Synthesis and antimicrobial evaluation of some novel 1,2,4-triazole and 1,3,4-thiadiazole derivatives [0.03%]
一些新型1,2,4-三氮唑和1,3,4-噻二唑衍生物的合成及抗菌活性评价
Lukasz Popiołek,Urszula Kosikowska,Liliana Mazur et al.
Lukasz Popiołek et al.
Abstract: This study presents the synthesis and spectral analysis of new derivatives of 1,2,4-triazole-3-thione and 1,3,4-thiadiazole. New compounds were prepared by cyclization reaction of acyl thiosemicarbazide derivati...
Synthesis and anticancer evaluation of novel 3,5-diaryl-thiazolo[4,5- d]pyrimidin-2-one derivatives [0.03%]
新型3,5-二芳基噻唑并[4,5-d]嘧啶酮衍生物的合成及其抗肿瘤活性评价
Lilianna Becan,Edwin Wagner
Lilianna Becan
The 2-oxo analogs of thiazolo[4,5-d]pyrimidine-2-thiones were prepared to study their cytotoxic activity. Five of the newly synthesized compounds were selected by the National Cancer Institute (Bethesda, MD, USA) for a primary in vitro anti...
Microbiologically active Mannich bases derived from 1,2,4-triazoles. The effect of C-5 substituent on antibacterial activity [0.03%]
由1,2,4-三唑衍生物合成的具有生物活性的曼尼希碱。C-5取代基对抗菌活性的影响
Tomasz Plech,Monika Wujec,Magdalena Majewska et al.
Tomasz Plech et al.
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...
Copper(II) complexes with derivatives of pyrazole as potential antioxidant enzyme mimics [0.03%]
作为抗氧化酶模拟物的吡唑衍生物铜(ii)配合物
Bogumiła Kupcewicz,Krzysztof Sobiesiak,Katarzyna Malinowska et al.
Bogumiła Kupcewicz et al.
A series of six mononuclear Cu(II) complexes with pyrazole-based ligands: 5-(2-hydroxybenzoyl)-3-methyl-1-(2-pyridinyl)-1H-pyrazol-4-phosphonic acid dimethyl ester (1a), 5-(2-hydroxyphenyl)-3-methyl-1-(2-pyridylo)-1H-pyrazole-4-carboxylic a...
Antiproliferative activity and synthesis of 8-prenylnaringenin derivatives by demethylation of 7-O- and 4'-O-substituted isoxanthohumols [0.03%]
异戊酰基香豆素衍生物的合成及其体外细胞毒活性研究
Mirosław Anioł,Anna Swiderska,Monika Stompor et al.
Mirosław Anioł et al.
Several analogues of 7-O- and 4'-O-substituted isoxanthohumol and 8-prenylnaringenin, the strongest known phytoestrogen and potential anticancerogenic agent, were synthesized. Acyl, alkyl, and allyl derivatives of isoxanthohumol underwent t...
Serotonin transporter activity of imidazolidine-2,4-dione and imidazo[2,1-f]purine-2,4-dione derivatives in aspect of their acid-base properties [0.03%]
基于其酸碱性质的亚氨基二硫酮和嘌呤并亚氨基二硫酮衍生物的五羟色胺转运体活性研究
Agnieszka Zagórska,Anna Czopek,Maciej Pawłowski et al.
Agnieszka Zagórska et al.
Affinities of arylpiperazinylalkyl derivatives of imidazo[2,1-f]purine-2,4-dione and imidazolidine-2,4-dione for serotonin transporter and their acid-base properties were evaluated. The dissociation constant (pK(a)) of compounds 1-22 were d...
Antimicrobial and antiprotozoal activities of secondary metabolites from the fungus Eurotium repens [0.03%]
欧托坚芽枝霉次生代谢产物的抗微生物和抗原虫活性研究
Jiangtao Gao,Mohamed M Radwan,Francisco León et al.
Jiangtao Gao et al.
In this study, we examined in vitro antibacterial, antifungal, antimalarial, and antileishmanial activities of secondary metabolites (1-8) isolated from the fungus Eurotium repens. All compounds showed mild to moderate antibacterial or anti...
Proapoptotic effects of novel pentabromobenzylisothioureas in human leukemia cell lines [0.03%]
新型五溴苯基异硫脲类化合物诱导人白血病细胞系凋亡的作用机制研究
Mirosława Koronkiewicz,Zdzisław Chilmonczyk,Zygmunt Kazimierczuk
Mirosława Koronkiewicz
A series of new pentabromobenzylisothioureas [ZKK-1-ZKK-5; (ZKKs)] carrying additional substituents on nitrogen atoms has been synthesized. The ZKKs were found to induce apoptosis in HL-60 (human promyleocytic leukemia) and K-562 (human chr...
Renata Perlikowska,Jakub Fichna,Jean Claude do-Rego et al.
Renata Perlikowska et al.
Endomorphins (EMs), two endogenous μ-opioid receptor selective ligands, are attractive lead compounds for opioid-based pain management studies. However, these peptides are quickly degraded by peptidases, in particular by dipeptidylpeptidas...
QSAR studies on a number of pyrrolidin-2-one antiarrhythmic arylpiperazinyls [0.03%]
几类吡咯烷酮抗心律失常芳环哌嗪的定量构效关系研究
Alicja Nowaczyk,Katarzyna Kulig
Alicja Nowaczyk
The activity of a number of 1-[3-(4-arylpiperazin-1-yl)propyl]pyrrolidin-2-one antiarrhythmic (AA) agents was described using the quantitative structure-activity relationship model by applying it to 33 compounds. The molecular descriptors o...