- Synthesis of Hydrazones from Amino Acids and their Antimicrobial and Cytotoxic Activities
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Hydrazones 6a–6n were synthesized from different amino acids with various aldehydes under reflux in methanol/ethanol. The structures of synthesized compounds were ascertained by elemental analysis and spectroscopic techniques. A comparative study of the antimicrobial activity and cytotoxicity was carried out of the N-protected amino acids, their esters, hydrazides, and the respective hydrazones, providing good results in cytotoxicity studies.
- Abid, Obaid-Ur-Rahman,Khatoon, Ghamama,Arfan, Muhammad,Sajid, Imran,Langer, Peter,Rehman, Wajid,Rahim, Fazal,Yasir, Muhammad,Waqar, Muhammad,Haleem, Kashif Syed
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- Chalcogen bonding mediates the formation of supramolecular helices of azapeptides in crystals
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To explore whether chalcogen bonding was able to drive the formation of supramolecular helices, alanine-based azapeptides containing a β-turn structure, with a thiophene group, respectively, incorporated in theN- orC-terminus, were employed as helical building blocks. While the former derivative formed a supramolecularM-helixviaintermolecular S?S chalcogen bonding in crystals, the latter formedP-helixviaintermolecular S?O chalcogen bonding.
- Cao, Jinlian,Jiang, Yun-Bao,Li, Zhao,Shi, Di,Weng, Peimin,Yan, Xiaosheng
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supporting information
p. 6397 - 6401
(2021/08/03)
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- Synthesis and antitumor evaluation of some 1,3,4-oxadiazole-2(3H)-thione and 1,2,4-triazole-5(1H)-thione derivatives
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A series of 1,3,4-oxadiazole-2-thione and 1,2,4-triazole-5-thione derivatives have been successfully synthesized and studied for their antitumor activity. These compounds were prepared from carboxylic acids and chiral aminoacid esters. The prepared compounds were evaluated for their cytotoxicity against cancer in vitro using hydroxyurea (HU) as positive control. A fair number of compounds were found to have significant antitumor activity. To study the molecular basis of interaction and affinity of binding of the target molecules, all the compounds were docked into the ATPase domain of TP-II and tubulin using Schroedinger. Springer Science+Business Media, LLC 2010.
- Feng, Cheng Tao,Wang, Ling Dong,Yan, Yu Gang,Liu, Jian,Li, Shao Hua
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p. 315 - 320
(2012/09/07)
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- Synthesis and comparison of antioxidant properties of indole-based melatonin analogue indole amino acid derivatives
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Increased levels of reactive oxygen species attributed to oxidative stress have been found to be responsible for the development of some vital diseases such as cardiovascular, neurodegenerative and autoimmune diseases. Recently, it was observed that melatonin is a highly important antioxidant, and melatonin analogues are under investigation to find out improved antioxidant activity. In this study, 14 melatonin -based analogue indole amino acid and N-protected amino acid derivatives were synthesized and elucidated spectrometrically. To investigate the antioxidant activity of the synthesized compounds and to compare with melatonin, butylhydroxytoluene and vitamin E, lipid peroxidation inhibition and 2,2-diphenyl-1-picrylhydrazyl radical-scavenging activities were tested. The results indicated that the synthesized new indole amino acid derivatives have similar activities to melatonin in 2,2-diphenyl-1-picrylhydrazyl radical-scavenging activity assay but more potent activities in lipid peroxidation inhibition assay. A series of indole-based melatonin analogue indole-amino acid and N-protected amino acid derivatives were synthesized to investigate antioxidant activity by different assays. The results indicated that the synthesized compounds have similar activities to melatonin in DPPH radical scavenging activity assay but more potent activities in lipid peroxidation inhibition assay.
- Suzen, Sibel,Cihaner, Seyhan Sezen,Coban, Tulay
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experimental part
p. 76 - 83
(2012/05/04)
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