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1.
The reaction of 3,4-dichlorophenyl-1,3,4-oxadiazole-2( 3H )-thione with piperidine derivatives via Mannich reaction was used to generate eleven novel compounds in moderate to good yields. Synthesized molecules were characterized according to their structure with 1H NMR, 13C NMR and FT-IR spectral foundations, which were compatible with literature informations. Antimicrobial activity and cytotoxicity studies were done by disc diffusion and NCI-60 sulphordamine B assay methods. The antimicrobial test results revealed that synthesized compounds have better activity against gram-positive species than gram-negative ones. A total analysis of the antibacterial, antifungal, and antiyeast activity revealed that newly synthesized compounds were really active against Bacillus cereus , Bacillus ehimensis, and Bacillus thuringiensis species . For cytotoxicity, among three different cancer cell lines (HCT116, MCF7, HUH7) compounds 5c, 5d, 5e, 5f, 5g, 5i, 5j and 5k were seemed especially effective on HUH7 cancer cell line via moderate to good activity. More significantly, against liver carcinoma cell line (HUH7) most of the compounds of the series ( 5c-5g and 5i-5j ) have better IC50 values (IC50= 18.78 µM) than 5-Florouracil (5-FU) and also compound 5d possessed 10.1 µM value, which represents good druggable cytotoxic activity. Further, the molecules were also screened for in silico chemoinformatic and toxicity data to gather the predicted bioavailibity and safety measurements. 相似文献
2.
Jumat Salimon Nadia Salih Emad Yousif Ayad Hameed Ayad Kreem 《Arabian Journal of Chemistry》2010,3(4):205-210
In the present study a new acridone derivatives were synthesized. The newly synthesized compounds were characterized by IR, NMR and C, H, N, S analyses. All newly synthesized compounds were screened for their antibacterial (Staphylococcus aureus, Streptococcus viridans and Escherichia coil) and antifungal (Gibberela, Cercospora arachidicola, Physolospora piricola and Fusarium oxysporum) studies. The results revealed that all synthesized compounds have a significant biological activity against the tested microorganisms. 相似文献
3.
《Arabian Journal of Chemistry》2014,7(4):418-424
In the present study o-phenylenediamine and naphtene-1-acetic acid/2-naphthoxyacetic acid were used as a starting material through a series of steps and 2-(naphthalen-1-ylmethyl/Naphthalen-2-yloxymethyl)-1H-benzimidazol-1-yl]acetohydrazide 5a, 5b were obtained. In the first series 1,3,4-oxadiazole derivatives have been synthesized from Schiff base of the corresponding hydrazide i.e. 2-[2-(naphthalen-1-ylmethyl)-1H-benzimidazol-1-yl]acetohydrazide 5a by using Chloramin-T. In the second series 1,3,4-oxadiazole has been synthesized from 2-{2-[(naphthalen-2-yloxy)methyl]-1Hbenzimidazol-1-yl}acetohydrazide 5b by using phosphorous oxychloride and aromatic acid. These compounds were evaluated by IR, NMR, Mass spectrometry, elemental analysis and finally in vitro anticancer evaluation was carried out by NCI 60 Cell screen at a single high dose (10–5 M) on various panel/cell lines. One compound 7c was found to be the most active on breast cancer cell line and compounds 4b and 7d were moderately active. 相似文献
4.
Lianqing Chen Jingui Qin Jia Gao Dongge Ma 《Journal of organometallic chemistry》2006,691(16):3519-3530
Four new iridium(III) complexes 1-4, with 1,3,4-oxadiazole derivative as cyclometalated ligand for the first time, have been synthesized and structurally characterized by NMR, EA, MS and X-ray diffraction analysis (except 1). The stronger ligand field strength of the dithiolate ancillary ligands results in higher oxidation potentials and lower HOMO energy levels of complexes than acetylacetone. The absorption spectra of these complexes display low-energy metal-to-ligand charge transfer transition ranging from 350 to 500 nm. Complexes with dithiolate ancillary ligand emit at maximum wavelengths of ca. 500 nm, blue shifting 17 and 11 nm with respect to their counterpart with acetylacetone ligand. The electrophosphorescent devices with 2-4 as phosphorescent dopant in emitting layer have been fabricated. All devices have a low turn-on voltage in the range of 4.5 and 4.9 V. A high-efficiency green emission with maximum luminous efficiency of 5.28 cd/A at current density of 1.37 mA/cm2 and a maximum brightness of 2592 cd/m2 at 15.2 V has been achieved in device using 2 as emitter. 相似文献
5.
Abbas Nikoo Karim Akbari Dilmaghani 《Phosphorus, sulfur, and silicon and the related elements》2013,188(2):268-275
Abstract A series of 1,2,4,5-tetrakis(1,2,4-triazolyl)benzenes and 1,2,4,5-tetrakis(1,3,4-oxadiazolyl)benzenes was synthesized by nucleophilic addition of sodium salts of 4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thiones and 1,3,4-oxadiazole-2(3H)-thiones to 1,2,4,5-tetrakis(bromomethyl)benzene. The structure of the newly synthesized compounds was confirmed by elemental analysis, IR and 1H and 13C NMR spectra. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental resource: 1H and 13C NMR spectra of products (Figures S1-S24). 相似文献
6.
7.
Ivan H.R. Tomi 《Journal of Saudi Chemical Society》2012,16(2):153-159
One new homologous series of compounds containing 1,2,4- and 1,3,4-oxadiazole rings in the same molecule was synthesized. 3-(4-Butoxyphenyl)-5-{4-[5-(4-alkoxyphenyl)-1,3,4-oxadiazol-2-yl]phenyl}-1,2,4-oxadiazole (VII)1–8 were synthesized by several procedures. This series has been characterized by FT-IR and 1H NMR spectroscopy. Their liquid crystalline properties were studied by polarizing optical microscopy (POM) and differential scanning calorimetry (DSC). This series did not show any liquid crystalline behaviors and only crystal to isotropic liquid transition was observed. 相似文献
8.
Ali Ramazani Ali Souldozi 《Phosphorus, sulfur, and silicon and the related elements》2013,188(12):3191-3198
The reaction of 3-substituted benzoic acid derivatives with (N-isocyanimino) triphenylphosphorane proceeds smoothly at room temperature to afford corresponding 1,3,4-oxadiazoles via an intramolecular aza-Wittig reaction in excellent yields under neutral conditions. 相似文献
9.
M. A. Pudovik L. K. Kibardina R. Kh. Al'myanova R. M. Kamalov A. N. Pudovik 《Russian Chemical Bulletin》1996,45(7):1769-1770
The reactions ofO-phenyl chloromethylisothiocyanatothioxophosphonate andO-phenyl chloromethylisocyanatophosphonate with trimethylsilyldiethylamine lead to the formation of 1,3,4-thiazaphosphol-2-ine and 1,3,4-oxazaphosphol-2-ine, respectively. Phosphorylation ofN-methyl-N-phenyl-N,N-bis(trimethylsilyl)urea withO-phenyl chloromethylchlorophos phonate gives 1,3,4-diazaphospholidin-2-one.Translated fromIzvestiya Akademii Nauk, Seriya Khimicheskaya, No. 7, pp. 1857–1859, July, 1996. 相似文献
10.
用5-氯邻羟苯甲醛与2-氨基-5-硝基噻唑(L1H)和4-氯苯甲醛与2-氨基-3-羟基吡啶(L2H)的反应,再用传统和微波方法将生成物与Cr髥,Co(II),Ni髤和Cu髤合成了一些席夫碱配合物。用元素分析,FTIR,快原子轰击质谱,摩尔电导率,电子光谱,1H-NMR,ESR,磁化率,热分析,电导率和XRD等对这些化合物进行了表征。这些配合物在空气中稳定并有颜色。分析数据表明所有配合物金属与配体的比均为1∶2,配位数为4或6。原子轰击质谱和热分析数据说明了这些配合物的降解方式。XRD图给出了这些配合物的结晶情况。席夫碱的上述金属配合物对革兰氏阳性菌:金黄色葡萄球菌和革兰氏阴性菌:大肠埃希菌(大肠杆菌)和真菌:黑曲霉和白色念珠菌显示出良好的抗菌活性。 相似文献
11.
M. M. Hamad S. A. Said Y. M. El-Ekyabi 《Monatshefte für Chemie / Chemical Monthly》1996,127(5):549-555
Summary The title compound (4) was synthesized from thioglycolic acid hydrazide and ethyl chloroformate. The reactions of4 with aromatic amines, amino derivatives, hydrazine hydrate, hydroxylamine, and formamide were studied. Addition of compound4 to ,-unsaturated compounds,i.e. chalcones, maleic anhydride, quinones, and acrylonitrile, was investigated.
Synthese und Reaktionen von 2-Mercaptomethyl-1,3,4-oxadiazolin-5-on
Zusammenfassung Die Titelverbindung (4) wurde aus Thioglycolsäurehydrazid und Chlorameisensäureethylester hergestellt. Die Reaktionen von4 mit aromatischen Aminen, Aminoderivaten, Hydrazinhydrat, Hydroxylamin und Formamid sowie die Addition von4 an ,-ungesättigte Verbindungen (Chalkone, Maleinsäureanhydrid, Chinone, Acetonitril) wurden untersucht.相似文献
12.
Franziska Emmerling Ingo Orgzall Günter Reck Burkhard W. Schulz Sabine Stockhause Burkhard Schulz 《Journal of Molecular Structure》2006,800(1-3):74-84
Crystal structures of four different di-aryl-1,3,4-oxadiazole compounds (aryl = 2-pyridyl-, 3-pyridyl-, 2-aminophenyl-, 3-aminophenyl-) are determined. Crystallization of di(2-pyridyl)-1,3,4-oxadiazole yielded monoclinic and triclinic polymorphs. The structures are characterized by the occurrence of π–π interactions. Additionally, in case of the aminophenyl compounds intra- as well as intermolecular hydrogen bonds are found that influence the packing motif as well. Since these molecules are often used as ligands in metal–organic complexes similarities and differences of the molecular conformation between the molecules in the pure crystals and that of the ligands in the complexes are discussed. 相似文献
13.
Eighteen novel ω-(5-Aryl-1,3.4-oxadiazol-2-thio)-ω-(1-H-1,2,4-triazol-1-yl)acetophenones ( 4a-4i ) and ω-(5-Aryl-1,3,4-oxadiazol-2-thioacetoxyl)-ω-(1-H-1,2,4-triazol-1-yl)acetophenones ( 5a-5i ) were synthesized. All the compounds synthesized were confirmed by elemental analyses and spectral data. The biological activity of representative compounds was evaluated. 相似文献
14.
Synthesis,Structural Characterization and Preliminary Biological Studies of Several Heterocyclic Transition Metal Carbonyl Complexes 下载免费PDF全文
Shanfang Hu Xianwei Cui Weimin He Xiangyi Chen Zikuan Gu Jingzhe Zhao Guang Zeng Zhan Shi Lei Zhu Hemin Nie 《无机化学与普通化学杂志》2015,641(14):2452-2459
The reaction of molybdenum, tungsten and manganese carbonyls with several thiazole heterocycle ligands yielded a number of coordinated transition metal complexes 1 – 10 . Of these complexes 1 – 6 are new compounds which have not been reported to date. The structures of new compounds were characterized by FT‐IR and 1H‐NMR spectroscopy as well as single‐crystal X‐ray diffraction analysis. Complexes 1 – 10 are carbon monoxide releasing molecules that show structure‐related anti‐cancer activity. The cytotoxicity of all compounds on Hela cells was evaluated by MTT assay, and the results show that carbon monoxide releasing molecules containing such Schiff base ligands may have biomedical applications for their anti‐tumor effect. 相似文献
15.
A novel quadridentate, N2O2 type Schiff base, synthesized from 1,4‐bis‐(o‐aminophenoxy)butane and 2‐hydroxynaphthalin‐1‐carbaldehyde, forms stable complexes with transition metal ions such as Co(II), Cu(II) and Ni(II) in DMF. Microanalytical data, elemental analysis, magnetic measurements, UV‐visible and IR‐spectra as well as conductance measurements were used to confirm the structures. Electrochemical measurements show that metal complexes undergo quasi‐reversible one‐electron redox processes. The voltammetric results also revealed that the CuL complex has the highest electron transfer rate indicating that both the Cu(II) and Cu(I) forms appear in a similar planar configuration, so the electron transfer does not require larger reorganization of the complex. 相似文献
16.
A series of bipolar-transporting europium(III) complexes containing carbazole and oxadiazole units were synthesized and characterized. Two intense UV absorption bands at around 286 nm and 352 nm, and sharply red emissions peaked at 614 nm were observed for these europium complexes in dichloromethane. Importantly, the bipolar-transporting europium(III) complexes exhibited higher thermal stability, more intense UV absorption at 286 nm and twofold increased photoluminescent quantum yield compared to the reported red chromophore of tri(dibenzoylmethane) (1,10-phenanthroline) europium(III). 相似文献
17.
多二茂铁基二氮杂己烷及其过渡金属配合物的合成 总被引:14,自引:1,他引:14
乙二胺与二茂铁甲醛或双二茂铁甲基氟硼酸盐反应,合成了1,6-二(二茂铁基)-2,5-二氮杂己烷和1,1,6,6-四(二茂铁基)-2,5-二氮己烷,它们与过渡金属(Fe^2+,Co^2+,Ni^2+,Cu^2+,Zn^2+)盐在乙醇或乙醇-二氯甲烷中反应,是14种过渡金属配合物,对这些化合物进行了表征,二种配体及其铜配合物用作复合固体推进剂的燃速调节剂时,基本不迁移,而燃速催化效率均超过辛基二茂铁。 相似文献
18.
Yu Liu Kong Qiang Xing Ji Yong Deng Mei Xiang Zhu Xia Yu Wang Wei Guo Zhu 《中国化学快报》2007,18(5):573-576
A novel terbium complex using 1,3,4-oxadiazole derivative as a neutral ligand was synthesized and characterized. Its thermal stability and photoluminescent properties were studied. The strong emission peaked at 546 nm with a full width at half maximum of 5 nm was observed in the pure terbium complex film under excitation of 328 nm light, which is attributed to the characteristic emission of terbium ion. The good thermal stability and intense sharp emission of this terbium complex display its potential application in electroluminescence devices. 相似文献
19.
K. A. Volkova V. N. Elokhina A. S. Nakhmanovich L. I. Larina A. I. Albanov 《Chemistry of Heterocyclic Compounds》2006,42(10):1343-1345
The reaction of benzoyl(2-furoyl)hydrazines with 1,3-dibromopropyne on heating in acetonitrile in 1:1 or 1:2 ratio of the
reagents gave exclusively substituted 2-phenyl(2-furyl)-1,3,4-oxadiazine hydrobromides.
__________
Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, 1555–1557, October, 2006. 相似文献
20.
The chemistry of metal-oxo compounds has been extensively and intensively studied for over a hundred years because of their theoritical importance and practical application[1]. Recent advance has afforded a study of inorganic or organometallic complexes containing metal-oxo anions[2]. Herein, the synthesis and structural characterization of two heteropolyoxomolybdnum-supported transition metal complexes (H2bpy)0.5Ni(H2O)5[Mo5P2O23]Ni(Hbpy)(H2O)4 (1) and (H2bpy)0.5Co(H2O)5[Mo5P2O23]Co(Hbpy) (H2O)4(2) are reported. 相似文献