An article Design, synthesis and evaluation of dihydropyranoindole derivatives as potential cholinesterase inhibitors against Alzheimer’s disease WOS:000647575300007 published article about INDOLE-DERIVATIVES; BIOLOGICAL EVALUATION; ACETYLCHOLINESTERASE; AGENTS; ANTIOXIDANT; RAT in [Shaikh, Sarfaraz; Pavale, Ganesh; Uparkar, Jasmin; Ramana, M. M., V] Univ Mumbai, Dept Chem, Santacruz E, Mumbai 400098, Maharashtra, India; [Dhavan, Pratik; Jadhav, B. L.] Univ Mumbai, Dept Life Sci, Santacruz E, Mumbai 400098, Maharashtra, India; [Singh, Pinky; Vaidya, S. P.] Haffkine Inst, Dept Microbiol, Mumbai 400012, Maharashtra, India in 2021, Cited 41. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5. HPLC of Formula: C8H8O2
A series of novel dihydropyranoindole derivatives containing sulphonamide group were designed, synthesized and evaluated for in-vitro anti-cholinesterase activity. The result showed that all the compounds exhibited potent acetylcholinesterase (AChE) activity (IC50 = 0.41-8.79 mu M) while demonstrated moderate to good activity for butyrylcholinesterase (BuChE) (IC50 = 1.17-30.17 mu M). The tested compounds exhibited selectivity towards AChE over BuChE. Compound 5o was most potent towards both AChE (IC50 = 0.41 mu M) and BuChE (IC50 = 1.17 mu M) when compared to standard galantamine and rivastigmine. Enzyme kinetics and molecular docking studies revealed that compound 5o shows mixed type inhibition and binds to peripheral anionic site (PAS) and the catalytic sites (CAS) of both the enzymes. Furthermore, cell viability studies were also performed against N2a cells along with neuroprotection studies against H2O2 in the same cell line. Antioxidant studies using DPPH radical and H2O2 were also performed which revealed that all compounds possessed some antioxidant activity. Also, DNA damage protection assay for compound 5o was performed implying that compound 5o was protective in nature. ADME studies were also performed which demonstrated good pharmacokinetics. These findings indicated that dihydropyranoindole derivatives could be possible drug lead in the search for new multifunctional AD drugs.
About 4-Methoxybenzaldehyde, If you have any questions, you can contact Shaikh, S; Pavale, G; Dhavan, P; Singh, P; Uparkar, J; Vaidya, SP; Jadhav, BL; Ramana, MMV or concate me.. Formula: C8H8O2
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles