Abstract：
Novel synthesized pyrimidine derivatives were investigated against carbonic anhydrase isoenzymes I and II (hCA I and II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glycosidase, and aldose reductase (AR) enzymes associated with some common diseases such as epilepsy, glaucoma, Alzheimer\'s disease, diabetes, and neuropathy. When the results were examined, novel synthesized pyrimidine derivatives were found to have effective inhibition abilities toward the metabolic enzymes. IC50 values and Ki values were calculated for each pyrimidine derivative and compared to positive controls. The synthesized novel pyrimidine derivatives exhibited Ki values in the range of 39.16 ± 7.70-144.62 ± 26.98 nM against hCA I, 18.21 ± 3.66-136.35 ± 21.48 nM toward hCA II, which is associated with different pathological and physiological processes, 33.15 ± 4.85-52.98 ± 19.86 nM on AChE, and 31.96 ± 8.24-69.57 ± 21.27 nM on BChE. Also, Ki values were determined in the range of 17.37 ± 1.11-253.88 ± 39.91 nM against α-glycosidase and 648.82 ± 53.74-1902.58 ± 98.90 nM toward AR enzymes. Within the scope of the study, the inhibition types of the novel synthesized pyrimidine derivatives were evaluated.
摘要：
针对碳酸酐酶同工酶I和II（hCAI和II）研究了新合成的嘧啶衍生物，乙酰胆碱酯酶(AChE),丁酰胆碱酯酶(BChE),α-糖苷酶,醛糖还原酶（AR）酶与一些常见疾病，如癫痫，青光眼,老年痴呆症,糖尿病,和神经病。当检查结果时，发现新合成的嘧啶衍生物对代谢酶具有有效的抑制作用。计算每种嘧啶衍生物的IC50值和Ki值,并与阳性对照比较。合成的新型嘧啶衍生物对hCAI的Ki值在39.16±7.70-144.62±26.98nM的范围内，对hCAII的18.21±3.66-136.35±21.48nM，这与不同的病理和生理过程有关，在AChE上为33.15±4.85-52.98±19.86nM，和在BChE上31.96±8.24-69.57±21.27nM。此外，Ki值在针对α-糖苷酶的17.37±1.11-253.88±39.91nM和针对AR酶的648.82±53.74-1902.58±98.90nM的范围内测定。在研究范围内，评价了新合成的嘧啶衍生物的抑制类型。
