Synthesis and antibacterial activity of some 1-(2-propynyl) and 1-propadienyl derivatives of 1,4-dihydro-4-oxoquinoline-3-carboxylic acids and similar heterocycles

1991 ◽  
Vol 56 (2) ◽  
pp. 439-448 ◽  
Author(s):  
Stanislav Rádl ◽  
Lenka Kovářová ◽  
Jiří Holoubek

N-Alkylation of IIIa, IIIb, IIId - IIIf and 9-acridanone with 3-bromopropyne in dimethyl sulfoxide in the presence of potassium carbonate yielded N-(2-propynyl) derivatives IVa - IVe and VIa, respectively. Ethyl esters IVa, IVb, and IVe were hydrolyzed to IVf - IVh, respectively. Compounds IVf, IVg, IVctreated with bases yielded N-propadienyl derivatives Va - Vc. On the other hand 2-substituted compounds IVd and IVh did not change under the same conditions. Compound VIa treated with powdered potassium hydroxide in dimethyl sulfoxide at room temperature yielded N-(1-propynyl) derivative VII.

2013 ◽  
Vol 9 ◽  
pp. 8-14 ◽  
Author(s):  
Yan Sun ◽  
Jing Sun ◽  
Chao-Guo Yan

A fast and convenient protocol for the synthesis of novel spiro[dihydropyridine-oxindole] derivatives in satisfactory yields was developed by the three-component reactions of arylamine, isatin and cyclopentane-1,3-dione in acetic acid at room temperature. On the other hand the condensation of isatin with two equivalents of cyclopentane-1,3-dione gave 3,3-bis(2-hydroxy-5-oxo-cyclopent-1-enyl)oxindole in high yields. The reaction mechanism and substrate scope of this novel reaction is briefly discussed.


1868 ◽  
Vol 16 ◽  
pp. 254-258

The results of my researches on the chloroform-derivatives of the primary monamines, which, as I have shown, are isomeric with the nitriles, could not fail to direct my attention to allied groups of bodies, with the view of discovering similar isomerisms. In a note communicated to the Royal Society some months ago, I expressed the expectations which even then appeared to be justified in the following manner:—“In conclusion, I may be permitted to announce as everv probable the existence of a series of bodies isomeric with the sulphocyanides. Already M. Cloëz has shown that the action of chloride of cyanogen on ethylate of potassium gives rise to the formation of an ethylic cyanate possessing properties absolutely different from those belonging to the cyanate discovered by M. Wurtz. On comparing, on the other hand the properties of the methylic and ethylic sulphocyamdes with those of the sulphocyanides of allyl and phenyl, it can scarcely be doubted that we have here the representatives of two groups entirely different, and that the terms of the methyl- and ethyl-series which correspond to oil of mustard, and to the sulphocyanide of phenyl, still remain to be discovered. Experiments with which I am now engaged will show whether these bodies cannot be obtained by the action of the iodides of methyl and ethyl on sulphocyanide of silver."


Author(s):  
Shweta Singh ◽  
Sureshbabu Popuri ◽  
Qazi Mohammad Junaid ◽  
Sabiah Shahul Hameed ◽  
Jeyakumar Kandasamy

A wide range of N-tosyl α–ketoamides underwent transamidation with various alkyl amines in the absence of catalyst, base, or additives. On the other hand, transamidation in N-Boc α–ketoamides is achieved...


2013 ◽  
Vol 479-480 ◽  
pp. 855-860
Author(s):  
Chii Huei Yu

This paper uses the mathematical software Maple as the auxiliary tool to study the differential problem of four types of rational functions. We can obtain the closed forms of any order derivatives of these rational functions by using binomial theorem. On the other hand, we propose four examples to do calculation practically. The research methods adopted in this study involved finding solutions through manual calculations and verifying these solutions by using Maple. This type of research method not only allows the discovery of calculation errors, but also helps modify the original directions of thinking from manual and Maple calculations. For this reason, Maple provides insights and guidance regarding problem-solving methods.


Author(s):  
SUSI NOVARYATIIN

Objective: The objective of this research was to investigate the preliminary phytochemical screening and antibacterial activity of Bawang Dayak(Eleutherine sp.) and Hati Tanah (Angiopteris sp.) and their combination against Propionibacterium acnes.Methods: The extracts were used for phytochemical screening. Antibacterial activity was performed using disc diffusion technique, with twovariations of the concentration of 5% and 10% for each extracts, and combination of both extracts with three combinations: (1) 5%: 5%, (2) 5%: 10%, and (3) 10%: 5%.Results: Both extracts contained tannins, saponins, and steroids. The antibacterial activity against P. acnes showed that the inhibition zones ofBawang Dayak ethanol extract were 6.1±1.5 mm (5%) and 8.7±1.3 mm (10%). On the other hand, the inhibition zones of Hati Tanah ethanol extract were 4.0±1.6 mm (5%) and 9.2±2.5 mm (10%). The inhibition zones produced in combinations 1, 2, and 3 were 5.8±0.3 mm, 10.8±2.0 mm, and 15.5±2.8 mm, respectively.Conclusion: In this study showed the presence of tannins, saponins, and steroids that might be responsible for antibacterial activity in both extract. The best antibacterial activity was produced by combining the two extracts (combination 3).


1979 ◽  
Vol 34 (3) ◽  
pp. 507-510 ◽  
Author(s):  
Nazmi A. Kassab ◽  
Sanaa O. Abd Allah ◽  
Said A. Elbahaii

Abstract The 5-arylhydrazono derivatives of rhodanine and isorhodanine were subjected to the action of hydrazine hydrate to afford the arylhydrazonomercaptomethyl-triazolinones (3) and -triazolinthiones (3) respectively. Treatment of 1 with benzylamine afforded thioxalic acid dibenzylamide (5). On the other hand treatment of 2 with the same reagent afforded the corresponding benzylimino derivatives (6).Alkylation of 1 and 2 with ethyl bromoacetate and chloroacetamide yielded the corresponding S-alkyl derivatives (7) and (8), respectively.


2001 ◽  
Vol 05 (11) ◽  
pp. 767-781 ◽  
Author(s):  
VLADIMIR I. BREGADZE ◽  
IGOR B. SIVAEV ◽  
DETLEF GABEL ◽  
DIETER WÖHRLE

The synthesis of compounds containing polyhedral boron cages and porphyrin or phthalocyanine units connected covalently in one molecule is reviewed. The importance of these compounds arises, on the one hand, from the use of polyhedral boron derivatives in neutron capture therapy for cancer; on the other hand, porphyrins and phthalocyanines are known as photosensitizers in photodynamic tumor therapy. Current interest in the binding of polyhedral boron compounds to porphyrins and phthalocyanines is due to the observation that porphyrins and phthalocyanines show improved uptake and good persistence in tissues. Medical applications of compounds containing polyhedral boron cages and porphyrin or phthalocyanine units in one molecule are briefly discussed.


2005 ◽  
Vol 7 (3) ◽  
pp. 121-124 ◽  
Author(s):  
Antje Neubauer ◽  
Sukumaran Murali ◽  
Wolfgang Rettig

Derivatives of N-phenyl pyrrole with a para-donor substituent on the acceptor benzene ring are compared. It is shown that by a suitable increase of the donor strength of the pyrrolo group, CT fluorescence can be achieved even for donor-donor substituted benzenes. On the other hand, introducing fluoro substituents into the acceptor moiety strongly enhances the CT formation tendency, and several new compounds with CT fluorescence even in alkane solvents are presented.


Author(s):  
Tina Mosiakina

The article regards the phenomenon of the icon in the interpretation of Greek theologian and philosopher Christos Yannaras. His work Personality and Eros is taken as a basis, where the author describes this phenomenon, based on a thorough body of works of Orthodox thought.The icon is primarily considered not only as a model of reality, reflection or image of events and objects, or allegory-allegory; attention is focused on the icon as a category of cognition. The study traces the conditions of functioning of the iconological language, as well as its connection with apophatic and cataphatic theological thought. The specifics of the poetics of the iconological language are also revealed, aiming at both concealment and elucidation of the truth.An attempt is also made to transfer the theory of the icon to the anthropological plane, in accordance with the erotic gesture of self-denial. The focus is on the aesthetic component of the iconic perception not only of icons but also of other phenomena of art or the surrounding world. Thus, owing to the derivatives of the theory of the icon, the analysis of art in the anthropological plane is carried out.Possible types of reduction of the iconological language according to the function of the icon as a means of cognition are also revealed. In this regard, the significance of the so-called ‘theology of assimilation’ and its possible connection with the moralistic reduction in the interpretation of Ch. Yannaras are analyzed. On the other hand, aesthetic reduction is also described, which, in turn, has the ability to provoke iconoclastic resistance.Thus, the aim of the work is to study the phenomenon of the icon as a category of knowledge in the works of Ch. Yannaras, as well as to consider the icon and the iconological language in their connection with issues of the aesthetic and anthropological nature.


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