Patel, Dushyant V. published the artcileNovel carbazole-stilbene hybrids as multifunctional anti-Alzheimer agents, Related Products of catalysis-chemistry, the publication is Bioorganic Chemistry (2020), 103977, database is CAplus and MEDLINE.
Mols. capable of engaging with multiple targets associated with pathol. condition of Alzheimer’s disease have proved to be potential anti-Alzheimer’s agents. The goal to develop multitarget-directed ligands for the treatment of Alzheimer’s disease, a novel series of carbazole-based stilbene derivatives (E)-I [R = H, NH2, 4-chlorobutanamidyl, 4-(pyrrolidin-1-yl)butanamidyl, ([3-(piperidin-1-yl)propyl]carbamoyl)azanyl, etc.; R1 = H, NO2, NH2, 2-chloroacetamidyl, ([2-(pyrrolidin-1-yl)ethyl]carbamothioyl)azanyl, etc.] was designed by the fusion of carbazole ring with stilbene scaffold. The designed compounds (E)-I were synthesized and evaluated for their anti-AD activities including cholinesterase inhibition, A¦Â aggregation inhibition, antioxidant and metal chelation properties. Amongst them, (E)-I [R = H; R1 = ([2-(pyrrolidin-1-yl)ethyl]carbamothioyl)azanyl, (A)] appeared to be the best candidate with good inhibitory activities against AChE (IC50 value of 2.64¦ÌM) and BuChE (IC50 value of 1.29¦ÌM), and significant inhibition of self-mediated A¦Â1-42 aggregation (51.29% at 25¦ÌM concentration). The metal chelation study showed that compound (A) possessed specific copper ion chelating property. Addnl., compound (A) exhibited moderate antioxidant activity. To understand the binding mode of (A), mol. docking studies were performed, and the results indicated strong non-covalent interactions of (A) with the enzymes in the active sites of AChE, BuChE as well as of the A¦Â1-42 peptide. Addnl., it showed promising in silico ADMET properties. Putting together, these findings evidently showed compound (A) as a potential multitarget-directed ligand in the course of developing novel anti-AD drugs.
Bioorganic Chemistry published new progress about 104-03-0. 104-03-0 belongs to catalysis-chemistry, auxiliary class Nitro Compound,Carboxylic acid,Benzene, name is 4-Nitrophenylacetic acid, and the molecular formula is C8H7NO4, Related Products of catalysis-chemistry.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia