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1.
A series of benzotriazole-azo-phenol/aniline derivatives were prepared and evaluated for their antifungal activities against six phytopathogenic fungi such as Fusarium graminearum, Fusarium solani, Alternaria alternate, Valsa mali, Botrytis cinerea, and Curvularia lunata. Among them, compounds IIf, IIn, and IIr showed a broad-spectrum of potent antifungal activities. Especially some compounds displayed 3.5–10.8 folds more potent activities than carbendazim against A. alternata and C. lunata. Notably, compounds IIc, IIm, and IIr exhibited good protective and therapeutic effects against B. cinerea at 200?μg/mL. Their structure-activity relationships were also discussed. 相似文献
2.
Giancarlo Gioia Lobbia Claudio Pettinari Brian W. Skelton 《Inorganica chimica acta》2005,358(13):3633-3641
New silver(I) derivatives [Ag{HnB(btz)4 − n}(PR3)x] (n = 1 or 2, x ranging from 1 to 3), containing monodentate tertiary phosphines and anionic poly(benzotriazol-1-yl)borates, have been prepared from the reaction of AgNO3 with PR3 (R = Ph, o-tolyl, m-tolyl, p-tolyl, Bns) and K[H2B(btz)2], or K[HB(btz)3] (Hbtz = 1,2,3-benzotriazole). When the reaction between K[H2B(btz)2] and AgNO3 was carried out in the presence of dppe (1,2-bis(diphenylphosphino)ethane), or dppf (1,1′-bis(diphenylphosphino)ferrocene), compounds [Ag{H2B(btz)2}]2(L) (L = dppe or dppf) formed, the diphosphine acting as a bidentate bridging P2-donor. Solid state and solution properties of all complexes have been investigated through analytical and spectroscopic measurements (IR, 1H, 31P NMR), the 1H and 31P NMR spectra being interpreted in terms of equilibria that involve mono- and di-nuclear complexes. Adducts [Ag{HB(btz)3}(PPh3)3] · (1/2H2O) and [Ag{H2B(btz)2}]2 (dppf) have been characterised by single crystal X-ray studies. In the former, the HB(btz)3 is unidentate in an NAgP3 coordination environment; the latter is a dimer, the dppf bridging the two silver atoms, while the H2B(btz)2 ligand, which chelates one silver, bridges to the second also, the array having 2-symmetry. 相似文献
3.
《Bioorganic & medicinal chemistry letters》2014,24(7):1856-1861
Amino acid conjugates of quinolone, metronidazole and sulfadiazine antibiotics were synthesized in good yields using benzotriazole methodology. All the conjugates were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Antibiotic conjugates were tested for activity in four medically relevant organisms; Staphylococcus aureus (RN4220), Escherichia coli (DH5α), Pseudomonas aeruginosa (PAO1), and Bacillus subtilis (168). Several antibiotic conjugates show promising results against several of the strains screened. 相似文献
4.
A series of novel benzotriazole N-acylarylhydrazone hybrids was synthesized according fragment-based design strategy. All the synthesized compounds were evaluated for their anticancer activity against 60 human tumor cell lines by NCI (USA). Five compounds: 3d, 3e, 3f, 3o and 3q exhibited significant to potent anticancer activity at low concentrations. Compound 3q showed the most prominent broad-spectrum anticancer activity against 34 tumor cell lines, with mean growth inhibition percent of 45.80%. It exerted the highest potency against colon HT-29 cell line, with cell growth inhibition 86.86%. All leukemia cell lines were highly sensitive to compound 3q. Additionally, compound 3q demonstrated lethal activity to MDA-MB-435 belonging melanoma. Compound 3e exhibited the highest anticancer activity against leukemic CCRF-CEM and HL-60(TB) cell lines, with cell growth inhibition 86.69% and 86.42%, respectively. Moreover, it exerted marked potency against ovarian OVCAR-3 cancer cell line, with cell growth inhibition 78.24%. Four compounds: 3d, 3e, 3f and 3q were further studied through determination of IC50 values against the most sensitive cancer cell lines. The four compounds exhibited highly potent anticancer activity against ovarian cancer OVCAR-3 and leukemia HL-60 (TB) cell lines, with IC50 values in nano-molar range between 25 and 130 nM. They showed 18–2.3 folds more potent anticancer activity than doxorubicin. The most prominent compound was 3e, (IC50 values 29 and 25 nM against OVCAR-3 and HL-60 (TB) cell lines, respectively), representing 10 and 18 folds more potency than doxorubicin. The anti-proliferative activity of these four compounds appeared to correlate well with their ability to inhibit FAK at nano-molar range between 44.6 and 80.75 nM. Compound 3e was a potent, inhibitor of FAK and Pyk2 activity with IC50 values of 44.6 and 70.19 nM, respectively. It was 1.6 fold less potent for Pyk2 than FAK. Additionally, it displayed inhibition in cell based assay measuring phosphorylated-FAK (IC50 = 32.72 nM). Inhibition of FAK enzyme led to a significant increase in the level of active caspase-3, compared to control (11.35 folds), accumulation of cells in pre-G1 phase and annexin-V and propidium iodide staining in addition to cell cycle arrest at G2/M phase indicating that cell death proceeded through an apoptotic mechanism. 相似文献
5.
Hydrothermal reactions of cobalt(II) salt with H2CAM or H2SDBA and HBTA in the presence of NaOH afford two interesting coordination polymers, Co3(CAM)2(BTA)2 (1) and Co3(SDBA)2(BTA)2 (2) (H2CAM = camphoric acid, H2SDBA = 4,4′-dicarboxybiphenyl sulfone, HBTA = benzotriazole), both of which have been structurally characterized by single-crystal X-ray, elemental analysis, infrared spectroscopy, and thermogravimetric analysis. Complexes 1 and 2 are isostructural and possess two-dimensional covalent network, comprising an unusual linear Co(II) chains of mixed Td-Oh-Td geometries. Temperature-dependent magnetic measurements indicate the existence of antiferromagnetic interactions in both 1 and 2. 相似文献
6.
Carlo Santini Maura Pellei Simone Alidori Donatella Fedeli 《Inorganica chimica acta》2004,357(12):3549-3555
New copper(I) complexes have been synthesized from the reaction of CuCl with 4- or 2-(diphenylphosphane)benzoic acid and KH2B(btz)2, KHB(btz)3, NaTpMe, KpzTp, KpzTpMe and KH2B(im)2(dmac). The complexes obtained have been characterized by elemental analyses and FT-IR in the solid state, and by NMR (1H and 31P{1H}) and electrospray mass spectroscopy in solution.Chemiluminescence technique was used to evaluate the superoxide scavenging activity of these new copper complexes. 相似文献
7.
A series of [4-(2H-1,2,3-benzotriazol-2-yl)phenoxy]alkanoic acids has been synthesized and tested as agonists of Peroxisome Proliferator-Activated Receptor (PPAR) alpha, gamma, and delta. Three compounds displayed 56 to 96% of maximal activity of the reference drug Wy-14643 on PPARalpha, and two of these, i.e., 1 and 5, exhibited also moderate activity on either PPARgamma or delta with efficacy equal to 50% and 46% of that of rosiglitazone and GW 501516, respectively. Thus, compounds 1 and 5 represent interesting starting point for preparing novel agents for the treatment of dyslipidemia or of dyslipidemic type-2 diabetes. 相似文献
8.
Hydrothermal synthesis of two novel three-dimensional cobalt(II) metal-organic frameworks based on polycarboxylate and benzotriazole 总被引:1,自引:0,他引:1
Guang-Xiang Liu Liang-Fang Huang Xue-Jun Kong Rong-Yi Huang Heng Xu 《Inorganica chimica acta》2009,362(6):1755-804
The hydrothermal reactions of 1,4-H2BDC or 1,4-H2CDC, HBTA, with Co(NO3)2 · 6H2O in basified solvent gave rise to two coordination polymers, Co5(μ3-OH)2(1,4-BDC)3(BTA)2 (1), [Co(1,4-CDC)0.5(BTA)] (2) (1,4-H2BDC = 1,4-benzenedicarboxylic acid, 1,4-H2CDC = 1,4-cyclohexanedicarboxylic acid, HBTA = benzotriazole) and characterized by elemental analysis, IR, single-crystal X-ray diffraction and variable-temperature magnetic measurements. Complex 1 crystallizes in the triclinic system, P space group; the structure determination reveals that 1 has a scarcely reported 8-connected 3D self-penetrating structure based on pentanuclear cobalt clusters. Complex 2 is monoclinic system, P21/c space group, and the X-ray structural analysis shows that 2 has a 3D infinite network with (4.64.8)(42.62.82) topology. Complex 1 exhibits moderately antiferromagnetic coupling, while complex 2 indicating strong spin-orbit coupling. 相似文献
9.
De Moor O Dorgan CR Johnson PD Lambert AG Lecci C Maillol C Nugent G Poignant SD Price PD Pye RJ Storer R Tinsley JM Vickers R Well R Wilkes FJ Wilson FX Wren SP Wynne GM 《Bioorganic & medicinal chemistry letters》2011,21(16):4828-4831
Families of 2-arylbenzotriazoles and 2-arylindazoles that show positive effects in screens predictive of endogenous utrophin upregulation have been identified. Synthesis and structure-activity relationships are described leading to compounds with attractive in vitro profiles. 相似文献
10.
A convenient strategy is reported for the synthesis of azole nucleoside analogues of D-pinitol (=3-O-methyl-D-chiro-inositol). The key intermediate 3-O-methyl-4,5-epoxy-D-chiro-inositol was obtained in excellent yield via an epoxidation from mono-methanesulfonate of D-pinitol. The process of opening of the epoxy ring by azole-bases appeared strongly regioselective in the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene. All newly synthesized carbocyclic azole nucleosides were assayed against lung and bladder cancer in vitro. Only the triazole and benzotriazole nucleoside analogues inhibited the growth of human lung cancer cell lines (PG) with EC(50) of 11.3 and 22.6 microM, respectively, and showed much less inhibitory activity against human bladder cell lines (T(24)). 相似文献