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1.
《Arabian Journal of Chemistry》2019,12(7):1641-1651
A series of (E)-2-[5-chloro-1-(1H-benzo[d]imidazol-2-yl)ethylidene] N-(substituted) hydrazine carbothioamide (7a–7t) and (E)-2-[1-(1H-benzo[d]imidazol-2-yl)ethylidene] N-(substituted) hydrazine carbothioamide (8a–8t) were prepared via the synthesis of 1-(substituted-1H-benzimidazol-2-yl) ethanol (3a–3b) which was synthesized by the condensation of substituted o-phenylenediamine (2a–2b) with dl-lactic acid (1) followed by oxidation with sodium hypochlorite in mild acidic condition to form the corresponding ketones 4a–4b. Final compounds were formed by condensation of 4a–4b with different thiosemicarbazides 6a–6t. A total of 40 compounds were synthesized and characterized by FT-IR, 1H NMR, 13C NMR, Mass spectral technique and elemental analysis, in addition they were evaluated for anti-malarial properties. Among the compounds tested 7o, 7p, 7q, 7r, 7s, 8e and 8h exhibited good antimalarial activity in vitro. 相似文献
2.
Zaibo Yang Pei Li Yinju He Jun Luo Jing Zhou Yinghong Wu Liantao Chen 《Journal of heterocyclic chemistry》2020,57(1):81-88
In this study, a series of novel pyrethrin derivatives containing an 1,3,4-oxadiazole thioether moiety were designed and synthesized. Bioassay results revealed that some of the target compounds possessed excellent insecticidal activities against Plutella xylostella (P. xylostella), Vegetable aphids (V. aphids), and Empoasca vitis (E. vitis), respectively. In particular, compound 4l revealed the best insecticidal activities against P. xylostella and V. aphids, with the 50% lethal concentration (LC50) values of 1.78 and 1.61 mg/L, respectively, meanwhile, compound 4k revealed the best insecticidal activity against E. vitis, with the LC50 value of 1.06 mg/L, which were superior to those of the commercial insecticidal agents of chlorpyrifos, beta cypermethrin, spinosad, and azadirachtin. These results indicated that novel pyrethrin derivatives containing an 1,3,4-oxadiazole thioether moiety could effectively inhibit P. xylostella, V. aphids, and E. vitis. 相似文献
3.
Bei Zhang Yan Fang Zhao Xin Zhai Wei Jie Fan Jun Ling Ren Chun Fu Wu Ping Gong 《中国化学快报》2012,23(8):915-918
A new series of diaryl urea derivatives bearing N-acylhydrazone moiety were designed and synthesized.All the target compounds were evaluated for their antiproliferative activities against human leukemia cell line(HL-60),human lung adenocarcinoma epithelial cell line(A549) and human breast cancer cell line(MDA-MB-231) in vitro by standard MTT assay.The pharmacological results indicated that some compounds exhibited promising antitumor activities.Compound 1j showed the most potent antiproliferative activity against the tested three cell lines with IC values of 0.13 mmol/L,0.7 mmol/L and 0.5 mmol/L,respectively. 相似文献
4.
《Journal of Coordination Chemistry》2012,65(7):1229-1239
An oxovanadium complex [VO(satsc)(phen)] (1) (satsc?=?salicylaldehyde thiosemicarbazone, phen?=?phenanthroline) and its derivative [VO(3,5-dibrsatsc)(phen)] (2) (3,5-dibrsatsc?=?3,5-dibromosalicylaldehyde thiosemicarbazone) have been synthesized and characterized by elemental analysis, infrared, electrospray-mass spectra, 1H NMR, and magnetic susceptibility measurements. The DNA-binding behaviors of these complexes with calf-thymus DNA (CT-DNA) were investigated by UV-Vis absorption titration, fluorescence spectra, viscosity measurements, thermal denaturation, and circular dichroism. Both 1 and 2 bind to CT-DNA by intercalation and 1 exhibits much stronger binding affinity to CT-DNA than 2. 相似文献
5.
Sonia Zulfiqar Zahoor Ahmad Muhammad Ilyas Sarwar 《Colloid and polymer science》2007,285(15):1749-1754
Soluble aromatic polyamide chains were prepared by reacting 4–4′-oxydianiline with isophthaloyl chloride in dimethylacetamide.
To quench the HCl produced during the polymerization reaction, a stoichiometric amount of triethylamine was added. The precipitates
formed were separated leaving behind clear polyamide resin. Thin and transparent film was obtained by evaporating the solvent
and was subjected for Fourier transform infrared (IR), nuclear magnetic resonance (NMR), gel permeation chromatography, thermogravimetric
analysis, differential scanning calorimetry, water absorption, and mechanical analyses. The transparent film was found to
be soluble in dimethylacetamide, dimethyl sulfoxide, and dimethylformamide. IR and NMR spectroscopic analyses confirmed the
structure of the polyamide while the gel permeation chromatography revealed the formation of a high-molecular-weight polymer.
Thermogravimetry, differential scanning calorimetry, water absorption, and mechanical testing were also performed to further
verify its physical properties. A soluble aromatic polyamide was successfully synthesized by solution polymerization and characterized.
The polyamide has film-forming property, and the film is transparent, mechanically strong, and thermally stable. 相似文献
6.
7.
A series of substituted-nicotinyl thiourea derivatives containing pyrimidine ring were synthesized in good to excellent yield using PEG-400 as solid?Cliquid phase transfer catalyst under ultrasonic irradiation. The structures of all newly synthesized compounds were elucidated and confirmed by IR, 1H NMR and elemental analysis. The preliminary biological tests show that some of the target compounds present good inhibitory activities against the root and stalk of dicotyledon plants and are safe for monocotyledon plants. 相似文献
8.
《Arabian Journal of Chemistry》2023,16(2):104479
In the search for more efficient and versatile anti-phytopathogen agents, a series of new 1,3,4-oxadiazole thioether/sulfone analogues bearing a flexible N-containing heterocyclic pattern were elaborately prepared, and their bioactivities against plant pathogenic microorganisms were systematically evaluated. Bioassay screening results demonstrated that compounds 32 and 33 significantly inhibited the growth of Xanthomonas oryzae pv. oryzae (Xoo) in vitro (32, EC50 = 5.17 mg L?1; 33, EC50 = 1.19 mg L?1), which were significantly surpass commercial bismerthiazol (BT) and thiodiazole copper (TC). Meanwhile, pot experiments confirmed the prospective applications of compound 33 in managing rice bacterial leaf blight and its good safety toward rice plants. Further studies showed that compound 33 interfered with the formation of bacterial biofilms and inhibited bacterial virulence factors. Furthermore, an in vitro antifungal bioassay showed that compound 32 possessed remarkable growth inhibitory activity against Sclerotinia sclerotiorum (S.s., EC50 = 22.16 mg L?1) and Verticillium dahlia (V.d. EC50 = 32.78 mg L?1). These results all confirmed that the designed 1,3,4-oxadiazole compounds displayed potential for managing plant microbial diseases through targeting dihydrolipoamide S-succinyltransferase (DLST). 相似文献
9.
In this study, a total of 31 novel isoxazole derivatives containing bisamide moiety were synthesized and evaluated for their insecticidal activity against Plutella xylostella (P. xylostella). Bioassays indicated that some of the target compounds exhibited good insecticidal activity against P. xylostella. In particular, compound E26 revealed excellent insecticidal activity against P. xylostella, with a 50% lethal concentration (LC50) value of 4.6 μg/mL, which was even better than those of chlorpyrifos (7.7 μg/mL), beta‐cypermethrin (12.8 μg/mL), and azadirachtin (10.2 μg/mL). These results indicated that isoxazole derivatives containing bisamide moiety could be developed as novel and promising insecticides. To the best of our knowledge, it is the first report on the insecticidal activity of this series of novel isoxazole derivatives containing bisamide moiety. 相似文献
10.
A novel series of diaryl urea derivatives bearing sulfonamide moiety have been designed and synthesized.Their in vitro antitumor effect against human cancer cell lines MX-1,A375,HepG2,Ketr3 and HT-29 was screened and evaluated by the standard MTT assay with sorafenib as the positive control.Some of the compounds showed significant inhibitory activity against multiple cell lines compared to sorafenib.In particular,2,6-dimethyl-4-{6-[3-(4-chloro-3-(trifluoromethyl)phenyl)urea]naphthalen-2-yl}sulfonyl morpholine(10d)was found to be the most potent against A375,HepG2 and Ketr3 with IC50values of 0.65–0.97mol/L,which were 5–20-fold more potent than sorafenib.Compound 10d emerged as a valuable lead for further optimization. 相似文献
11.
12.
《Journal of Coordination Chemistry》2012,65(15):1369-1375
The crystal and molecular structures of the organomercury(II) complexes [Hg(C6H5)(chtsc)], 1, and [Hg(C6H5C5H4N)(btsc)], 2, obtained from the reaction of phenylmercury(II) acetate with cyclohexanone thiosemicarbazone (Hchtsc) and that of [2-(pyridin-2′-yl)]phenyl]mercury(II) acetate with benzaldehyde thiosemicarbazone (Hbtsc), respectively, are described. Both 1 and 2 are monoclinic, space group C2/c. Complex 1 has a distorted T-shaped geometry {C-Hg-S, 161.91(10)°} and 2 can be considered to have a distorted seesaw geometry {C-Hg-S, 171.2(10)°}. In both complexes the ligands act as bidentate chelating anions bonding through azomethine N1 and thiolato S atoms. 相似文献
13.
A facile, one-pot synthesis of new phenanthridine derivatives by a three-component reaction between phenantridine, dialkyl acetylenedicarboxylates(DAADs), and aromatic aldehydes is described. The reaction is characterized by mild conditions, high selectivity, and tolerance to various functional groups. 相似文献
14.
Josane A. LessaAuthor VitaeDébora C. ReisAuthor Vitae Isolda C. MendesAuthor VitaeNivaldo L. SpezialiAuthor Vitae Lucas F. RochaAuthor VitaeValéria R.A. PereiraAuthor Vitae Cristiane M.L. MeloAuthor VitaeHeloisa BeraldoAuthor Vitae 《Polyhedron》2011,30(2):372-380
The antimony(III) complexes [Sb(2Fo4Ph)Cl2] (1), [Sb(2Ac4Ph)Cl2] (2) and [Sb(2Bz4Ph)Cl2] (3) were prepared with N(4)-phenyl-2-formyl- (H2Fo4Ph), 2-acetyl- (H2Ac4Ph) and 2-benzoylpyridine (H2Bz4Ph) thiosemicarbazones. The antimony(III) complexes presented antitrypanosomal activity against the epimastigote and trypomastigote forms of Trypanosoma cruzi. Complexes (1) and (2) exhibited higher activity than the reference drugs benznidazole and nifurtimox. 相似文献
15.
T. N. Kudryavtseva P. I. Sysoev S. V. Popkov G. V. Nazarov L. G. Klimova 《Russian Chemical Bulletin》2015,64(6):1341-1344
Novel acridone derivatives bearing 1,3,4-moiety were synthesized by intramolecular cyclization of N´-[2-(9-oxoacridin-10(9H)-yl)acetyl]arylhydrazides. Study of antimicrobial activity of the synthesized compounds reveals that some of them are more active than the comparator drug rivanol. 相似文献
16.
《Tetrahedron》2019,75(39):130550
Various aromatic nitriles could be obtained in good yields by the treatment of aryl bromides with n-butyllithium and then pivalonitrile, followed by the treatment with molecular iodine at 70 °C, without metal cyanides under transition-metal-free conditions. The present reaction proceeds through the radical β-elimination of imino-nitrogen-centered radicals formed from the reactions of imines and N-iodoimines under warming conditions. © 2019 Elsevier Science. All rights reserved. 相似文献
17.
AbstractA series of novel pyrethrin derivatives containing hydrazone and 1,3,4-oxadiazole thioether moieties were designed, synthesized, and evaluated for their insecticidal activity. Bioassays indicated that some of the target compounds exhibited good insecticidal activities against Plutella xylostella (P. xylostella), Vegetable aphids (V. aphids), and Empoasca vitis (E. vitis). In particular, compound (E)-2-((5-(2,2-dimethyl-3-(2-methylprop-1-en-1-yl)cyclopropyl)-1,3,4-oxadiazol-2-yl)thio)-N'-(4-(trifluoromethyl)benzylidene)acetohydrazide (6s) revealed excellent insecticidal activities against P. xylostella, V. aphids, and E. vitis with the 50% lethal concentration (LC50) values of 5.23, 7.07, and 1.61?mg/L, respectively, which were similar to or even better than those of chlorpyrifos, beta cypermethrin, spinosad, and azadirachtin. These results indicated that novel pyrethrin derivatives containing hydrazone and 1,3,4-oxadiazole thioether moieties could be developed as novel and promising insecticides. 相似文献
18.
Four aroylhydrazine-amides receptors AR1-4 with a hydrazine spacer have been designed, synthesised and characterised as novel colorimetric chemosensors by typical spectroscopic techniques. The receptors AR1–3 exhibited certainly selectivity and sensitivity towards F? and AcO? , forming 1:1 stoichiometry complex by hydrogen-bond interaction. Furthermore, AR4 has especially shown obvious colour change in the presence of these two important biologically anions. 相似文献
19.
A new series of N-arylquinoline derivatives 5a-x bearing 2-morpholinoquinoline moiety has been synthesized by one pot base catalyzed cyclocondensation reaction of 2-morpholinoquinoline-3-carbaldehydes 2a-c,malononitrile 3 andβ-enaminones 4a-h. All the synthesized compounds were screened for their in vitro antimicrobial activity against six bacterial pathogens,namely Streptococcus pneumoniae,Clostridium tetani,Bacillus subtilis,Salmonella typhi,Vibrio cholerae,Escherichia coli and against two fungal pathogens,Aspergillus fumigatus and Candida albicans using broth microdilution MIC method.Of the compounds studied,majority of the compounds were found to active against C.tetani,B.subtilis and C.albicans as compared to first-line standard drugs. 相似文献
20.
Zhenjun Ye 《Tetrahedron letters》2010,51(38):4991-4994
Polyfunctionalized 4H-pyran derivatives bearing fluorochloro pyridyl moiety were readily prepared in high yields via one-pot multicomponent reaction catalyzed by piperidine. This present protocol provides an efficient synthetic route to the target compounds with the characteristics of short reaction time, high yield, and easy separation of the products. 相似文献