Authors Chauhan, D; George, G; Sridhar, SNC; Bhatia, R; Paul, AT; Monga, V in WILEY-V C H VERLAG GMBH published article about in [Chauhan, Divya; Bhatia, Rohit; Monga, Vikramdeep] ISF Coll Pharm, Dept Pharmaceut Chem, Moga 142001, Punjab, India; [George, Ginson; Sridhar, S. N. C.; Paul, Atish T.] Birla Inst Technol & Sci, Dept Pharm, Lab Nat Prod Chem, Pilani Campus, Pilani 333031, Rajasthan, India in 2019.0, Cited 27.0. Product Details of 93-02-7. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7
A series of rhodanine-3-acetic acid derivatives were synthesized via Knoevenagel condensation of rhodanine-3-acetic acid with various substituted aromatic aldehydes. The synthesized derivatives were screened in vitro for understanding the inhibitory potential towards pancreatic lipase (PL), a key enzyme responsible for the digestion of dietary fats. Derivative 8f exhibited a potential inhibitory activity towards PL (IC50 =( )5.16 mu M), comparable to that of the standard drug, orlistat (0.99 mu M). An increase in the density of the aromatic ring resulted in potential PL inhibition. The enzyme kinetics of 8f exhibited a reversible competitive-type inhibition, similar to that of orlistat. Derivative 8f exhibited a MolDock score of -125.19 kcal/mol in docking studies, and the results were in accordance with their PL inhibitory potential. Furthermore, the reactive carbonyl group of 8f existed at a distance adjacent to Ser152 (approximate to 3 angstrom) similar to that of orlistat. Molecular dynamics simulation (10 ns) of the 8f-PL complex revealed a stable binding conformation of 8f in the active site of PL (maximum root mean square displacement of approximate to 2.25 angstrom). The present study identified novel rhodanine-3-acetic acid derivatives with promising PL inhibitory potential, and further lead optimization might result in potent PL inhibitors.
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