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1.
《Journal of Saudi Chemical Society》2014,18(6):1015-1021
A series of 1-(4-substitutedphenyl)-3-phenyl-1H-pyrazole-4-carbaldehydes 4a–l have been synthesized and tested for their biological activities. Formation of the pyrazole derivatives was achieved by treating with Vilsmeier-Haack reagent. The newly synthesized compounds were evaluated for their anti-inflammatory and analgesic activities compared to Diclofenac sodium as standard drug. Compounds 4g, 4i and 4k exhibited the maximum anti-inflammatory and analgesic activities. The detailed synthesis, spectroscopic and toxicity data are reported. 相似文献
2.
Ghoneim AA 《Chemistry Central journal》2011,5(1):7
Practical procedures for production of variously blocked compounds from L-rhamnose have been developed. These compounds are
highly useful as indirect β-L-rhamnosyl donors. This approach represents a new method for the synthesis of aromatic nucleoside analogues and the synthesis
of (
3S, 4S, 5S, 6R) 3, 4, 5-triacetoxy-2-methyl-7,9-diaza-1-oxa-spiro [4,5]decane-10-one-8-thione (7). 相似文献
3.
Phenyltriazolinones are one of the most important classes of herbicides targeting the protoporphyrinogen oxidase enzyme. A series of triazolinone derivatives containing a strobilurin pharmacophore were designed and synthesized with the aim of discovering new phenyltriazolinone analogues with high activity. The herbicidal activity of the synthesized compounds was assayed and some of the test compounds displayed moderate herbicidal activity at 150 g ai/ha. 相似文献
4.
An environmentally benign, one-pot, four-component synthesis of chemically and pharmaceutically interesting dithiocarbamate derivatives is reported. The one-pot reaction of various aromatic aldehydes, ketones, aliphatic amines, and carbon disulfide, in the presence of potassium hydroxide in urea-choline chloride deep eutectic solvent or ethanol, leads to the corresponding dithiocarbamates in good to excellent yields. This method provides a convenient and time-saving strategy, with a simple work-up procedure. 相似文献
5.
Mostafa Kiamehr 《Tetrahedron letters》2009,50(48):6723-1999
An efficient synthesis of pentacyclic indole derivatives is achieved via domino Knoevenagel-hetero-Diels-Alder reactions of indolin-2-thiones and O-propargylated salicylaldehyde derivatives in CH3CN in the presence of 10 mol % of ZnO as a heterogeneous catalyst. The products are formed in good to excellent yields. 相似文献
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Xing-Hai Liu Jian-Quan Weng Bao-Lei Wang Yong-Hong Li Cheng-Xia Tan Zheng-Ming Li 《Research on Chemical Intermediates》2014,40(8):2605-2612
Microwave irradiation was used for synthesis of a series of novel fluorinated 1,2,4-triazole derivatives. The molecular structures of the compounds were determined by use of 1H NMR and FTIR spectroscopy and MS and HRMS. Study of their biological activity showed most of the compounds had good herbicidal activity. 相似文献
8.
Sandra Jiménez-Alonso Haydee Chávez Ana Estévez-Braun Ángel G. Ravelo Gabriela Feresin 《Tetrahedron》2008,64(37):8938-8942
The synthesis of novel pyrano embelin derivatives has been achieved through domino Knoevenagel hetero Diels-Alder reactions of embelin (1) with paraformaldehyde and electron rich alkenes. This synthetic approach is highly efficient when microwave irradiation is used. 相似文献
9.
Naofumi Terada Minoru Morimoto Hiroyuki Saimoto Yoshiharu Okamoto Saburo Minami Yoshihiro Shigemasa 《先进技术聚合物》2003,14(1):40-51
Oxidized chitosan derivatives with various degrees of oxidation (DS, 0.1–1.0) were prepared by the treatment of chitosan with CrO3/aq HClO4 or by the oxidation of 3‐O‐ and N‐protected chitosan with 30% aq H2O2/Na2WO4 followed by 3‐O‐ and N‐deprotection. The oxidized products were then N‐acetylated with Ac2O in order to improve their water‐solubility. Although the oxidized chitosan derivative of DS 0.28 and the degree of N‐acetylation of chitosan (DA) 38% was insoluble in the pH 3–8 region, that of DS 0.26 and DA 76% was soluble in the neutral pH range. The newly‐prepared acetylated and oxidized chitosan derivatives were found to suppress the chemiluminescence response of inflammatory cells such as canine polymorphonuclear cells (PMNs). Analysis by the surface plasmon resonance method revealed that the bind and release behavior of PMNs to acetylated oxidized chitosan derivatives was similar to that against carboxymethylated chitosan derivatives. The amount of water‐soluble chitosan derivative bound to cytokine IL‐8 was found to be affected by the structural and electronic features of the chitosan substituents in the chitosan chain. Copyright © 2003 John Wiley & Sons, Ltd. 相似文献
10.
Takashi Kitayama Maki Nakahira Kae Yamasaki Hiromi Inoue Chika Imada Yuji Yonekura Masataka Awata Hikaru Takaya Yasushi Kawai Kohta Ohnishi Akira Murakami 《Tetrahedron》2013
Zerumbone 1, having powerful latent reactivity and containing two conjugated double bonds and a double conjugated carbonyl group is the major component of the essential oil of wild ginger, Zingiber zerumbet Smith. The conjugation system plays an important role in the expression of biological activity. N-Bromosuccinimide (NBS) reaction of 1 gave high reactive intermediate 2 with an exo-methylene group, which was obtained from 1 quantitatively. Treatment of 2 with nucleophiles gave various zerumbone-pendant derivatives, including C–H, C–O, C–N, and C–C bond formation, maintaining the conjugation system through SN2′-type reaction. Almost all zerumbone-pendant derivatives showed a good value of IC50 against the suppressive effect of NO generation. Among them, amine derivative 5, binding with 2 mol of zerumbone, showed the strongest activity (IC50: 0.24 μM). 相似文献
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Fustero S Salavert E Sanz-Cervera JF Piera J Asensio A 《Chemical communications (Cambridge, England)》2003,(7):844-845
A series of potentially biologically active fluorinated uracil derivatives has been prepared in three steps from oxazolines and fluorinated nitriles with good chemical yields. 相似文献
13.
The ring openings of 1-acetyl-4-phenyl-3-oxabicyclo[3.1.0]hexane afforded alpha-acetyl-gamma-butyrolactone that underwent a novel diazo-transfer reaction, followed by C-H insertion, to provide a series of endo,exo-furofuranone analogues. 相似文献
14.
This review covers the chemistry of allobetulin analogs, including their formation by rearrangement from betulin derivatives, their further derivatisation, their fusion with heterocyclic rings, and any further rearrangements of allobetulin compounds including ring opening, ring contraction and ring expansion reactions. In the last part, the most important biological activities of allobetulin derivatives are listed. One hundred and fifteen references are cited and the relevant literature is covered, starting in 1922 up to the end of 2010. 相似文献
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Kamiya S Shirahase H Yoshimi A Nakamura S Kanda M Matsui H Kasai M Takahashi K Kurahashi K 《Chemical & pharmaceutical bulletin》2000,48(6):817-827
We synthesized a series of indoline derivatives with an amide or urea moiety and examined their inhibitory effects on acyl-CoA:cholesterol acyltransferase (ACAT) activity, lipid-peroxidation and serum cholesterol levels in experimental animals. Among the derivatives synthesized, a series of N-(1-alkyl-4,6-dimethylindolin-7-yl)-2,2-dimethylpropanamides++ + potently inhibited rabbit intestinal ACAT activity and lipid-peroxidation of rat brain homogenate. The effect on ACAT activity was related to the length of the alkyl chain at the 1-position of indoline. N-(4,6-Dimethyl-1-octylindolindolin-7-yl)-2,2-dimethylpropanami de hydrochloride (55) showed inhibitory effects on intestinal and hepatic ACAT activity slightly weaker than those of YM-750, and an inhibitory effect on low density lipoprotein (LDL)-peroxidation similar to that of probucol. Compound 55 also reduced serum cholesterol at 10 mg/kg/d in hyperlipidemic rats and 20 mg/kg/d in normolipidemic hamsters. The plasma concentration of 55 reached 716 ng/ml in dogs (10 mg/kg, p.o.), which is an effective concentration against hepatic ACAT activity and LDL-peroxidation. In conclusion, compound 55 is a novel bioavailable ACAT inhibitor with anti-peroxidative activity and is thus a promising anti-atherosclerotic and anti-hyperlipidemic drug. Indoline proved to be a useful pharmacophore for molecular design of new anti-peroxidative drugs. 相似文献
17.
Rapid one-step synthesis of hitherto unreported indole-annulated pentacyclic heterocycles containing oxygen, nitrogen, and sulfur has been described by domino-Knoevenagel-hetero-Diels-Alder reaction. The reaction sequence provides a route to the synthesis of a novel type of polyheterocycles in excellent yields with high stereoselectivity. 相似文献
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We present a convenient synthesis of novel pyrrole- and indole-fused 1-oxo-1,2,3,4-tetrahydropyrazine heterocyclic structures using a novel modification of four-component Ugi condensation. We demonstrate the usefulness and versatility of the developed approach for the synthesis of variously substituted compounds, and discuss the scope and limitations of the chemistry involved. 相似文献
20.
Zhong Lv Zhang Zhi Jie Sun Fei Xue Xian Jin Luo Nai Yun Xiu Li Teng Zong Gen Peng 《中国化学快报》2009,20(8):921-923
A series of novel benzimidazole derivatives was synthesized and their anti-Coxsackie virus B_3(CVB_3) activity was evaluated in VERO cells.Compounds 9 and 10 exhibited better inhibitory activity than those of ribavirin(RBV) with IC_(50) values of 5.30 and 1.06μg/mL,respectively. 相似文献