- A minimalistic approach to develop new anti-apicomplexa polyamines analogs
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The development of new chemical entities against the major diseases caused by parasites is highly desired. A library of thirty diamines analogs following a minimalist approach and supported by chemoinformatics tools have been prepared and evaluated agains
- Panozzo-Zénere, Esteban A.,Porta, Exequiel O.J.,Arrizabalaga, Gustavo,Fargnoli, Lucía,Khan, Shabana I.,Tekwani, Babu L.,Labadie, Guillermo R.
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p. 866 - 880
(2017/12/13)
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- Synthesis and investigation of new cyclic haloamidinium salts
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The presented work describes the synthesis of new six- and seven-membered haloamidinium salts and their reaction with different metals. The isolated metal complexes were tested in a catalytic reaction. Two different synthetic routes were applied to prepare five different salts. Chloroamidinium salts were very water-sensitive in comparison to their corresponding bromoamidinium salts. Hence, the preparation of the less sensitive bromoamidinium salts was higher prioritized. The formed salts were converted with metal sources to N-heterocyclic carbene (NHC) metal complexes through an oxidative insertion into the C-X bond. This type of formation is less examined for the synthesis of extended NHC metal complexes. Pd(PPh3)4 and cobalt powder were applied as metal sources, whereby two palladium complexes were isolated, characterized, and their crystal and molecular structures determined. The palladium complexes were investigated in the Suzuki-Miyaura reaction and showed promising catalytic activity.
- Rais, Eduard,Fl?rke, Ulrich,Wilhelm, René
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p. 667 - 676
(2016/07/06)
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- Photophysical properties of di-Schiff bases: Evaluating the synergistic effect of non-covalent interactions and alkyl spacers in enhanced emissions of solids
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Photophysical properties of di-Schiff base compounds in the solution and solid states are explored. The di-Schiff bases with alkyl spacers (ethyl, butyl and hexyl) showed enhanced light emitting properties in the solid state, while quenching was observed for di-Schiff bases with a hydrazine spacer. The photoluminescence spectra and the crystal structure were compared with bis-pyridyl-ethyl-di-imine and bis-pyridyl-butyl-di-imine. The crystal structure analysis of the compounds rationalizes the observed results. The concentration dependent 1H-NMR and NOESY spectra showed the aggregation behaviour of the compounds.
- Das, Moyna,Baig, Fayaz,Sarkar, Madhushree
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p. 57780 - 57792
(2016/07/06)
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- Synthesis and antikinetoplastid activity of a series of N,N×-substituted diamines
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A series of 25 N,N×-substituted diamines were prepared by controlled reductive amination of free aliphatic diamines with different substituted benzaldehydes. The library was screened in vitro for antiparasitic activity on the causative agents of human Afr
- Caminos, Andrea P.,Panozzo-Zenere, Esteban A.,Wilkinson, Shane R.,Tekwani, Babu L.,Labadie, Guillermo R.
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supporting information; experimental part
p. 1712 - 1715
(2012/04/10)
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- Design, synthesis and biological activity of peptidomimetic analogs of insect allatostatins
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Allatostatins (ASTs) comprise a family of insect neuropeptides isolated from cockroaches and found to inhibit the production of juvenile hormone (JH) by the corpora allata (CA). For this reason, the ASTs can be regarded as possible IGR candidates for pest control. Six peptidomimetic analogs according to the C-terminal pentapeptide of ASTs were prepared by solid-phase organic synthetic methods in an attempt to obtain new simple substitution agents. Assays of inhibition of JH biosynthesis in vitro by corpora allata from the cockroach Diploptera punctata showed that the activity of analog I (IC50: 0.09 μM) was more active than that of the C-terminal pentapeptide (Tyr-Xaa-Phe-Gly-Leu-NH2, IC50: 0.13 μM) it mimicked and the activity of the analog II (IC50: 0.13 μM) proved roughly equivalent to the C-terminal pentapeptide. The results indicate that a new simple mimicry for Tyr-Xaa-Phe-Gly has been discovered; analog I may be a novel compound candidate for potential IGRs. This study will be useful for the design of new AST analogs for insect management.
- Xie, Yong,Kai, Zhen Peng,Tobe, Stephen S.,Deng, Xi Le,Ling, Yun,Wu, Xiao Qin,Huang, Juan,Zhang, Li,Yang, Xin Ling
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experimental part
p. 581 - 586
(2012/01/13)
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- Double dearomatization of bis(diphenviphosphinamides) through anionic cyclization. A facile route of accessing multifunctional systems with antitumor properties
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(Chemical Equation Presented) The sequential one-pot double dearomatization of bis(N-benzyl-P,P-diphenylphosphinamides) via anionic cyclization is described for the first time. Protonation and alkylation of the dearomatized dianions provide bis(tetrahydro
- Ruiz-Gomez, Gloria,Iglesias, Maria Jose,Serrano-Ruiz, Manuel,Garcia-Granda, Santiago,Francesch, Andres,Lopez-Ortiz, Fernando,Cuevas, Carmen
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p. 3790 - 3799
(2008/02/02)
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- Synthesis and spectral data of new 1,2-bis-(2-hetaryl-4-oxothiazolidin-3- yl)ethanes and 1,4-bis-(2-hetaryl-4-oxothiazolidin-3-yl)butanes
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New α,ω-bis-(2-hetaryl-4-oxothiazolidin-3-yl)alkanes were prepared via a common two step procedure using N,N-bis-hetarylidenamines condensation with α-mercaptoacetic acid. The used bis-aldimines were obtained from reaction between ethylenediamine or putrescine and benzaldehyde or the isomeric pyridinecarboxyaldehydes. The bis-(2-phenyl-4-oxothiazolidin-3-yl) alkanes were prepared by one-pot three component reaction of diamine, aldehyde and α-mercaptoacetic acid under very mild conditions.
- Kouznetsov, Vladimir V.,Amado, Diego F.,Bahsas, Ali,Amaro-Luis, Juan
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p. 447 - 452
(2007/10/03)
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- Synthesis of imines, diimines and macrocyclic diimines as possible ligands, in aqueous solution
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Although it is recognized that the presence of water is disadvantageous for imine synthesis, we demonstrate that such synthesis can be effective in completely aqueous media, without any catalyst and under mild conditions. Thus, arylaryl, aryl-alkyl, alkyl-aryl and alkyl-alkyl monoimines as well as a large variety of diimines are obtained by direct condensation of the corresponding carbonyl compounds and amines, in water. The same process is used to synthesize macrocyclic diimines starting from methylene, ethylene, trimethylene and tetramethylene glycol bis(2-formylphenyl ether) and ethylene-, trimethylene- and tetramethylene-diamine, some of these macrocycles being known for their chelating properties.
- Simion, Alina,Simion, Cristian,Kanda, Tadeshige,Nagashima, Satoko,Mitoma, Yoshiharu,Yamada, Tomoko,Mimura, Keisuke,Tashiro, Masashi
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p. 2071 - 2078
(2007/10/03)
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- Syntheses of a Series of Linear Pentaamines with Three and Four Methylene Chain Intervals
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Ten kinds of linear pentaamines with various combinations of 3 or 4 methylene chain intervals were synthesized.The methods were tentatively classified into two, leading to symmetrical and unsymmetrical pentaamines, all of which were prepared by succesive alkylation of secondary amino derivatives of benzylamine with N-(3-bromopropyl or 4-bromobutyl)phthalimide in the presence of KF-Celite, coupled with the purification of the phthaloyl compounds by silica gel column chromatography.Protecting benzyl and phthaloyl groups were removed by usual methods.The carbon-13 nuclear magnetic resonance (13C-NMR) spectra ot the ten pentaamines were recorded in D2O as fully protonated forms, and a comparative analysis of their spectra allowed the complete assignment of all 13C chemical shifts.Keywords-polyamine; pentaamine; benzylamine; N-(3-bromopropyl)phthalimide; N-(4-bromobutyl)phthalimide; alkylation; potassium fluoride-Celite; 13C-NMR spectrum
- Niitsu, Masaru,Samejima, Keijiro
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p. 1032 - 1038
(2007/10/02)
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- Reagents for the Stepwise Functionalization of Spermidine, Homospermidine, and Bis(3-aminopropyl)amine
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A high-yield synthesis of reagents for the selective mono-, di-, or tri-N-functionalization of the polyamines spermidine, homospermidine, and norspermidine is described.The polyamine protecting groups utilized in these reagents are each easily removable u
- Bergeron, Raymond J.,Garlich, Joseph R.,Stolowich, Neal J.
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p. 2997 - 3001
(2007/10/02)
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- Studies on Thiazolidinones. Part-XIV: Synthesis of 3,3'-Bisthiazolidinones and 2,2-Disubstituted Thiazolidinones from Azomethines
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Several new 3,3'-bisthiazolidinones (III) and 2,2-disubstituted thiazolidinones (VIII) have been synthesised by the cycloadditive dehydration of thioglycolic acid to the azomethin derivatives (II) and (VII) prepared from the aliphatic diamines and heterocyclic monoamines respectively.The structure of the compounds have been confirmed from the spectral data and elemental analysis.The fungicidal and bactericidal activities of the compounds have also been evaluated.
- Sahu, J.,Sahu, T. K.,Naik, S. K.,Nayak, A.
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p. 861 - 863
(2007/10/02)
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