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1.
Flekhter O. B. Boreko E. I. Nigmatullina L. R. Pavlova N. I. Nikolaeva S. N. Savinova O. V. Eremin V. F. Baltina L. A. Galin F. Z. Tolstikov G. A. 《Russian Journal of Bioorganic Chemistry》2003,29(3):296-302
New nitrogen-containing derivatives of betulinic and betulonic acids, hydrazides and N"-benzalhydrazides, were synthesized. Their antiviral activities toward viruses of influenza A virus, herpes simplex type I virus, enterovirus ECHO6, and HIV-1 were studied in vitro. Betulinic acid 3-oxime was found to have the highest activity against the influenza virus. Betulonic acid, betulinic acid 4-chlorobenzalhydrazide, betulonic acid 3-oxime benzalhydrazide, and betulinic acid hydrazide inhibited the replication of herpes simplex type I virus. Betulinic acid hydrazide also showed antiviral activity toward HIV-1. All the derivatives of betulinic acid under study displayed a low antiviral activity toward enterovirus ECHO6. 相似文献
2.
Protein carbonyl detection has been commonly used to analyze the degree of damage to proteins under oxidative stress conditions. Most laboratories rely on derivatization of carbonyl groups with dinitrophenylhydrazine followed by Western blot analysis using antibodies against the dinitrophenyl moiety. This paper describes a protein carbonyl detection method based on fluorescent Bodipy, Cy3 and Cy5 hydrazides. Using this approach, Western blot and immunodetection are no longer needed, shortening the procedure and increasing accuracy. Combination of Cy3 and Cy5 hydrazides allows multiplexing analyses in a single two-dimensional gel. Derivatization with Bodipy hydrazide allows easy matching of the spots of interest and those obtained by general fluorescent protein staining methods, which facilitates excising target proteins from the gels and identifying them. This method is effective for detecting protein carbonylation in samples of proteins submitted to metal-catalyzed oxidation "in vitro" and assessing the effect of hydrogen peroxide and chronological aging on protein oxidative damage in yeast cells. 相似文献
3.
2-substitued-benzopyrimidinones 2 were synthesized in high to excellent yields in a single step via condensation of 2-aminobenzamide 1 with some aryl-aldehydes in the presence of iodine. Cyclocondensation reaction of hydrazides 3 which were obtained in two steps from benzopyrimidinones 2, with some electrophilic species such as 2,4-pentandione, 2,5-hexandione, 1-phenylbutan-1,3-dione and cyclic anyhdrides provided the new compounds 4a–c, 5a–c, 6a–c, 7a–c, 8a–c and 9a–c. The synthesized compounds were characterized by spectroscopic means. They were also evaluated for their anti-tyrosinase potential. The structure-activity relationship (SAR) was discussed on the basis of the molecular docking analysis. 相似文献
4.
Camarero Julio A. Adeva Alberto Muir Tom W. 《International journal of peptide research and therapeutics》2000,7(1):17-21
Summary This paper describes a practical new use of 3-mercaptopropionic acid as a highly versatile multidetachable linker for solid-phase
synthesis. Our approach is based on the stability of the alkylthioester functionality to optimized Boc-SPPS protocols and
HF treatment, as well as on the mild activation of the thioester functionality toward nucleophilic or reductive displacement.
This allows several C-terminal modifications to be introduced into a synthetic molecule during the cleavage step. We have
shown that unprotected peptides can be efficiently cleaved from a propyl thioester-polyethylene glycol-poly-(N,N-dimethylacrylamide) copolymer resin using a great variety of nucleophiles to give the corresponding C-terminally modified
peptides (esters, thioesters, carboxylic acids, thioacids, amides, hydroxamic acids, hydrazides, alcohols). The nucleophilic
cleavage reaction is both rapid and exceptionally clean in all the cases tested.
Abbreviations: HBTU,N-[(1H-benzotriazol-1-yl)(dimethylamino)methylene]-N-methylmethanaminium hexafluorophosphateN-oxide); DIEA,N,N-diisopropylethylamine; DMF,N,N-dimethyl formamide; ES-MS, electrospray mass spectrometry; FAB-MS, fast atom bombardment mass spectrometry; HMBA, hydroxymethylbenzoic
acid; HPLC, high performance liquid chromatography; PBS: phosphate buffer saline; PEGA, polyethylene glycolpoly-(N,N-dimethylacrylamide); TFA, trifluoroacetic acid; SPPS, solid-phase peptide synthesis. Standard IUPAC single and triple letter
codes for amino acids are used throughout 相似文献
5.
Õrfi László Wáczek Frigyes Kövesdi István Mészáros György Idei Miklós Horváth Anikó Hollósy Ferenc Mák Marianna Szegedi Zsolt Szende Béla Kéri György 《International journal of peptide research and therapeutics》1999,6(5-6):325-333
A parallel combinatorial library of over 1600 compounds has been designed and synthesized for the development of new potential peptidomimetic protein tyrosine kinase (PTK) inhibitor leads. These peptidomimetic molecules are aimed at intervening with the substrate binding site of the pp60c-src enzyme. The new structures were based on known PTK inhibitors with at least two variously substituted aromatic moieties attached by spacer groups of different length and flexibility. Eleven bis-aryl-type inhibitory compounds were found in the range of 18–100 μM IC50 concentrations from combinations of 12 different substituents. Molecular modeling of the active compounds showed a characteristic distance of 12–14 Å between the farthest sp2 carbon atoms of the two aromatic rings. Conformational analysis of several peptide substrates recently found for pp60c-src PTK showed that the energy-minimized conformers had the same distance between the two aromatic moieties. Several compounds in the library not only showed remarkable PTK inhibitory activity but also a significant apoptosis-inducing effect on HT-29 human colon tumor cells. 相似文献
6.
Anindita Sarkar 《Inorganica chimica acta》2009,362(10):3807-1603
In acetonitrile, reactions of bis(acetylacetonato)oxidovanadium(IV) ([VO(acac)2]) with 4-R-benzoylhydrazine in 1:1 mole ratio provide coordinatively symmetrical complexes (1-5) of the {OV(μ-O)VO}4+ motif in 40-47% yields. On the other hand, in methanol the same reactants provide complexes (6-10) containing the {OV(μ-OMe)2VO}4+ core in 37-50% yields. In both series of complexes, the ligand is the O,N,O-donor deprotonated Schiff base system 4-R-benzoic acid (1-methyl-3-oxo-butylidene)-hydrazide formed by template condensation of acac− with 4-R-benzoylhydrazine (R = H, Cl, OMe, NO2 and NMe2). All the complexes have been characterized by elemental analysis, magnetic and spectroscopic (IR, UV-Vis and NMR) measurements. Molecular structures of three representative complexes (4, 6 and 7) have been determined by X-ray crystallography. In each complex, the dianionic planar ligand is coordinated to the metal centre via the enolate-O, the imine-N and the O-atom of the deprotonated amide functionality. Cyclic voltammetric measurements in dichloromethane revealed that complexes 1-5 are redox inactive, while complexes 6-10 display a metal centred reduction in the potential range −0.06 to 0.0.32 V (versus Ag/AgCl). 相似文献
7.
《Bioorganic & medicinal chemistry》2014,22(5):1672-1679
A range of novel hydrazine bridged bis-indoles was prepared from readily available indole-7-glyoxyloylchlorides and 7-trichloroacetylindoles and underwent cyclodehydration to produce 2,5-di(7-indolyl)-1,3,4-oxadiazoles and a 2,2′-bi-1,3,4-oxadiazolyl with phosphoryl chloride in ethyl acetate. This efficient protocol was subsequently used for the synthesis of 2- and 7-indolyl 2-(1,3,4-thiadiazolyl)ketones from related indolyl-hydrazine carbothioamides. The synthesised bis-indoles were evaluated for their antimicrobial properties, particularly the inhibition of protein–protein complex formation between RNA polymerase and σ factor and their bactericidal effect on Gram positive Bacillus subtilis and Gram negative Escherichia coli. 相似文献
8.
Evaluation of mutagenicity of the antitubercular naphthylglycine hydrazides insalmonella typhimurium
N-(2-naphthyl)glycine hydrazide and N-methyl-N-(2-naphthyl) glycine hydrazide, which inhibitMycobacterium tuberculosis H37 RV and show activity against experimental tuberculosis, were evaluated for their mutagenic potential inSalmonella typhimurium. Both the compounds at concentration ranges from 0.1 Μgplate to 1000 Μg/plate failed to induce mutations at the histidine
locus either directly or after treatment with rat liver homogenate fraction-“S-9”. N-(2-naphthyl)glycine hydrazide and its
N-methyl derivative elicited toxicity at concentrations of 500 Μg/plate and 1000 Μg/plate. However, in the presence of the
liver homogenate system, reduction in toxicity was noticed probably due to detoxification and/ or conjugation of the compounds.
Under the assay conditions employed, standard mutagens like 4-nitroquinoline-N-oxide, 9-aminoacridine and benzo(a)pyrene were positive. The non-mutagenic nature of N-(2-naphthyl)glycine hydrazide and N-methyl-N-(2-naphthyl)glycine hydrazide
should enhance their potential for inclusion in treatment protocols for management of tuberculosis 相似文献
9.
Ahsana Dar Khalid M. Khan Humayun S. Ateeq Shagufta Khan Shagufta Rahat Shahnaz Perveen 《Journal of enzyme inhibition and medicinal chemistry》2013,28(3):269-274
A series of hydrazine derivatives was synthesized in order to evaluate their monoamine oxidase A (MAO-A) inhibitory effects. MAO-A inhibitory activity of 4-tosyl benzoic acid carbohydrazide was quite potent, similarly to that of the corresponding 4-benzyloxy-benzoic acid carbohydrazide and its N-cyanoethylated derivative. Structural variations of these compounds, such as the replacement of the 4-substitutent, of the aromatic ring on which the carbohydrazide moiety is grafted, as well as cyclization of the hydrazide moiety in five- or six-membered rings caused either significant decline or complete loss of MAO inhibitory properties. The most active compound (4-tosyl benzoic acid carbohydrazide) was also subjected to the forced swim test, an animal model of depression, eliciting a marked reduction in immobility time in rats, without affecting the locomotor activity, implying that it possesses anti-depressant properties due to inhibition of MAO type-A. 相似文献
10.
Malhotra V Pathak SR Nath R Mukherjee D Shanker K 《Bioorganic & medicinal chemistry letters》2011,21(3):936-939
A series of novel substituted imidazole derivatives were synthesized and have been screened in vivo for their hypotensive and acute toxicity activities. Out of seventeen compounds eight compounds (2b, 2c, 3b, 3c, 3f, 4a, 4b and 4c) have shown good hypotensive and bradycardiac responses. Compounds 3b, 3c, 3f and 4c have shown better activity than reference drug clonidine. All the compounds have shown ALD50 >1000 mg/kg with maximum in 2e and 4c (>1200 mg/kg). 相似文献