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首页> 外文期刊>Archiv der Pharmazie >Ureas/thioureas of benzo[d]isothiazole analog conjugated glutamic acid: Synthesis and biological evaluation
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Ureas/thioureas of benzo[d]isothiazole analog conjugated glutamic acid: Synthesis and biological evaluation

机译:苯并[d]异噻唑类似物共轭谷氨酸的尿素/硫脲:合成与生物学评价

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摘要

A series of urea and thiourea derivatives of glutamic acid conjugated to 3-(1-piperazinyl)-1,2-benzisothiazole were synthesized, spectroscopically characterized, and evaluated for their in vitro antiglycation and urease inhibitory activities. Preliminary screening of the synthesized compounds 1-35 showed significant results. Amongst these, compounds 17-21 and 30-35 bearing fluoro and methoxy substituents, respectively, exhibited inhibitory potency greater than the reference standards. Hence, they may serve as new lead compounds for further development. Urea and thiourea derivatives of glutamic acid conjugated to 3-(1-piperazinyl)-1,2-benzisothiazole were evaluated for their in vitro antiglycation and urease inhibitory activities. Compounds 17-21 and 30-35 bearing fluoro and methoxy substituents, respectively, exhibited inhibitory potency greater than the reference compounds.
机译:合成了一系列与3-(1-哌嗪基)-1,2-苯并噻唑共轭的谷氨酸尿素和硫脲衍生物,对其进行了光谱表征,并评价了它们的体外抗糖化和脲酶抑制活性。合成化合物1-35的初步筛选显示了显着结果。在这些化合物中,分别带有氟和甲氧基取代基的化合物17-21和30-35表现出比参考标准更高的抑制效力。因此,它们可以用作进一步开发的新的先导化合物。评价了谷氨酸的尿素和硫脲衍生物与3-(1-哌嗪基)-1,2-苯并噻唑共轭的体外抗糖基化和脲酶抑制活性。分别带有氟和甲氧基取代基的化合物17-21和30-35表现出比参考化合物更大的抑制效力。

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