151392-08-4Relevant academic research and scientific papers
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 of some novel thiourea derivatives obtained from 5-[(4-aminophenoxy)methyl]-4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones and evaluation as antiviral/anti-HIV and anti-tuberculosis agents
Kuecuekguezel, Ilkay,Tatar, Esra,Kuecuekguezel, S. Gueniz,Rollas, Sevim,De Clercq, Erik
, p. 381 - 392 (2008/09/19)
As a continuation of our previous efforts on N-alkyl/aryl-N′-[4-(4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thione-5-yl)phenyl]thioureas 1-19 and N-alkyl/aryl-N′-[4-(3-aralkylthio-4-alkyl/aryl-4H-1,2,4-triazole-5-yl)phenyl]thioureas 20-22, a series of novel 5-[(4-aminophenoxy)methyl]-4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones 23-26 and several related thioureas, N-alkyl/aryl-N′-{4-[(4-alkyl/aryl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methoxy]phenyl}thioureas 27-42 were synthesized for evaluation of their antiviral potency. Structures of the synthesized compounds were confirmed by the use of 1H NMR, 13C NMR and HR-MS data. All compounds 1-42 were evaluated in vitro against HIV-1 (IIIB) and HIV-2 (ROD) strains in MT-4 cells, as well as other selected viruses such as HSV-1, HSV-2, Coxsackie virus B4, Sindbis virus and Varicella-zoster virus using HeLa, Vero, HEL and E6SM cell cultures, and anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv. Compounds 4 and 5 showed weak activity against HSV-1, HSV-2 and TK- HSV, whereas eight compounds showed marginal activity against Coxsackie virus B4. The most active derivative in this series was compound 38 which showed moderate protection against Coxsackie virus B4 with an MIC value of 16 μg/ml and a selectivity index of 5. This compound was also active against thymidine kinase positive Varicella-zoster virus (TK+ VZV, OKA strain) with an EC50 value of 9.9 μg/ml. Compound 38 was the most active compound with 79% inhibition against M. tuberculosis H37Rv.
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.
