Synthesis and Carbonic Anhydrase Inhibition of Novel 2-(4-(Aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione Derivatives was written by Kocyigit, Umit M.;Aslan, Osman Nuri;Gulcin, Ilhami;Temel, Yusuf;Ceylan, Mustafa. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2016.Reference of 6318-74-7 This article mentions the following:
A number of 2-(4-(aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives were synthesized and evaluated for their inhibitory characteristics against the human CA isoenzymes I and II (hCA I and hCA II). The structures of the new isoindolylthiazole derivatives were confirmed by means of IR, 1H NMR, 13C NMR, and elemental anal. These compounds exhibited excellent inhibitory effects, in the low nanomolar range, with Ki values in the range of 27.07-37.80 nM against hCA I and in the range of 11.80-25.81 nM against hCA II. Our findings suggested that the new isoindolylthiazole derivatives have superior inhibitory effect over acetazolamide (AZA), which was used as clin. CA inhibitor with Ki values of 34.50 and 28.93 nM against the hCA I and hCA II isoenzymes, resp. In the experiment, the researchers used many compounds, for example, 4,5-Diphenylthiazol-2-amine (cas: 6318-74-7Reference of 6318-74-7).
4,5-Diphenylthiazol-2-amine (cas: 6318-74-7) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Reference of 6318-74-7
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica