- METHODS FOR PRODUCING (6S,15S)-3,8,13,18-TETRAAZAICOSANE-6,15-DIOL
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The present invention provides methods of synthesizing (6S,15S)-3,8,13,18-tetraazaicosane-6,15-diol and salts thereof.
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Page/Page column 6-7
(2019/08/26)
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- 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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- Synthesis and evaluation of hexahydropyrimidines and diamines as novel hepatitis C virus inhibitors
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In order to identify novel anti-hepatitis C virus (HCV) agents we devised cell-based strategies and screened phenotypically small molecule chemical libraries with infectious HCV particles, and identified a hit compound (1) containing a hexahydropyrimidine (HHP) core. During our cell-based SAR study, we observed a conversion of HHP 1 into a linear diamine (6), which is the active component in inhibiting HCV and exhibited comparable antiviral activity to the cyclic HHP 1. In addition, we engaged into the biological characterization of HHP and demonstrated that HHP does not interfere with HCV RNA replication, but with entry and release of viral particles. Here we report the results of the preliminary SAR and mechanism of action studies with HHP.
- Hwang, Jong Yeon,Kim, Hee-Young,Jo, Suyeon,Park, Eunjung,Choi, Jihyun,Kong, Sunju,Park, Dong-Sik,Heo, Ja Myung,Lee, Jong Seok,Ko, Yoonae,Choi, Inhee,Cechetto, Jonathan,Kim, Jaeseung,Lee, Jinhwa,No, Zaesung,Windisch, Marc Peter
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p. 315 - 325
(2013/11/19)
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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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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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p. 581 - 586
(2012/01/13)
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- MODULATORS OF PHARMACOKINETIC PROPERTIES OF THERAPEUTICS
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The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.
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Page/Page column 294
(2008/06/13)
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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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- 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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