Skip to product information
1 of 1

Independent Author

Synthesis and Biological Evaluation of 6 fluoro 3 piperidin 4 yl benzo d isoxazole derivatives for their Antipsychotic Properties

Synthesis and Biological Evaluation of 6 fluoro 3 piperidin 4 yl benzo d isoxazole derivatives for their Antipsychotic Properties

Regular price €36,95 EUR
Regular price Sale price €36,95 EUR
Sale Sold out
Shipping calculated at checkout.
Format

Our present study focuses on synthesis, characterisation and antipsychotic evaluation of 6-fluoro-3-(piperidin-4-yl) benzo[d]isoxazole derivatives. A new series of benzisoxazole derivatives were synthesized, which are close structural analogs of risperidone, a known second generation antipsychotic drug. The structures of the newly synthesized molecules were confirmed by 1) NMR, LC MS, FTIR and elemental analysis. In silico analysis of the parameters of lipinski s rule of five, along with polar surface area (PSA), absorption%(%ABS), drug likeness indicated that all the synthesized compounds may have prospective role as antipsychotic molecules. In silico structure-toxicity predictions and bioactive scores of synthesized molecules showed identical properties as that of known antipsychotic drugs haloperidol and risperidone. The antipsychotic behavioural studies also indicate the antagonistic property of synthesized molecules (S1-S4) to dopamine D2 and serotonin receptors and also lower propensity to caused extrapyramidal symptoms (EPS). The possibility and efficiency of these synthesized molecules to penetrate through the Blood Brain Barrier is of utmost importance to determine its treatment efficacy. In this line of investigation, in the present study, in silico and in vitro methods are employed to evaluate the permeability in comparison with that of standard antipsychotic drugs, risperidone and haloperidol. In vitro analysis was done by parallel artificial membrane permeability assay (PAMPA) in PBS, where in permeability of S2(8.3x10-6) and S3(6.6x10-6) molecules showed higher permeability than known standards warfarin(1x10-6), risperidone(2.3x10-6) and haloperidol(3.5x10-6), and the molecules exhibited recovery above 50% and in silico studies also showed high permeability rate



Author: Sharath Chandra S. P.
Publisher: Independent Author
Published: 03/19/2023
Pages: 104
Binding Type: Paperback
Weight: 0.36lbs
Size: 9.00h x 6.00w x 0.25d
ISBN: 9781805251224
View full details