Qamar Noshab, Sultan Hira, Raheel Ahmad, Ashfaq Maria, Azmat Rafia, Naz Raheela, Lateef Mehreen, Khan Khalid Mohammed, Arshad Tanzila
Department of Chemistry, University of Karachi, Karachi, Pakistan.
Department of Chemistry, NED University of Engineering and Technology, Karachi, Pakistan.
Pak J Pharm Sci. 2019 May;32(3 (Supplementary)):1179-1183.
The current article discusses the activities of several synthesized metal heterochelates in in-vitro as anti-ulcer agents followed by their docking study. For this purpose, two important ligands like 8-hydroxyquinoline and DL-methionine were used in synthesis of heterochelates of metal including Cr (III), Mn (II), Fe (III), Co (II), Ni (II), Cu (II), Zn (II), Cd (II) and Pb (II). It was observed that these complexes showed excellent urease inhibition activities in which thiourea was the standard having IC value 21.6 ± 0.12μM. The Cu (II) complex showed potent inhibitory activity (22.6 ± 0.72 μM) when compared with the standard thiourea (21.6±0.12μM) among the nine synthesized complexes while Mn (II), Fe (III), Cd (II) and Pb (II) also showed better inhibitory activities. The urease inhibitory activities of hetercochelates also tested and validated by docking analysis.
本文讨论了几种合成金属杂螯合物作为抗溃疡剂在体外的活性及其对接研究。为此，在合成包括Cr（III）、Mn（II）、Fe（III）、Co（II）、Ni（II）、Cu（II）、Zn（II）、Cd（II）和Pb（II）的金属杂螯合物时，使用了8-羟基喹啉和DL-蛋氨酸这两种重要的配体。据观察，这些配合物表现出优异的脲酶抑制活性，其中硫脲为标准物，IC值为21.6±0.12μM。在九种合成配合物中，与标准硫脲（21.6±0.12μM）相比，Cu（II）配合物表现出较强的抑制活性（22.6±0.72μM），而Mn（II）、Fe（III）、Cd（II）和Pb（II）也表现出较好的抑制活性。杂螯合物的脲酶抑制活性也通过对接分析进行了测试和验证。
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