دورية أكاديمية
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
| العنوان: | Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan. |
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| المؤلفون: | Choung W; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea., Jung HJ; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea., Nam EH; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea., Yang D; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea., Yoo B; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea., Choi H; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea., Lee BR; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea., Park M; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea., Jang SM; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea., Lim JS; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea., Kim KH; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Republic of Korea., Chin J; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Republic of Korea., Jung K; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Republic of Korea., Lee G; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Republic of Korea., Kim SH; Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea. Electronic address: rose1998@boryung.co.kr. |
| المصدر: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Oct 15; Vol. 28 (19), pp. 3155-3160. Date of Electronic Publication: 2018 Aug 28. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| مواضيع طبية MeSH: | Angiotensin II Type 1 Receptor Blockers/*pharmacology , Biphenyl Compounds/*pharmacology , PPAR gamma/*agonists , Pyrimidines/*pharmacology , Tetrazoles/*pharmacology, Angiotensin II Type 1 Receptor Blockers/chemistry ; Angiotensin II Type 1 Receptor Blockers/pharmacokinetics ; Animals ; Antihypertensive Agents/chemistry ; Antihypertensive Agents/pharmacokinetics ; Antihypertensive Agents/pharmacology ; Area Under Curve ; Biphenyl Compounds/chemistry ; Biphenyl Compounds/pharmacokinetics ; Disease Models, Animal ; Drug Discovery ; Drug Partial Agonism ; Half-Life ; Hypoglycemic Agents/chemistry ; Hypoglycemic Agents/pharmacokinetics ; Hypoglycemic Agents/pharmacology ; Proof of Concept Study ; Pyrimidines/chemistry ; Pyrimidines/pharmacokinetics ; Structure-Activity Relationship ; Tetrazoles/chemistry ; Tetrazoles/pharmacokinetics |
| مستخلص: | Inspired by the well-known PPARγ partial agonism of angiotensin II type 1 receptor (AT1R) antagonists exemplified by an antihypertensive drug, Telmisartan, efforts to identify compounds with the dual activities have been pursued in order to control the two major metabolic disorders, hypertension and hyperglycemia simultaneously. Lead compound 18 derived from the AT1R antagonist, Fimasartan, has successfully presented the possibility to control the medical conditions by a single molecule. (Copyright © 2018. Published by Elsevier Ltd.) |
| فهرسة مساهمة: | Keywords: Angiotensin II type 1 receptor antagonist; Antidiabetics; Antihypertensives; Drug discovery; Dual modulator; Fimasartan; PPARγ |
| المشرفين على المادة: | 0 (Angiotensin II Type 1 Receptor Blockers) 0 (Antihypertensive Agents) 0 (Biphenyl Compounds) 0 (Hypoglycemic Agents) 0 (PPAR gamma) 0 (Pyrimidines) 0 (Tetrazoles) P58222188P (fimasartan) |
| تواريخ الأحداث: | Date Created: 20180905 Date Completed: 20190522 Latest Revision: 20190522 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1016/j.bmcl.2018.08.036 |
| PMID: | 30177375 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3405 |
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| DOI: | 10.1016/j.bmcl.2018.08.036 |