Weinstock, Joseph published the artcileSynthesis and evaluation of non-catechol D-1 and D-2 dopamine receptor agonists: benzimidazol-2-one, benzoxazol-2-one, and the highly potent: benzothiazol-2-one 7-ethylamines, HPLC of Formula: 108773-00-8, the main research area is benzimidazolone ethylamine preparation dopaminergic; benzoxazolone ethylamine preparation dopaminergic; benzothiazolone ethylamine preparation dopaminergic; dopaminergic benzimidazolone benzoxazolone benzothiazolone; dopamine receptor agonist non catechol.
Title heterocyclic compounds I, II, and III (R = R1 = Pr, R2 = H, Cl, R3 = OH; R = R1 = Pr, H, R2 = R3 = H; R = R2 = H, R1 = H, Me, R3 = OH) were prepared by standard methods. Thus, III (R = R1 = Pr, R2 = Cl, R3 = OH) was prepared from phenylacetic acid IV in several steps in which the key step was the cyclization of aminobenzenethiol V with COCl2 to give III (R = R1 = Pr, R2 = Cl, R3 = OMe). These compounds were evaluated for their affinity and agonist activity at D-1 and D-2 receptors by using in vitro assays. Replacement of the m-hydroxyl in N,N-dipropyldopamine with the thiazol-2-one group resulted in a dramatic increase in D-2 receptor affinity and activity compared to that of N,N-dipropyldopamine or to that of oxindole VI. III (R = R1 = Pr, R2 = H, R3 = OH) is the most potent D-2 receptor agonist reported to date in the field-stimulated rabbit ear artery (ED50 = 0.028 nM). I and II showed D-2 receptor agonist potency similar to that of VI.
Journal of Medicinal Chemistry published new progress about Dopamine agonists. 108773-00-8 belongs to class thiazole, name is 2-Chloro-4-methoxy-7-methylbenzo[d]thiazole, and the molecular formula is C9H8ClNOS, HPLC of Formula: 108773-00-8.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica