A short synthesis of 7-amino alkoxy homoisoflavonoides

The synthesis of novel derivatives of homoisoflavonoids as potentially interesting medicinally important heterocycles in an efficient catalytic alternative two-step route has been introduced

Amino-7,8-dihydro-4H-chromenone derivatives as potential inhibitors of acetylcholinesterase and butyrylcholinesterase for Alzheimer’s disease management; in vitro and in silico study

Abstract In this article, we present the design and synthesis of amino-7,8-dihydro-4H-chromenone derivatives as possible inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) for the management of Alzheimer’s disease (AD). The target compounds were evaluated against AChE and BChE in vitro, and 4k exhibited good potency against BChE (IC50 = 0.65 ± 0.13 µM) compared with donepezil used as a positive control. Kinetic studies revealed that compound 4k exhibited a competitive-type inhibition with a K i value of 0.55 µM. Molecular docking and molecular dynamics simulations further supported the rationality of our design strategy, as 4k showed promising binding interactions with the active sites of BChE. Overall, our findings highlight the potential of amino-7,8-dihydro-4H-chromenone derivatives as promising candidates for developing novel therapeutics targeting cholinesterase in managing AD

Synthesis and Evaluation of Coumarin–Resveratrol Hybrids as 15-Lipoxygenaze Inhibitors

<div><p></p><p>A series of coumarin–resveratrol hybrids, 3-arylcoumarin derivatives <b>3a–u</b>, were synthesized through the intermolecular condensation reaction of various salicylaldehydes and phenylacetic acids in the presence of 1,4-diazabicyclo[2.2.2]octane under solvent-free conditions. All the synthesized compounds were screened for their inhibitory potency against soybean 15-lipoxygenase. Among them, three compounds (<b>3c</b>, <b>3j</b>, and <b>3q</b>) showed good enzyme-inhibitory activities.</p></div

Additional file 1 of Amino-7,8-dihydro-4H-chromenone derivatives as potential inhibitors of acetylcholinesterase and butyrylcholinesterase for Alzheimer’s disease management; in vitro and in silico study

Additional file 1. Fig. S1. 1H NMR spectrum of product 4c. Fig. S2. 13CNMR spectrum of product 4c. Fig. S3. 1H NMR spectrum of product 4d. Fig. S4. 13CNMR spectrum of product 4d. Fig. S5. 1H NMR spectrum of product 4e. Fig. S6. 13CNMR spectrum of product 4e. Fig. S7. 1H NMR spectrum of product 4f. Fig. S8. 13CNMR spectrum of product 4f. Fig. S9. 1H NMR spectrum of product 4g. Fig. S10. 13CNMR spectrum of product 4g. Fig. S11. 1H NMR spectrum of product 4h. Fig. S12. 13CNMR spectrum of product 4h. Fig. S13. 1H NMR spectrum of product 4i. Fig. S14. 13CNMR spectrum of product 4i. Fig. S15. 1H NMR spectrum of product 4j. Fig. S16. 13CNMR spectrum of product 4j. Fig. S17. 1H NMR spectrum of product 4k. Fig. S18. 13CNMR spectrum of product 4k. Fig. S19. 1H NMR spectrum of product 4l. Fig. S20. 13CNMR spectrum of product 4l. Fig. S21. 1H NMR spectrum of product 4m. Fig. S22. 13CNMR spectrum of product 4