testing of human carbonic anhydrase I, and II isoenzymes (hCA I, and hCA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and -glycosidase (-Gly) inhibitors for the development of novel chalcone structures towards for treatment of some diseases. The compounds demonstrated values between 13.6 ± 1.1 and 50.0 ± 17.1 nM on hCA I, 9.9 ± 0.8 and 39.5 ± 15.1 nM on hCA II, 3.1 ± 0.2 and 20.1 ± 1.9 nM on AChE, 4.9 ± 0.4 and 14.7 ± 5.2 nM on BChE and 3.9 ± 0.2 and 22.4 ± 10.7 nM on -Gly enzymes. The results revealed that novel tris-chalcones can have promising drug potential for glaucoma, leukaemia, epilepsy; Alzheimer's disease that was associated with the high enzymatic activity of hCA I, hCA II, AChE, and BChE enzymes.
在本研究中，我们报告了新型三查耳酮的合成以及对人碳酸酐酶I和II同工酶（hCA I和hCA II）、乙酰胆碱酯酶（AChE）、丁酰胆碱酯酶（BChE）和β-糖苷酶（β-Gly）抑制剂的测试，以开发用于治疗某些疾病的新型查耳酮结构。这些化合物对hCA I的抑制常数（Ki）值在13.6±1.1至50.0±17.1 nM之间，对hCA II的抑制常数（Ki）值在9.9±0.8至39.5±15.1 nM之间，对AChE的抑制常数（Ki）值在3.1±0.2至20.1±1.9 nM之间，对BChE的抑制常数（Ki）值在4.9±0.4至14.7±5.2 nM之间，对β-Gly酶的抑制常数（Ki）值在3.9±0.2至22.4±10.7 nM之间。结果表明，新型三查耳酮对于青光眼、白血病、癫痫；与hCA I、hCA II、AChE和BChE酶的高酶活性相关的阿尔茨海默病可能具有有前景的药物潜力。
