Multi-pharmacophore Approach to Bio-therapeutics: Piperazine Bridged Pseudo-peptidic Urea/Thiourea Derivatives as Anti-oxidant Agents
| Autor: | Rangappa Shobith, Ningegowda Mallesha, Kuppalli R Kiran, Toreshettahally R. Swaroop, Maralinganadoddi P. Sadashiva, Seegehalli M Anil, Narasimhamurthy Rajeev |
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| Rok vydání: | 2019 |
| Předmět: |
010405 organic chemistry
Chemistry DPPH Bioengineering Phenylalanine 01 natural sciences Biochemistry Combinatorial chemistry 0104 chemical sciences Analytical Chemistry Piperazine chemistry.chemical_compound Thiourea Docking (molecular) Drug Discovery Urea Side chain Molecular Medicine Pharmacophore |
| Zdroj: | International Journal of Peptide Research and Therapeutics. 26:151-158 |
| ISSN: | 1573-3904 1573-3149 |
| DOI: | 10.1007/s10989-019-09824-4 |
| Popis: | In an attempt to develop synergetic, potential and selective anti-oxidant agents, a series of novel piperazine bridged pseudo-peptidic urea/thiourea derivatives (5a-x) are designed by molecular docking study, synthesized and evaluated for their in-vitro anti-oxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and dimethyl-4-phenylenediamine (DMPD) methods. The results revealed that compounds 5q, 5s, 5w and 5x are good anti-oxidant agents. Amongst, compounds with aromatic side chain, thioureal fragment with electron donating group-substitution, particularly, 5s and 5w are the most active members exhibiting remarkable anti-oxidant property. The docking results are complementary to the experimental results. The correlation study revealed that compounds derived from phenylalanine and tryptophan containing electron donating group are excellent antioxidants. |
| Databáze: | OpenAIRE |
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