苯并异噻唑啉酮类化合物的合成与活性研究

通过烷基醇与固体三光气(BTC)反应后加入1,2-苯并异噻唑啉-2(3H)-酮(BIT)继续反应的“一锅法”制备了8种未见文献报道的2-(苯并异噻唑啉-3-酮-2-基)甲酸酯类化合物.化合物结构经IR、1HNMR和元素分析确认,并且对枯草芽孢杆菌、金黄色葡萄球菌、嗜水单细胞菌和大肠杆菌进行了初步抑菌活性实验,实验结果表...     

Morpholines. Synthesis and biological activity

The review analyzes methods of synthesis of 1,4-oxazines (morpholines) starting from vicinal amino alcohols and their derivatives, oxiranes, and aziridines. Examples of using morpholines in medicinal and organic chemistry as catalysts, auxiliaries, biologically active substances, and building blocks for their preparation are considered. The data published until February 2013 have been covered.     

Synthesis and biological activity of certain O-pyrimidinylketoximes

By the interaction of substituted chloropyrimidines with the sodium salts of oximes of aliphatic and alicyclic ketoximes, series of O-(4,6-dimethyl-2-pyrimidinyl)- and O-(2,4-dimethyl-6-pyrimidyl)ketoximes have been obtained. Through reactions of 2-methyl-4,6-dichloropyrimidine with salts of ketoximes, the corresponding monosubstituted and disubstituted products have been synthesized. The biological activities of the synthesized substances have been investigated.Erevan Institute of the National Economy, Erevan 375025. M. V. Lomonosov Moscow State University, Moscow 119899. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 950–956, July, 1997.     

Synthesis and biological activity of apratoxin derivatives

This review covers the total asymmetric synthesis and biological evaluation of derivatives of the marine natural products known as the apratoxins.     

Synthesis and biological activity of bactobolin glucosides

Bactobolin glucosides, 5-O-(alpha-D-glucopyranosyl)-, 5-O-(beta-D-glucopyranosyl)- and 6-O-(beta-D-glucopyranosyl)-bactobolin were prepared by glycosidation of bactobolin (1) with the glucopyranosyl trichloroacetoimidate. These compounds were evaluated antimicrobial activity and cytotoxicity.     

Synthesis and biological activity of mycalolide analogs

Mycalolide analog 4, consisting only of the side chain of mycalolide B (2), a trisoxazole macrolide of marine origin, was stereoselectively synthesized using Roush crotylboration, an Evans aldol reaction, and a Paterson aldol reaction as key steps. The analog 4 was found to have strong actin-depolymerizing activity.     

Synthesis and biological activity of yuccagenin bisrhamnoside

The two hydroxyls of yuccagenin can be glycosylated by Koenigs-Knorr condensation with acetobromorhammose in dichloroethane in the presence of mercuric cyanide. The bisrhamnoside of yuccagenin markedly lowers the cholesterol and triglyceride content in blood serum of healthy animals and animals with experimental hyperlipidemia.Translated from Khimiya Prirodnykh Soedinenii, No. 3, pp. 242–243, May–June, 2000.     

Monoterpenoids dithiophosphates. Synthesis and biological activity

O,O-Dialkyldithiophosphoric acids adds at the double bond of the racemic camphene and (+)- limonene in the presence of Lewis acids in accordance with the Markownikoff rule with the formation of Sterpenyl esters of dithiophosphoric acids. The reaction with camphene is accompanied by the rearrangement of camphane structure to that of bornane. Addition of dithiophosphoric acid to (+)-limonene proceeds with the participation of the exocyclic double bond. Toxic and genotoxic properties of the monoterpenoid dithiophosphates were studied.     

Synthesis and biological activity of bridgehead nitrogen heterocycles

The reaction of 3-(2,4-dichlorophenyl)-5-mercapto 1,2,4–1H-triazole with α-haloketones and with 1,2-dibromoethane leading to the formation of fused heterocycles were carried out and the orientation of cyclization was studied. The reaction of 3-(2,4-dichlorophenyl)-5-mercapto-4-amino-1,2,4-s-triazole with α-haloketones     

Synthesis and biological activity of dialkylamino-substituted phosphine oxides

A series of dialkylamino-substituted phosphine oxides was synthesized and their physiological activity was studied.     

Synthesis and biological activity of novel phenyltriazolinone derivatives

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.     

Synthesis and biological activity of novel epothilone aziridines

[reaction: see text]. A series of 12alpha,13alpha-aziridinyl epothilone derivatives were synthesized in an efficient manner from epothilone A. The final semisynthetic route involves a formal double-inversion of stereochemistry at both the C12 and C13 positions. All aziridine analogues were tested for effects on tubulin binding polymerization and cytotoxicity. The results indicate that the aziridine moiety is a viable isosteric replacement for the epoxide in the case of epothilones.     

哒嗪酮的乙酰胺类化合物的合成及生物活性

2-叔丁基-4-氯-5-羟基-哒嗪-3(2H)-酮(3)与相应的N-烷基或N,N-二烷基氯乙酰胺(4a-4l)反应,合成了2-叔丁基-5-[(N-烷基或N,N-二烷基乙酰胺)氧基]-4-氯-哒嗪-3(2H)-酮(1a-1l),生物活性测定结果表明部分化合物(1a-1l)具有杀虫活性。     

Synthesis and biological activity of some gossypol derivatives

Translated from Khimiya Prirodnykh Soedinenii, No. 1, pp. 44–49, January–February, 1995. Original article submitted October 17, 1994.     

Synthesis and biological activity of some fluorinated arylhydrazotriazoles

Potential biologically active derivatives of arylhydrazotriazole (3a–l) were prepared by the condensation reaction of diazonium salts using various aromatic amines (1a–l) and 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl) ethanones (2). The synthesized products were obtained in 75–85% yield. All the synthesized products were having good-excellent antifungal activity as compared with standard (Fluconazole and Ketoconazole) drugs.     

Synthesis and biological activity of triorganogermanium substituted heteropolytungstates

Four new compounds, [Me₄N]₄H₅[(RGe)₃(XW₉O_34−n)₂] (R = HOOCCH₂CH₂, HOOCCH₂(m-NO₂C₆H₄)CH, X = P, n = 0; X = Sb, n = 1) have been prepared from trichlorogermanium precursors and lacunary polyoxometallates ([PW₉O₃₄]⁹⁻ and [SbW₉O₃₃]⁹⁻). The products were characterized by means of elemental analysis, IR spectroscopy, ¹H NMR and ¹⁸³W NMR spectroscopy. ¹⁸³W NMR spectra of the complexes support the stoichiometry of the new heteropolyanions and the probable retention of the XW₉ units in water. The organogermanium substituted complexes showed promising activity against two human tumor cell lines (leucocythemia Hela cells and S180 cells) in vitro and [Me₄N]₄H₅[(HOOCCH₂CH₂Ge)₃(SbW₉O₃₃)₂] exhibited some certain antitumoral activity in vivo and can increase the immune ability of the spleen.