A series of novel isochroman mono-carboxylic acid derivatives were synthesized, characterized and evaluated for their ability to inhibit protein tyrosine phosphatase 1B (PTP1B) in vitro in order to use them as potential anti-diabetic agents. Analysis of structure–activity relationships led to the identification of potent compound 4n which inhibited PTP1B with IC₅₀ value of 51.63 ± 0.91 nM. In general, high potency was associated with a dithiolane ring with a spacer of five carbons to the isochroman ring. Compound 4n has been selected for in vivo evaluation as drug candidate for anti-diabetic activity.

中文翻译：

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某些新型潜在的抗糖尿病药物异色满羧酸衍生物的合成与评价

合成，表征和评估了其在体外抑制蛋白酪氨酸磷酸酶1B（PTP1B）的能力，以此为潜在的抗糖尿病药物，对一系列新型异色满一元羧酸衍生物进行了表征。通过分析结构-活性之间的关系，可以鉴定出有效的化合物4n，其抑制PTP1B的IC ₅₀值为51.63±0.91 nM。通常，高效能与二硫杂环戊烷环相关，异硫氰酸环具有五个碳原子的间隔基。已选择化合物4n作为抗糖尿病活性的候选药物进行体内评估。