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 ...