Salazar M O, Osella M I, Ramallo I A, Furlan R L E
Farmacognosia, Departamento de Química Orgánica, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario Suipacha 531 Rosario S2002LRK Argentina
RSC Adv. 2018 Oct 24;8(63):36209-36218. doi: 10.1039/c8ra06625f. eCollection 2018 Oct 22.
-benzenesulfonylhistamine, a new semi-synthetic β-glucosidase inhibitor, was obtained by bioactivity-guided isolation from a chemically engineered extract of L. prepared by reaction with benzenesulfonyl chloride. In order to identify better β-glucosidase inhibitors, a new series of , -di-arylsulfonyl and -arylsulfonyl histamine derivatives was prepared. Biological studies revealed that the β-glucosidase inhibition was in a micromolar range for several -arylsulfonyl histamine compounds of the series, -4-fluorobenzenesulfonyl histamine being the most powerful compound. Besides, this reversible and competitive inhibitor presented a good selectivity for β-glucosidase with respect to other target enzymes including α-glucosidase.
苯磺酰组胺是一种新型半合成β-葡萄糖苷酶抑制剂，通过生物活性导向分离从与苯磺酰氯反应制备的化学工程化的L提取物中获得。为了鉴定更好的β-葡萄糖苷酶抑制剂，制备了一系列新的α，α-二芳基磺酰基和α-芳基磺酰基组胺衍生物。生物学研究表明，该系列中的几种α-芳基磺酰基组胺化合物对β-葡萄糖苷酶的抑制作用在微摩尔范围内，其中α-4-氟苯磺酰基组胺是最强效的化合物。此外，这种可逆性竞争性抑制剂相对于包括α-葡萄糖苷酶在内的其他靶酶对β-葡萄糖苷酶具有良好的选择性。
