Novel Antidiabetic and Hypolipidemic Agents. 3. Benzofuran-Containing Thiazolidinediones
| العنوان: | Novel Antidiabetic and Hypolipidemic Agents. 3. Benzofuran-Containing Thiazolidinediones |
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| المؤلفون: | Bajji Ac, K. A. Reddy, Reddy Kv, Rao Nv, Ranjan Chakrabarti, Rao In, Bhushan, Krishna Th, Ramanujam Rajagopalan, Reddy Pr, T. Dileepkumar, B. B. Lohray, Hemant K. Jajoo |
| المصدر: | Journal of Medicinal Chemistry. 42:1927-1940 |
| بيانات النشر: | American Chemical Society (ACS), 1999. |
| سنة النشر: | 1999 |
| مصطلحات موضوعية: | Blood Glucose, Male, Pyrrolidines, medicine.drug_class, Stereochemistry, Receptors, Cytoplasmic and Nuclear, Chemical synthesis, Pyrrolidine, Mice, Structure-Activity Relationship, chemistry.chemical_compound, Phenylene, Drug Discovery, medicine, Animals, Hypoglycemic Agents, Moiety, Rats, Wistar, Thiazolidinedione, Benzofuran, Triglycerides, Hypolipidemic Agents, Rats, Mice, Inbred C57BL, Thiazoles, chemistry, Molecular Medicine, Female, Linker, Transcription Factors |
| الوصف: | Several thiazolidinedione derivatives having 5-hydroxy-2,3-dihydro-2, 2,4,6,7-pentamethylbenzofuran moieties and their 5-benzyloxy derivatives and 5-hydroxy-2,4,6,7-tetramethylbenzofuran moieties were synthesized and evaluated in db/db mice. Insertion of an N-Me group into the linker between thiazolidinedione and substituted benzofuran pharmacophores showed considerable improvement in their euglycemic activity. Further improvement has been observed when a pyrrolidine moiety is introduced in the structure to give 5-[4-[N-[3(R/S)-5-benzyloxy-2,3-dihydro-2,2,4,6, 7-pentamethylbenzofuran-3-ylmethyl]-(2S)-pyrrolidin-2- ylmethoxy]pheny lene]thiazolidine-2,4-dione (21a). At a 100 mg/kg/day dose of the maleate salt, compound 21a reduced the plasma glucose and triglyceride to the level of lean littermate, i.e. 8 +/- 1 mM, and is the most potent and efficacious compound reported in this series. |
| تدمد: | 1520-4804 0022-2623 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f90de7358e00e0949ea8be3a9155785 https://doi.org/10.1021/jm980549x |
| رقم الأكسشن: | edsair.doi.dedup.....5f90de7358e00e0949ea8be3a9155785 |
| قاعدة البيانات: | OpenAIRE |
Find this issue from the American Chemical Society | تدمد: | 15204804 00222623 |
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