Synthesis and Antioxidant Activity of N-Aminomethyl Derivatives of Ethosuximide and Pufemide Anticonvulsants

It was reported that the 1, 2, 4-triazole and the derivatives of this compound demonstrate numerous activities in a pharmacological point of view. 1, 2, 4-Triazole moieties were employed in an extensive range of drug candidates, which are therapeutically promising and include anti-inflammatories, anti-anxiety compounds, sedatives, CNS stimulants, antimicrobial agents, and antimycotic ones such as intraconazole, fluconazole and voriconazole. In the current investigation, several aminomethyl derivatives, which contain bis-1, 2, 4-triazole, were newly synthesized and their impacts on the levels of antioxidant vitamins (A, C and E) and malondialdehyde (MDA) were examined in serum, kidney and liver of rats. The investigation of the levels of the vitamins (A, C and E) and malondialdehyde (MDA) were performed by calculations in HPLC system. In the study, the observed antioxidant activity revealed that all the analyzed compounds, have promising antioxidant activities, which may be the result of the presence of benzylpiperazine and dipropylamine, and a methylpiperidine moiety as well as the allyl group. Therefore, it was concluded that ample scope exists for further studies.

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The Effect of N-4 Substituent on Antibacterial Activity of Novel Hydroxymethyl/Aminomethyl Derivatives of 1,2,4-Triazole-3-thione

Letters in Drug Design & Discovery ◽

10.2174/157018012800673056 ◽

2012 ◽

Vol 9 (6) ◽

pp. 633-637 ◽

Cited By ~ 1

Author(s):

Tomasz Plech ◽

Monika Wujec ◽

Urszula Kosikowska ◽

Anna Malm ◽

Magdalena Barylka ◽

...

Keyword(s):

Antibacterial Activity ◽

Aminomethyl Derivatives ◽

Derivatives Of

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Synthesis, Cytotoxicity and Antioxidant Activity of New Analogs of RC-121 Synthetic Derivatives of Somatostatin

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520618666180417164344 ◽

2019 ◽

Vol 18 (10) ◽

pp. 1417-1424 ◽

Cited By ~ 2

Author(s):

Emilia Naydenova ◽

Diana Wesselinova ◽

Svetlana Staykova ◽

Ivan Goshev ◽

Ljubomir Vezenkov

Keyword(s):

Antioxidant Activity ◽

Antioxidant Capacity ◽

Cell Line ◽

Cancer Cell ◽

Cancer Cell Line ◽

Colorectal Cancer Cell Line ◽

Cervical Cancer Cell Line ◽

Synthetic Derivatives ◽

Derivatives Of

Background: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. Objectives: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). Methods: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (Human Colorectal Cancer Cell Line), MDA-MB-23 (Human Breast Cancer Cell Line), Hep G-2 (Human Hepatocellular Carcinoma Cell Line) and HeLa (cervical cancer cell line). The antioxidant capacities were tested by ORAC (Oxygen Radical Antioxidant Capacity) and HORAC (Hydroxyl Radical Averting Capacity) methods. Results: All substances expressed significantly higher antioxidant capacity by comparison with galic acid and Trolox. All substances showed considerable antioxidant capacity as well. Compound 2T (D-Phe-c(Cys-Tyr-DTrp- Dap-Tle-Cys)-Thr-NH2)had the highest antioxidant effect. The compound 4T (D-Phe-c(Cys-Tyr-D-Trp- Orn-Tle-Cys)-Thr-NH2) displayed antiproliferative effect on HeLa cells with IC50 30 µM. The peptide analog 3T (D-Phe-c(Cys-Tyr-D-Trp-Lys-Tle-Cys)-Thr-NH2) exerted the most pronounced inhibition on the cell vitality up to 53%, 56% and 65% resp. against MDA-MB-23, Hep G-2, HeLa in the higher tested concentration. Conclusion: The somatostatin analogs showed moderate influence on the vitality of different tumor cells and could be used in changing their pathology.

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