Synthesis, molecular modeling and evaluation of α-glucosidase inhibition activity of 3,4-dihydroxy piperidines
| Autor: | Dilep Kumar Sigalapalli, Sujatha Surarapu, Jaya Shree Anireddy, Krishna S. Ethiraj, Srinivas Uppalanchi, Perumal Yogeeswari, Shubham Dwivedi, Siva Prasad Kasturi, Nagendra Babu Bathini |
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| Rok vydání: | 2018 |
| Předmět: |
Models
Molecular 0301 basic medicine Molecular model Stereochemistry Ring (chemistry) 01 natural sciences Structure-Activity Relationship 03 medical and health sciences Piperidines Drug Discovery Voglibose medicine Humans Glycoside Hydrolase Inhibitors Acarbose Biological evaluation Pharmacology Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Chemistry Miglitol α glucosidase Organic Chemistry alpha-Glucosidases General Medicine 0104 chemical sciences 030104 developmental biology Cis–trans isomerism medicine.drug |
| Zdroj: | European Journal of Medicinal Chemistry. 150:39-52 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2018.02.072 |
| Popis: | Biological evaluation of 3,4-dihydroxy piperidines as α-glucosidase inhibitors is being reported for the first time. Forty-five derivatives (amides, di-amides and sulfonamides) were made using cis and trans 3,4-dihydroxy piperidines to evaluate their α-glucosidase inhibition activity. Polar groups (-OH, -NH2) on phenyl ring having derivatives 5i, 5l, 7g, 7i & 12j showed excellent activity compared to standard references. Acarbose, Voglibose and Miglitol were used as standard references. Molecular docking simulations were done for compounds to identify important binding modes responsible for inhibition activity of α-glucosidase. |
| Databáze: | OpenAIRE |
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