38240-75-4Relevant academic research and scientific papers
Synthesis of new 1,2,4-Triazole-5-thiones and their thioglycoside derivatives as potential antibacterial agents
Dilmaghani, Karim Akbari,Nasuhi Pur, Fazel,Jazani, Nima Hoseini,Alavi, Asma,Niknam, Zahra,Mirfakhraee, Farrin
, p. 81 - 87 (2014/01/06)
Abstract The glycosylation of 1,2,4-triazole-5-thiones has been performed with peracetylated β-pyranosyl bromide in the presence of potassium carbonate. The synthesized compounds were tested for their antimicrobial activity against bacterial (Gram-negative and Gram-positive) and yeasts strains in vitro. The synthetic compounds showed different inhibition zones against tested bacterial and yeasts strains. Among them, compounds which possessed 2-furyl and p-bromophenyl moieties showed the best results against Acinetobacter calcoaceticus ATCC 23055.
Antimicrobial and Physicochemical Characterizations of Thiosemicarbazide and S-Triazole Derivatives
Kusmierz, Edyta,Siwek, Agata,Kosikowska, Urszula,Malm, Anna,Plech, Tomasz,Wrobel, Andrzej,Wujec, Monika
, p. 1539 - 1545 (2015/10/29)
Two series of thiosemicarbazide derivatives and three series of s-triazole derivatives have been synthesized. All of these compounds were tested for their in vitro antibacterial activity against Gram-positive and Gram-negative bacterial strains. Among tested thiosemicarbazide derivatives, the best bioactivity was detected for two 1-formylthiosemicarbazides with 3-/4-tolyl substitution (1 l, 1 m) (MICs range between 31.25 and 250 μg/mL). All tested s-triazole derivatives exhibited lower antibacterial activity than their acyclic precursors.
Microbiologically active Mannich bases derived from 1,2,4-triazoles. the effect of C-5 substituent on antibacterial activity
Plech, Tomasz,Wujec, Monika,Majewska, Magdalena,Kosikowska, Urszula,Malm, Anna
, p. 2531 - 2537 (2013/07/26)
Our research proved that chemical character of the C-5 substituent significantly determines the antibacterial activity of the Mannich bases derived from 4,5-disubstituted 1,2,4-triazole-3-thiones. This activity was considerably increased by an introduction of a chlorine atom to the phenyl ring. The obtained compounds were particularly active against opportunistic bacteria (Bacillus subtilis and Bacillus cereus). The antibacterial activity of some Mannich bases was similar or higher than the activity of commonly used antibiotics such as ampicillin and cefuroxime.
Synthesis and tuberculostatic activity of some 2-piperazinmethylene derivatives 1,2,4-triazole-3-thiones
Foks, Henryk,Janowiec, Mieczyslaw,Zwolska, Zofia,Augustynowicz-Kopec, Ewa
, p. 537 - 543 (2007/10/03)
The Mannich reaction's products of 1,2,4-triazole-3-thiones, substituted in position 4 (with ethyl, allyl, phenyl, Ph-4-Br) or 5 (with phenyl, Ph-4-OH, Ph-3,4,5-(OMe)3, 2-phenyl) were obtained. Their amino-components were 1-phenylpiperazine, 1-
1,3,4-Thiadiazole derivatives. Synthesis, structure elucidation, and structure-antituberculosis activity relationship investigation
Oru?, El?in E.,Rollas, Sevim,Kandemirli, Fatma,Shvets, Nathaly,Dimoglo, Anatholy S.
, p. 6760 - 6767 (2007/10/03)
A series of 2,5-disubstituted-1,3,4-thiadiazoles were synthesized, the compounds structures were elucidated and screened for the antituberculosis activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system. Among the tested compounds, 2-phenylamino-5-(4-fluorophenyl) -1,3,4-thiadiazole 22 showed the highest inhibitory activity. The relationships between the structures of compounds and their antituberculosis activity were investigated by the Electronic-Topological Method (ETM) and feed forward neural networks (FFNNs) trained with the back-propagation algorithm. As a result of the approach, a system of pharmacophores and anti-pharmacophores has been found that effectively separates compounds of the examination set into groups of active and inactive compounds. The system can be applied to the screening and design of new active compounds possessing skeletons similar to those used in the present study.
An efficient solid-state method for the preparation of acyl thiosemicarbazides
Li,Luo,Wang,Wang
, p. 1793 - 1797 (2007/10/03)
Solid-state syntheses of acyl thiosemicarbazides are reported for the first time. Eleven acyl thiosemicarbazides have been synthesized at room temperature in excellent yields (84.5 ~ 91.0%). Among them, eight compounds 3a, 3d, 3e, 3g-k are new. The reacti
