(2-Aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines as NHE-1 inhibitors.

Lee S; Yi KY; Youn SJ; Lee BH; Yoo SE

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(2-Aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines as NHE-1 inhibitors.

机译：（2-芳基-5-甲基咪唑-4-基羰基）胍和（2-芳基-5-甲基恶唑-4-基羰基）胍作为NHE-1抑制剂。

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A series of (2-aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines were synthesized and evaluated as NHE-1 inhibitors. The structure-activity relationships well matched those of furan derivatives, which were previously investigated. The (2,5-disubstituted)phenyl compounds showed better activities than the other analogues in both imidazole and oxazole compounds. Especially, 2-(2,5-dichlorophenyl)imidazole 52, and 2-(2-methoxy-5-chlorophenyl)imidazole 54 compounds exhibited potent cardioprotective efficacy both in vitro and in vivo as well as high NHE-1 inhibitory activities.

机译：合成了一系列（2-芳基-5-甲基咪唑-4-基羰基）胍和（2-芳基-5-甲基恶唑-4-基羰基）胍，并将其评估为NHE-1抑制剂。结构-活性关系很好地匹配了呋喃衍生物，以前已经进行了研究。在咪唑和恶唑化合物中，（2,5-二取代）苯基化合物均显示出比其他类似物更好的活性。特别是2-（2，5-二氯苯基）咪唑52和2-（2-甲氧基-5-氯苯基）咪唑54化合物在体外和体内均显示出强力的心脏保护功效以及高的NHE-1抑制活性。

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《Bioorganic and Medicinal Chemistry Letters》 |2009年第5期|共3页
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Lee S; Yi KY; Youn SJ; Lee BH; Yoo SE;
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1. (2-Aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines as NHE-1 inhibitors. [J] . Lee S, Yi KY, Youn SJ, Bioorganic and Medicinal Chemistry Letters . 2009,第5期

机译：（2-芳基-5-甲基咪唑-4-基羰基）胍和（2-芳基-5-甲基恶唑-4-基羰基）胍作为NHE-1抑制剂。
2. 3-Substituted-(5-arylfuran-2-ylcarbonyl)guanidines as NHE-1 inhibitors. [J] . Lee S, Kim T, Lee BH, Bioorganic and Medicinal Chemistry Letters . 2007,第5期

机译：3-取代的（5-芳基呋喃-2-基羰基）胍作为NHE-1抑制剂。
3. 4-Substituted (benzo(b)thiophene-2-carbonyl)guanidines as novel Na+/H+ exchanger isoform-1 (NHE-1) inhibitors. [J] . Lee S, Lee H, Yi KY, Bioorganic and Medicinal Chemistry Letters . 2005,第12期

机译：4-取代（苯并（b）噻吩-2-羰基）胍作为新型的Na + / H +交换异构体1（NHE-1）抑制剂。
4. Synthesis of 5-benzylidene-hydantoin and 5-benzylidene-creatinine derivatives under mixed catalyst systems of urea-p-toluenesulfonic acid (Urea-PTSA) and guanidine hydrochloride-triethylamine (GnHCl-TEA) [C] . Kautsar Ul Haq, Septi Rosiana Dewi, Sherly Dwi Cicilianingrum, Joint Conference on Chemistry . 2020

机译：尿素 - 对甲苯磺酸（尿素-PTSA）混合催化剂体系中的5-苄基 - 乙内酰胺和5-苄基 - 肌酐衍生物的合成，盐酸盐 - 三乙胺（GNHCL-TEA）
5. A new guanidinylation procedure for the preparation of functionalized guanidines and investigations towards the synthesis of cyclic guanidine compounds. [D] . Ramsden, Philip Dean. 2003

机译：一种新的胍基化方法，用于制备功能化的胍和研究合成环状胍化合物。
6. Interactions of Protonated Guanidine and Guanidine Derivatives with Multiply Deprotonated RNA Probed by Electrospray Ionization and Collisionally Activated Dissociation [O] . Jovana Vušurović, Eva‐Maria Schneeberger, Dr. Kathrin Breuker 2017

机译：电喷雾电离和碰撞活化解离探测质子化的胍和胍衍生物与多重去质子化的RNA的相互作用。
7. Quantitative Structure-Activity Relationship Study of N-(3-Oxo-3,4-dihydro-2H-benzo 1,4thiazine-6-carbonyl)guanidines as Potent Na/H Exchange Inhibitors. [O] . Takeshi YAMAMOTO, Manabu HORI, Ikuo WATANABE, 2000

机译：N-（3-氧代-3,4-二氢-2H-苯并1,4噻嗪-6-羰基）胍作为有效的NA / H换脂抑制剂的定量结构 - 活性关系研究。
8. Review of Toxicity and Use and Handling Considerations for Guanidine, Guanidine Hydrochloride, and Urea [R] . Ertell, K. 2006

机译：回顾胍，盐酸胍和尿素的毒性，使用和处理注意事项

(2-Aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines as NHE-1 inhibitors.

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