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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >1H -benzo[d]imidazoles evaluated as effective H + /K + -ATPase inhibitors and anti-ulcer therapeutics
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1H -benzo[d]imidazoles evaluated as effective H + /K + -ATPase inhibitors and anti-ulcer therapeutics

机译：1H -benzo [D]咪唑评估为有效的H + / K + -ATP酶抑制剂和抗溃疡治疗剂

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Abstract Efforts were made to synthesize a series of substituted methoxybenzyl-sulfonyl- 1H -benzo[d]imidazole derivatives ( 8a-l ) and investigate their anti-ulcer therapeutics. Prior to evaluating antiulcer potentials of 8a-l , a preliminary binding assay against H + /K + -ATPase from goat gastric mucosa was carried out, since it plays an important role in the ulcer development. In order to get more insight into the binding mode of the compounds to H + /K + -ATPase, a molecular docking study was carried out and the best binding affinities were unveiled. Many of the substituted methoxybenzyl-sulfonyl- 1H -benzo[d]imidazole derivatives ( 8a-l ) were active for the proposed activity. The key finding was that, least inhibitory constant ( ki ) values of 8a-l were found between 0.02 and 1.8?μM in the molecular docking study. Almost the same range was reflected/correlated in the H + /K + -ATPase inhibition assay (IC 50 0.14–1.29?μM). Remarkably, compounds 8a-l showed a relative activity percentage range of 72–92%. Efficient HRBC membrane stabilization activity of 8a-l ensured the non-harm/safety and the suitability/alternative towards anti-ulcer therapy. Graphical abstract Display Omitted Highlights ? Substituted methoxybenzyl-sulfonyl- 1H -benzo[d]imidazoles ( 8a-l ) developed as anti-ulcer therapeutic. ? Preliminary binding assay against H + /K + -ATPase from goat gastric mucosa was executed. ? Effective inhibition of H + /K + -ATPase is the key ulcer therapeutic sign. ? 8a-l showed relative activity percentage range of 72–92%.
机译：摘要采用努力合成一系列取代的甲氧基苄基 - 磺酰基-1H- -benzo [D]咪唑衍生物（8a -1）并研究其抗溃疡治疗剂。在评估8A-L的抗燃烧电势之前，进行了山羊胃粘膜的H + / K + -ATP酶的初步结合测定，因为它在溃疡发育中起重要作用。为了使化合物的结合模式更加洞察于H + / K + -ATP酶，进行分子对接研究，揭开了最佳的结合亲和力。许多取代的甲氧基苄基 - 磺酰基-1H-Benzo [D]咪唑衍生物（8A-1）是拟议活性的活性。关键发现是，在分子对接研究中，在0.02和1.8μm之间发现了8a-l的最小抑制常数（ki）值。在H + / K + -ATP酶抑制测定中反映/相关的几乎相同的范围（IC 500.14-1.29≤μm）。值得注意的是，化合物8A-L显示出相对活性百分比范围为72-92％。 8A-L的高效HRBC膜稳定活性确保了非危害/安全性和适用性/替代抗溃疡疗法。图形抽象显示省略了亮点？取代的甲氧基苄基 - 磺酰基-1H-Benzo [D]咪唑（8A-L）开发为抗溃疡治疗。还是对来自山羊胃粘膜的H + / K + -ATP酶进行初步结合测定。还是有效抑制H + / K + -ATPase是关键溃疡治疗标志。还是图8A-L显示相对活性百分比范围为72-92％。

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