Synthesis, molecular docking studies, and in vitro screening of sulfanilamide-thiourea hybrids as antimicrobial urease inhibitors

Aamer Saeed; Sumera Zaib; Arshid Pervez; Amara Mumtaz; Mohammad Shahid; Jamshed Iqbal

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Synthesis, molecular docking studies, and in vitro screening of sulfanilamide-thiourea hybrids as antimicrobial urease inhibitors

机译：磺胺-硫脲杂化物作为抗微生物脲酶抑制剂的合成，分子对接研究和体外筛选

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A series of novel hybrid molecules containing sulfanilamide and thiourea templates was designed and synthesized. These compounds were screened for antimicrobial and urease inhibitory activities. Some of the compounds revealed promising antibacterial and antifungal activities. Fascinatingly, the majority of the compounds exhibited potential urease inhibitory activities with IC50 ranging from 0.20 to 7.50 muM. Compound 2b was identified as the most potent urease inhibitor (IC50 0.20 muM), and was 100-fold more potent than thiourea, the standard inhibitor. Molecular docking studies of compounds were performed on 3D crystal structures of Jack bean and Helicobacter pylori ureases.

机译：设计并合成了一系列含有磺胺和硫脲模板的新型杂化分子。筛选了这些化合物的抗微生物和脲酶抑制活性。一些化合物显示出令人鼓舞的抗菌和抗真菌活性。令人着迷的是，大多数化合物显示出潜在的脲酶抑制活性，IC50为0.20至7.50μM。化合物2b被确定为最有效的脲酶抑制剂（IC50为0.20μM），并且比标准抑制剂硫脲的效力高100倍。化合物的分子对接研究是在Jack bean和幽门螺杆菌脲酶的3D晶体结构上进行的。

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《Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents》 |2013年第8期|共10页
作者
Aamer Saeed; Sumera Zaib; Arshid Pervez; Amara Mumtaz; Mohammad Shahid; Jamshed Iqbal;
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正文语种 eng
中图分类药学;
关键词
1 -Aroyl-3-(4-aminosulfonylphenyl)thioureas; Sulfanilamide-thiourea hybrids; Antibacterial activity; Molecular docking; Urease inhibition;

机译：1-Aroyl-3-（4-aminosulfonylphenyl）thioureas;Sulfanilamide-thiourea hybrids;抗菌活性;分子对接;脲酶抑制;

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1. Synthesis, molecular docking studies, and in vitro screening of sulfanilamide-thiourea hybrids as antimicrobial urease inhibitors [J] . Aamer Saeed, Sumera Zaib, Arshid Pervez, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2013,第8期

机译：磺胺-硫脲杂化物作为抗微生物脲酶抑制剂的合成，分子对接研究和体外筛选
2. Synthesis, biological assay in vitro and molecular docking studies of new Schiff base derivatives as potential urease inhibitors. [J] . Aslam MA, Mahmood SU, Shahid M, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2011,第11期

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5. 1alpha,25-dihydroxyvitamin D3 Agonist and Histone Deacetylase Inhibitor Bifunctional Ligand Discovery Virtual Docking, Synthesis, Fluorescence Polarization-Based Screening, and Molecular Dynamics Simulations . [D] . Burger, Melanie C. 2011

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6. Synthesis Antimicrobial Screening Homology Modeling and Molecular Docking Studies of a New Series of Schiff Base Derivatives as Prospective Fungal Inhibitor Candidates [O] . Yahya Toubi, Farid Abrigach, Smaail Radi, 2019

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机译：新一系列席夫碱衍生物作为前瞻性真菌抑制剂候选人的合成，抗菌筛查，同源性建模和分子对接研究

Synthesis, molecular docking studies, and in vitro screening of sulfanilamide-thiourea hybrids as antimicrobial urease inhibitors

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