132372-37-3Relevant academic research and scientific papers
Synthesis and aldose reductase inhibitory activity of pyridazine derivatives possessing acetic acid group
Coudert,Rubat,Duroux,Bastide,Couquelet,Tronche,Albuisson
, p. 37 - 46 (2007/10/02)
N-acetic acid and S-acetic acid derivatives of 5-arylidene pyridazines were synthesized for evaluation as new aldose reductase inhibitors. Intrinsic activity for each compound was assessed by measuring inhibition of enzymatic activity in an isolated pig lens enzyme preparation. All prepared compounds exhibited a significant in vitro aldose reductase inhibitory effect (10-5 M ≤ IC50 ≤ 10-4 M). It was found that lipophilicity was important in increasing activity. Furthermore, this activity (log l/IC50) could be correlated directly to a lipophilic parameter (log kw) for the whole data set.
