4-(硝基苯基)-3-硫代脲酸烷基酯类的合成及其生物活性研究

通过硝基苯胺同烷氧酰基异硫氰酸酯的化合反应以及钛酸丁酯的酯交换反应共合成了9个4-(硝基苯基)-3-硫代脲酸烷基酯类化合物(1-9)。通过各种波谱分析确定了它们的化学结构, 并研究了这类物质对农杆菌的抑制作用。     

4-Hydroxy-2-quinolones 7. Synthesis and biological properties of 1-R-3-(2-benzimidazolyl)-4-hydroxy-2-quinolones

Condensation of 1-R-3-carbethoxy-4-hydroxy-2-quinolones with o-phenylene diamine gives the corresponding 1-R-3-(2-benzimidazolyl)-4-hydroxy-2-quinolones. Data on a study of the antithyroid activity of the synthesized compounds is presented.For Communication 6, see [1].Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 1, pp. 105–108, January, 1993.We express our sincere thanks to A. A. Kirichenko and T. S. Bozhko for the study of the antithyroid activity.     

Enamine formation from anilines and methyl propiolate. The synthesis of 4(1h)-quinolones

The addition of substituted anilines to methyl propiolate produces labile cis-trans mixtures of enamines which can be isomerized by acid, solvent variation, and thermal techniques. Thermal cyclization of these enamines provides a synthesis of 4( lH)-quinolones.     

1-芳酰基-4-菊酰基氨基硫脲类化合物的合成及生物活性

本文利用菊酰基异硫氰酸酯与芳基酰肼的加成反应合成了16个新的酰氨基硫脲类化合物，其结构经^1H NMR，IR，MS和元素分析所确证，生物活性测定表明它们具有一定杀菌活性。     

Silyl methods for the modification of penicillin and cephalosporin (review)

The principal pathways of modification of -lactam antibiotics by means of silyl methods, including silylation, the preparation of N-acyl and amide analogs of penicillin and cephalosporin, the deacylation of N-protective groups, the epimerization of the side chain, the transformation of penicillin to cephalosporin, and other transformations, are examined.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 147–162, February, 1982.     

4-hydroxy-2-quinolones. 191.* synthesis,tautomerism and biological activity of benzimidazol-2-ylamides of 1-r-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acids

A series of benzimidazol-2-ylamides of 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acids was prepared in a search for biologically active compounds. These compounds exist in the crystal exclusively in the amide form, while in solution amide↔imide tautomerism is observed. The results of a study of the antithyroid and antituberculosis activities of these compounds are given.     

Pyranonaphthoquinones--isolation, biological activity and synthesis

A review of the isolation, biological activity and synthesis of pyranonaphthoquinones and closely related compounds is provided.     

硫脲类衍生物及其生物活性研究

本文以氯代甲酸酯与硫氰酸钾的反应产物烷氧酰基异硫氰酸酯同各种芳胺反应合成了十个硫脲类衍生物4-芳基-3-硫代脲酸酯类化合物(1～10),其中七个化合物尚未见文献报道。通过^1HNMR,IR,MS及元素分析和熔点的测定,确定了这十个化合物的结构,并研究了它们对农杆菌的抑制作用。     

4-hydroxy-2-quinolones. 176*. 4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids. synthesis,physicochemical and biological properties

We have carried out the synthesis and a comparative analysis of the acidic properties of a large group of 4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids. Features of the recorded NMR spectra of these compounds are discussed together with their analgesic properties.     

4-Hydroxy-2-quinolones 150*. Efficient synthesis,structure, and biological activities of 4-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid alkyl amides

A simple and efficient method for preparing 4-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid alkyl amides is proposed. The results of a study of the diuretic activity of the compounds synthesized are reported. *For communication 149 see [1]. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 12, pp. 1841-1848, December, 2008.     

A mild and efficient synthesis of 4-quinolones and quinolone heterocycles

The cycloacylation of aniline derivatives to 4-quinolones in the presence of Eaton's reagent is described. This high-yielding methodology is applicable to a wide variety of functionalized anilines and requires milder conditions than those traditionally employed. This cyclization protocol is used to prepare a host of heterocycles and bis-quinolones and is characterized by relatively low reaction temperature and ease of product isolation.     

(Aza,thio)xanthenylated amines and imines: synthesis,properties, and biological activity

Russian Chemical Bulletin - The review addresses the synthetic potential of cations or hydrols of (aza,thio)xanthenes in reactions with primary and secondary amines and imines. The diversity of...     

4-hydroxy-2-quinolones 170*. synthesis and bromination of N-allylisatin

Independently of the reaction conditions N-allylisatin forms only the 2,3-dibromo derivative upon treatment with molecular bromine in contrast to N-allyl-substituted quinolin- or pyrid-2-ones which readily undergo halocyclization to the corresponding 2-bromomethyl oxazoles.     

Synthesis of benzo-halogenated 4-hydroxy-2(1H)-quinolones

Malondianilides 3 derived from dichloro substituted anilines 2 undergo cyclization to afford 4-hydroxy-2(1H)-quinolones 4 in very good yields using methane sulfonic acid-phosphorus pentoxide as catalyst. 3,4-Dichloro anilines 5 can be shown to yield two isomers, 7 and 8 , whereas 3-substituted anilines 9 afford merely 7-substituted 4-hydroxy-2(1H)-quinolones 11.     

Copper(II) complexes with bioactive carboxyamide: synthesis, characterization and biological activity

Complexes of Cu(II) with bioactive carboxyamide ligands N',N'-bis(3-carboxy-1-oxoprop-2-enyl)2-amino-N-arylbenzamidine, N',N'-bis(3-carboxy-1-oxopropanyl)2-amino-N-arylbenzamidine and N',N'-bis(3-carboxy-1-oxophenelenyl)2-amino-N-arylbenzamidine have been synthesized and characterized by various physico-chemical techniques. Mass spectrum explains the successive degradation of the molecular species in solution and justifies ML complexes. Vibrational spectra indicate coordination of amide and carboxylate oxygen of the ligands along with water molecules. Electronic spectra and magnetic susceptibility measurements reveal octahedral geometry for Cu(II) complexes. The EPR of the reported complex show g( parallel)>g( perpendicular)>2.0023 and G value within the range 2.08-4.49 are consistent with [Formula: see text] ground state in an octahedral geometry. The voltammogram of the copper(II) complex shows a quasi-reversible redox process and a simple one electron process assignable to the Cu(II)/Cu(I) couple. Kinetic and thermodynamic parameters were computed from the thermal data using Coats and Redfern method, which confirm first order kinetics. The bio-efficacy of the ligands and its copper complexes have been examined against the growth of bacteria and pathogenic fungi in vitro to evaluate their antimicrobial potential. The results indicate that the ligand and its metal complexes possess notable antimicrobial properties.     

New fascaplysin-based CDK4-specific inhibitors: design, synthesis and biological activity

The first biologically active non-planar analogues of the toxic anti-cancer agent, fascaplysin, have been produced; we present the design, synthesis and biological activity of three tryptamine derivatives.