On February 1, 2019, Buemi, Maria Rosa; Di Fiore, Anna; De Luca, Laura; Angeli, Andrea; Mancuso, Francesca; Ferro, Stefania; Monti, Simona Maria; Buonanno, Martina; Russo, Emilio; De Sarro, Giovanbattista; De Simone, Giuseppina; Supuran, Claudiu T.; Gitto, Rosaria published an article.Safety of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Exploring structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety. And the article contained the following:
Guided by the crystal structure of 4-(3,4-dihydroquinolin-1(2H)-ylcarbonyl)benzenesulfonamide in complex with hCA II (PDB code 4Z0Q), a novel series of cycloalkylamino-1-carbonylbenzenesulfonamides was designed and synthesized. Thus, we replaced the quinoline ring with an azepine/piperidine/piperazine nucleus and introduced further modifications on cycloalkylamine nucleus by means the installation of hydrophobic/hydrophilic functionalities able to establish addnl. contacts in the middle area of the enzyme cavity. Among the synthesized compounds, the derivatives 7a, 7b, 8b (I – III, resp.) exhibited a remarkable inhibition for hCA II and the brain-expressed hCA VII in sub-nanomolar range. The binding of these mols. to the target enzymes was characterized by means of a crystallog. anal., providing a clear snapshot of the most important interactions established by this class of inhibitors into the hCA II and hCA VII catalytic site. Notably, our results showed that the benzylpiperazine tail of compound 8b is oriented both in hCA II and in hCA VII toward a poorly explored region of the active site. These features should be further investigated for the design of new isoform selective CA inhibitors. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Safety of 4-(4-Chlorophenyl)piperidin-4-ol
The Article related to cycloalkylaminocarbonylbenzenesulfonamide human carbonic anhydrase inhibitor structure, benzenesulfonamides, ca inhibitors, carbonic anhydrases, x-ray crystallography, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Sulfenic, Sulfinic, and Sulfonic Acids and Derivatives and other aspects.Safety of 4-(4-Chlorophenyl)piperidin-4-ol
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem