On June 30, 2019, Abo-Ashour, Mahmoud F.; Eldehna, Wagdy M.; Nocentini, Alessio; Ibrahim, Hany S.; Bua, Silvia; Abdel-Aziz, Hatem A.; Abou-Seri, Sahar M.; Supuran, Claudiu T. published an article.Synthetic Route of 2010-06-2 The title of the article was Novel synthesized SLC-0111 thiazole and thiadiazole analogues: Determination of their carbonic anhydrase inhibitory activity and molecular modeling studies. And the article contained the following:
In the presented work, we report the design and synthesis of novel SLC-0111 thiazole and thiadiazole analogs (11a-d, 12a-d, 16a-c and 17a-d). A bioisosteric replacement approach was adopted to replace the 4-fluorophenyl tail of SLC-0111 with thiazole and thiadiazole ones, which were thereafter extended with lipophilic un/substituted Ph moieties. All the newly synthesized SLC-0111 analogs were evaluated in vitro for their inhibitory activity towards a panel of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) isoforms (hCA I, II, IX and XII), using a stopped-flow CO2 hydrase assay. All the examined isoforms were inhibited by the primary sulfonamide derivatives (11a-d and 12a-d) in variable degrees with the following KI ranges: 162.6-7136 nM for hCA I, 9.0-833.6 nM for hCA II, 7.9-153.0 nM for hCA IX, and 9.4-94.0 nM for hCA XII. In particular, compounds 12b and 12d displayed 5.5-fold more potent inhibitory activity (KIs = 8.3 and 7.9 nM, resp.) than SLC-0111 (KI = 45 nM) towards hCA IX. Mol. docking study was carried out for 12d within the hCA IX (PDB 3IAI) active site, to justify its inhibitory activity. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Synthetic Route of 2010-06-2
The Article related to carbonic anhydrase inhibitors mol docking slc0111 analogs, carbonic anhydrase inhibitors, molecular docking, slc-0111 analogues, thiazoles and thiadiazoles, ureido-benzenesulfonamide and other aspects.Synthetic Route of 2010-06-2
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica