Synthesis and Anticonvulsant Activity Evaluation of 7-Alkoxy[1,2,4]triazolo[3,4-b]benzothiazol-3(2H)-ones was written by Liu, Da-Chuan;Deng, Xian-Qing;Wang, Shi-Ben;Quan, Zhe-Shan. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2014.Computed Properties of C11H14N2OS The following contents are mentioned in the article:
A new series of 7-alkoxy[1,2,4]triazolo[3,4-b]benzothiazol-3(2H)-ones were synthesized and evaluated for their anticonvulsant activities. Among these compounds, 7-propoxy[1,2,4]triazolo[3,4-b]benzothiazol-3(2H)-one and 7-butoxy[1,2,4]triazolo[3,4-b]benzothiazol-3(2H)-one (I) showed the highest activity against maximal electroshock (MES)-induced tonic extension [(ED)50 = 11.4 and 13.6 mg/kg, resp.]. It is worth mentioning that compound I showed especially low neurotoxicity, which led to a high protective index (PI >51). The orally anticonvulsant activity data of compound I further confirmed its efficacy, in an MES test, and its high safety with a PI value of 50.2. In addition, the potency of compound I against seizures induced by pentylenetetrazole, 3-mercaptopropionic acid, and bicuculline in the chem.-induced seizure tests suggested that compound I may exert its anticonvulsant activity through affecting the GABAergic system. This study involved multiple reactions and reactants, such as 6-Butoxybenzo[d]thiazol-2-amine (cas: 14372-65-7Computed Properties of C11H14N2OS).
6-Butoxybenzo[d]thiazol-2-amine (cas: 14372-65-7) 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.Computed Properties of C11H14N2OS
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica