Shidore, Mahesh published the artcileBenzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer’s Agents: Synthesis and Biological Evaluation, HPLC of Formula: 39546-32-2, the publication is Journal of Medicinal Chemistry (2016), 59(12), 5823-5846, database is CAplus and MEDLINE.
A novel series of hybrid mols. were designed and synthesized by fusing the pharmacophoric features of cholinesterase inhibitor donepezil and diarylthiazole as potential multitarget-directed ligands for the treatment of Alzheimer’s disease (AD). The compounds showed significant in vitro anticholinesterase (anti-ChE) activity, the most potent compound I among them showing the highest activity (IC50 value of 0.30 ± 0.01 μM) for AChE and (1.84 ± 0.03 μM) for BuChE. Compound I showed mixed inhibition of AChE in the enzyme kinetic studies. Some compounds exhibited moderate to high inhibition of AChE-induced Aβ1-42 aggregation and noticeable in vitro antioxidant and antiapoptotic properties. Compound I showed significant in vivo anti-ChE and antioxidant activities. Furthermore, compound I demonstrated in vivo neuroprotection by decreasing Aβ1-42-induced toxicity by attenuating abnormal levels of Aβ1-42, p-Tau, cleaved caspase-3, and cleaved PARP proteins. Compound I exhibited good oral absorption and was well tolerated up to 2000 mg/kg, po, dose without showing toxic effects.
Journal of Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C8H8O3, HPLC of Formula: 39546-32-2.
Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem