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Carbonic Anhydrase Inhibitors Part 721 Synthesis and Antiglaucoma Properties of Metal Complexes of p-Fluorobenzolamide

机译:碳酸酐酶抑制剂721部分 合成与抗青光眼 对氟苯甲酰胺金属配合物的性质

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摘要

Metal complexes of a heterocyclic sulfonamides possessing very strong carbonic anhydrase (CA)inhibitory properties, i.e., 5-(p-fluorobenzenesulfonylamido)-1,3,4-thiadiazole-2-sulfonamide (p-fluorobenzolamide)were prepared. The new complexes contained metal ions such as Zn(II), Cu(II), Co(II), Ni(II),Cd(II) and Mn(II). The new compounds were characterized by standard physico-chemical procedures, andassayed as inhibitors of three CA isozymes, CA I, II and IV. Very good inhibition has been evidenced bothfor the parent sulfonamides as well as for the prepared complexes, against all three investigated isozymes.Some of these new complexes as well as the parent sulfonamide, strongly lowered intraocular pressure (IOP)in normotensive rabbits when administered as a 2% solution into the eye.
机译:制备具有非常强的碳酸酐酶(CA)抑制特性的杂环磺酰胺的金属配合物,即5-(对氟苯磺酰胺基)-1,3,4-噻二唑-2-磺酰胺(对氟苯甲酰胺)。新的络合物包含金属离子,例如Zn(II),Cu(II),Co(II),Ni(II),Cd(II)和Mn(II)。通过标准物理化学方法对新化合物进行了表征,并测定为三种CA同工酶CA I,II和IV的抑制剂。已证明母体磺酰胺类和制备的复合物对所有三种研究的同工酶均具有很好的抑制作用。当这些新复合物以及母体磺酰胺以一定剂量给药时,降血压兔的眼压(IOP)会大大降低。 2%溶液进入眼睛。

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