75129-75-8Relevant articles and documents
Synthesis of 1,3,4-oxadiazole derivatives with anticonvulsant activity and their binding to the GABAA receptor
Lei, Kang,Li, Guangyong,Li, Jun,Liu, Hui,Liu, Renmin,Quan, Zheshan,Wang, Shiben,Wang, Xuekun
, (2020/08/19)
In this study, a series of 1,3,4-oxadiazole derivatives (5a-s, 10a-s, and 16a-d) were designed and synthesized using maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) models, to test the anticonvulsant activity of the target compounds
Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells
Kulaba?, Necla,Tatar, Esra,Bing?l ?zakp?nar, ?zlem,?zsavc?, Derya,Pannecouque, Christophe,De Clercq, Erik,Kü?ükgüzel, ?lkay
, p. 58 - 70 (2016/08/18)
In this study, a series of thiosemicarbazide derivatives 12–14, 1,2,4-triazol-3-thione derivatives 15–17 and compounds bearing 2-(4H-1,2,4-triazole-3-ylthio)acetamide structure 18–32 have been synthesized starting from phenolic compounds such as 2-naphthol, paracetamol and thymol. Structures and purity of the target compounds were confirmed by the use of their chromatographic and spectral data besides microanalysis. All of the synthesized new compounds 12–32 were evaluated for their anti-HIV activity. Among these compounds, three representatives 18, 19 and 25 were selected and evaluated by the National Cancer Institute (NCI) against the full panel of 60 human cancer cell lines derived from nine different cancer types. Antiproliferative effects of the selected compounds were demonstrated in human tumor cell lines K-562, A549 and PC-3. These compounds inhibited cell growth assessed by MTT assay. Compound 18, 19 and 25 exhibited anti-cancer activity with IC50values of 5.96?μM (PC-3?cells), 7.90?μM (A549/ATCC cells) and 7.71?μM (K-562?cells), respectively. After the cell viability assay, caspase activation and Bcl-2 activity of the selected compounds were measured and the loss of mitochondrial membrane potential (MMP) was detected. Compounds 18, 19 and 25 showed a significant increase in caspase-3 activity in a dose-dependent manner. This was not observed for caspase-8 activity with compound 18 and 25, while compound 19 was significantly elevated only at the dose of 50?μM. In addition, all three compounds significantly decreased the mitochondrial membrane potential and expression of Bcl-2.
Synthesis and antibacterial activity of a series 1-aryl-2-mercapto-5--1,3,4-triazoles, thiadiazoles and 2--3,4,5-trisubstituted pyrazoles
Nagrund, L. V. G.,Reddy, G. R. N.,Hariprasad, V.
, p. 499 - 502 (2007/10/03)
A series of new 1-aryl-2-mercapto-5--1,3,4-triazoles, 2-arylamino-5--1,3,4-thiadiazoles, p-acetamido(phenoxy)acetyl thio-semicarbazides and 2--3-amino-4-carboxamido-5-methylthiopyrazole have been prepared and evaluated for comparative antibacterial activity.The antibacterial activity of the target compounds and their relevant reference agent have been determined in vitro using serial 2-fold dilution technique on an assortment of Gram negative and Gram positive organisms.It has been observed that the in vitro antibacterial activity of cyclized 1,3,4-triazoles and 1,3,4-thiadiazoles are significantly greater than thiosemicarbazides.The derivatives 4b, 5b have better in vitro antibacterial activity.
