Synthesis of New 3,5-disubstituted-1,2,4-Triazoles and Evaluation of Antibacterial, Antiurease and Antioxidant Activities

Sahin, Huseyin/0000-0002-6018-1494WOS: 000390364000016Acylhydrazone 2 was synthesized by the condensation of iminoester hydrochloride 1 with acyl hydrazine. The treatment of acylhydrazone with hydrazine hydrate afforded 4-amino-3,5-dialkyl-1,2,4-triazole 3. The treatment of compound 3 with various aromatic aldehydes resulted in the formation of 4-arylidenamino-3, 5-dialkyl-1,2,4-triazoles 4a-c. Sodium borohydride reduction of 4-arylidenamino derivatives afforded 4-alkylamino-3,5-dialkyl- 1,2,4-triazoles 5a-c. The obtained products were identified by FTIR, H-1-NMR, C-13-NMR, Mass spectroscopic and elemental analysis. A series of compounds were evaluated for their, antibacterial, antiurease, antioxidant activities. The results showed that the synthesized new compounds had effective antibacterial, antioxidant, antiurease activities

Oxidative, Genotoxic and Cytotoxic Damage Potential of Novel Borenium and Borinium Compounds

In this study, the biological properties of novel borenium and borinium compounds in terms of their oxidative, genotoxic, and cytotoxic effects were assessed on cultured human peripheral blood cells, as well as several types of cancer cells. Our results revealed that the borinium compounds yielded the best results in terms of supporting total antioxidant capacity (TAC). In fact, borenium 1, borenium 2, borenium 3, borinium 4, and borinium 5 compounds elevated TAC levels of cultured human blood cells at rates of 42.8%, 101.5%, 69.8%, 33.3%, and 49.2%, respectively. There were no statistically significant differences (p > 0.05) between the negative control and the groups treated with all borinium and borenium concentrations from the micronucleus (MN) and chromosome aberration (CA) assays, demonstrating the non-genotoxic effects. Moreover, borenium 1 (60.7% and 50.7%), borenium 2 (70.4% and 57.2%), borenium 3 (53.1% and 45.2%), borinium 4 (55.1% and 48.1%), and borinium 5 (51.0% and 36.1%) minimized the mitomycin C(MMC)-induced genotoxic damages at different rates as determined using CA and MN assays, respectively. Again, it was found that the borinium compounds exhibited higher cytotoxic activity on cancer cells when compared to borenium compounds. Consequently, in light of our in vitro findings, it was suggested that the novel borinium and borenium compounds could be used safely in pharmacology, cosmetics, and various medical fields due to their antioxidant and non-genotoxic features, as well as their cytotoxicity potential on cancer cells

In vitro cytotoxic and genotoxic effects of newly synthesised boron ionic liquids

In this study, new molecules containing boron were added to the family of ionic organic compounds, in particular, ionic liquids with a cationic center. This study aimed to determine the cytotoxic and genetic effects of a total of four newly synthesised borenium and borinium compounds on human peripheral lymphocytes in vitro. Human peripheral lymphocytes were obtained from heparinised blood samples collected from healthy females aged between 29 and 32 years, with no history of exposure to toxic agents. The cytotoxicity was assayed via the MTT (3-(4.5-dimethylthiazole- 2-yl)-2.5-diphenyltetrazolium-bromide) and LDH (lactate dehydrogenase) tests; the genotoxicity and cytotoxicity, via the micronucleus (MN) and sister chromatid exchange (SCE) tests. The results showed that the borenium compounds did not exhibit cytotoxic activity in the MTT and LDH tests even in high concentrations, the borinium compound did not exhibit cytotoxic effects in lower concentrations in vitro. The borenium compounds did not show genotoxic effects in SCE and MN tests. However, at a high concentration, borinium increased the micronucleus rate in comparison to the negative control group. The obtained results suggest that these newly synthesised cationic boron compounds can be used reliably in health, cosmetics or other industries, taking into consideration their types and concentrations

Synthesis, antibacterial, antielastase, antiurease and antioxidant activities of new methoxy substitued bis-1,2,4-triazole derivatives

yanardag, refiye/0000-0003-4185-4363WOS: 000313663400009PubMed: 22085138The methoxy substitued two novel bis triazole-schiff bases (6 a-b) were synthesized with 4-amino-3,5-diethyl-4H-1,2,4-triazole and various bis-aldehydes. Their amine derivatives prepared by reduced with NaBH4 (5 a-b). The obtained products 6 a-b and 7 a-b were identified by FT-IR, H-1-NMR, C-13-NMR. The bis triazole-schiff bases and amine derivatives were tested for antimicrobial activity using the agar diffusion technique against 11 bacteria. The synthesized compounds (6 a-b and 7 a-b) were screened for their antielastase, antiurease and antioxidant activities. The resuts showed that the synthesized compounds (6 a-b and 7 a-b) had effective antielastase and antiurease activities

Antibacterial, Antiurease, and Antioxidant Activities of Some Arylidene Barbiturates

Some series of arylidene barbiturates and thiobarbiturates were evaluated for their antibacterial, antioxidant, and urease inhibition activities. The arylidene barbiturates and thiobarbiturates were tested for antimicrobial activity using the agar well diffusion technique against 13 bacteria. The synthesized compounds (1a–g) were screened for antiurease and antioxidant activities. The results showed that the synthesized compounds (1a–g) had effective antiurease, antioxidant, and antibacterial activities