75129-75-8Relevant academic research and scientific papers
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
3,4,5-trisubstituted-1,2,4-triazole derivatives as antiproliferative agents: Synthesis, in vitro evaluation and molecular modelling
Yurtta?, Leyla,Evren, Asaf Evrim,Kubilay, Asl?han,Temel, Halide Edip,?ift?i, Gül?en Akal?n
, p. 1502 - 1515 (2020/10/29)
Background: Cancer is the name given to various diseases that are mainly uncontrolled, related to cell growth and can affect various organs. Among them, lung cancer is the one, which, in its earliest stages, is difficult to diagnose, and it is asymptomati
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 evaluation of anti-inflammatory and analgesic activity of 3-[(5-substituted-1,3,4-oxadiazol-2-yl-thio)acetyl]-2H-chromen-2-ones
Ingale, Nista,Maddi, Veeresh,Palkar, Mahesh,Ronad, Pradeepkumar,Mamledesai, Shivalingrao,Vishwanathswamy,Satyanarayana, Darbhamulla
, p. 16 - 36 (2012/06/04)
A novel series of 3-[(5-substituted-1,3,4-oxadiazol- 2-yl-thio)acetyl]-2H- chromen-2-one (7a-i) were synthesized by the condensation between the appropriately substituted 5-substituted-1,3,4-oxadiazolyl-2-thione (4a-i) derived from various existing NSAIDs and 3-(2-bromoacetyl)- 2H-chromen-2-one (6) under reflux in the presence of sodium ethoxide. Structure of the synthesized compounds was established on the basis of physicochemical, elemental analysis, and spectral data. The title compounds were screened for in vivo acute anti-inflammatory and analgesic activities at a dose of 200 mg/kg bw. Among the series, four compounds 7c, 7e, 7f, and 7h were found to possess a significant anti-inflammatory and analgesic activity profile. In addition, these compounds were also found to possess a less degree of ulcerogenic potential as compared to standard NSAIDs. Springer Science+Business Media, LLC 2010.
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.
Anti-inflammatory activity of substituted 1,3,4-oxadiazoles
Nargund,Reddy,Hariprasad
, p. 246 - 248 (2007/10/02)
Various 5-[[(acetamidophen-4-yl)oxy]methyl]-2-(p-substituted phenylamino)- 1,3,4-oxadiazoles (4a-4d) were synthesized by cyclization of the corresponding N1-[[(acetamidophen-4-yl)oxy]acetyl]-N4-(p-substituted phenylamino)-3-thiosemicarbazides (3a-3d). All four of the thiosemicarbazides [250 mg/kg, orally (p.o.)] and the corresponding oxadiazoles (250 mg, p.o.) possessed anti-inflammatory activity. In the Carrageenan-induced edema test in rat paw, the activity ranged from 28 to 47% for 3a-3d and 44 to 63% for 4a-4d, with indomethacin (10 mg/kg, p.o.), used as the standard reference drug, showing 88.5% protection. The compounds (1 mM) were also tested for the inhibition of bovine serum albumin denaturation, and this activity ranged from 27 to 68%. No correlation was seen between the anti-inflammatory activity of 3a-4d and the inhibition of denaturation of bovine serum albumin. The low toxicity of these compounds was reflected by their high approximate 50% lethal dose (LD50) values, ranging from 2000 to 2500 mg/kg.
