- Aqueous aza-michael reaction of conjugated alkenes: Toward spermine
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An aqueous aza-Michael reaction is efficiently achieved with excellent conversions without any additives. The method works very well on a molar scale with selectively for aliphatic amines. An intermediate for spermine is also made by this green process.
- Joshi, Jigar H.,Saiyed, Akeel S.,Bedekar, Ashutosh V.
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- Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities
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A series of alkylated (bis)urea and (bis)thiourea polyamine analogues were synthesized and screened for antimalarial activity against chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. All analogues showed growth inhibitory ac
- Verlinden, Bianca K.,Niemand, Jandeli,Snyman, Janette,Sharma, Shiv K.,Beattie, Ross J.,Woster, Patrick M.,Birkholtz, Lyn-Marie
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- Synthesis and biological evaluation of s-triazine substituted polyamines as potential new anti-Trypanosomal drugs
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The P2 transporter is a nucleoside transporter which is unique to the protozoan parasite Trypanosoma brucei, the causative organism of Human African Trypanosomasis. The transporter has been shown to bind some structural motifs not recognized by other tran
- Klenke,Stewart,Barrett,Brun,Gilbert
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Read Online
- Syntheses of a library of molecules on the marine natural product ianthelliformisamines platform and their biological evaluation
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Ianthelliformisamines A-C are a novel class of bromotyrosine-derived antibacterial agents isolated recently from the marine sponge Suberea ianthelliformis. We have synthesized ianthelliformisamines A-C straightforwardly by the condensation of (E)-3-(3,5-dibromo-4-methoxyphenyl)acrylic acid and the corresponding Boc-protected polyamine followed by Boc-deprotection with TFA. Further, using this reaction protocol, a library of their analogues (39 analogues) has been synthesized by employing 3-phenylacrylic acid derivatives and Boc-protected polyamine chains through various combinations of these two fragments differing in phenyl ring substitution, double bond geometry or chain length of the central spacer of the polyamine chain (shown in red color). All the synthesized compounds (ianthelliformisamines A-C and their analogues) were screened for antibacterial activity against both Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) strains. All synthetic analogues of ianthelliformisamine A showed bacterial growth inhibition against both strains (Escherichia coli and Staphylococcus aureus), having MIC values in the range of 117.8-0.10 μM, while none of the synthetic analogues of ianthelliformisamine C as well as the parent compound showed any detectable antibacterial activity. Interestingly, some of the synthetic analogues of ianthelliformisamines A and B exerted a bactericidal effect against both E. coli and S. aureus strains, decreasing viable bacterial count by 99% at concentrations as low as 2 × MIC. This journal is the Partner Organisations 2014.
- Khan, Faiz Ahmed,Ahmad, Saeed,Kodipelli, Naveena,Shivange, Gururaj,Anindya, Roy
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p. 3847 - 3865
(2014/06/09)
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- Polyamine functionalized carbon nanotubes: Synthesis, characterization, cytotoxicity and siRNA binding
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In this work we have synthesized a new series of cationic carbon nanotubes (CNTs) for siRNA binding. Both single- and multi-walled CNTs have been modified by addition or amidation reaction with short linear polyamine chains including putrescine, spermidin
- Singh, Prabhpreet,Samori, Cristian,Toma, Francesca Maria,Bussy, Cyrill,Nunes, Antonio,Al-Jamal, Khuloud T.,Menard-Moyon, Cecilia,Prato, Maurizio,Kostarelos, Kostas,Bianco, Alberto
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supporting information; experimental part
p. 4850 - 4860
(2011/10/09)
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- (Bis)urea and (Bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators
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The recently discovered enzyme lysine-specific demethylase 1 (LSD1) plays an important role in the epigenetic control of gene expression, and aberrant gene silencing secondary to LSD1 overexpression is thought to contribute to the development of cancer. W
- Sharma, Shiv K.,Wu, Yu,Steinbergs, Nora,Crowley, Michael L.,Hanson, Allison S.,Casero, Robert A.,Woster, Patrick M.
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scheme or table
p. 5197 - 5212
(2010/09/09)
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- ESTER-LINKED GEMINI SURFACTANT COMPOUNDS FOR USE IN GENE THERAPY
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This invention relates to newly identified ester-linked gemini surfactant compounds of formula (I), where Y is either H or (Aa)x where (Aa) is a basic amino acid and x is 1 to 6, to the use of such compounds and to their production. The invention also relates to the use of the ester-linked gemini surfactant compounds to facilitate the transfer of polynucleotide into cells.
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Page/Page column 9
(2008/06/13)
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- NEW ADJUVANT
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The present invention provides a novel adjuvant for polynucleotide vaccines, and in particular the present invention provides immunogenic compositions comprising a polynucleotide encoding an antigen capable of eliciting an immune response and an adjuvant
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Page/Page column 56; 57
(2010/11/25)
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- Solid-phase synthesis of diamine and polyamine amino acid derivatives as HIV-1 Tat-TAR binding inhibitors
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A series of diamine and polyamine derivatives, either free amines or salts (HCl or TFA), of aspartic and glutamic acid were prepared in excellent yields using Rink Amide solid-phase synthesis. The asparagine and glutamine derivatives were all evaluated for their ability to inhibit Tat-TAR binding using a FIGS cellular assay, with the polyamine derivatives exhibiting the most promising binding activity.
- Bueno, G. Jimenez,Klimkait,Gilbert,Simons
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- Sinulamide: An H,K-ATPase inhibitor from a soft coral Sinularia sp.
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Sinulamide (1), a new tetraprenylated spermine derivative, has been isolated from a soft coral Sinularia sp. as an H,K-ATPase inhibitor. The structure was assigned on the basis of spectroscopic data and confirmed by a total synthesis.
- Sata, Noriko U.,Sugano, Michihiro,Matsunaga, Shigeki,Fusetani, Nobuhiro
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p. 719 - 722
(2007/10/03)
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- Penaramides, which inhibit binding of ω-conotoxin GVIA to N-type Ca2+ channels, from the marine sponge Penares aff. Incruston s
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Penaramides which inhibit binding of ω-conotoxin GVIA to N-type Ca2+ channels have been isolated from the marine sponge Penares aff. incrustans and their structures determined by spectral and chemical methods to be bis-amides of an unusual poly
- Ushio-Sata, Noriko,Matsunaga, Shigeki,Fusetani, Nobuhiro,Honda, Kazuo,Yasumuro, Kenichi
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p. 225 - 228
(2007/10/02)
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- THE USE OF β-LACTAMS IN THE SYNTHESIS OF SPERMINE AND SPERMIDINE ALKALOIDS. TOTAL SYNTHESIS OF HOMALINE
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The optically active plant product homaline (6) has been synthesized in a convergent sequence starting with β-phenyl-β-alanine and putrescine (14).The key transformation in this sequence is the ring expansion by transamidation of a functionalized chiral β-lactam precursor.
- Wasserman, Harry H.,Berger, Gregory D.
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p. 2459 - 2464
(2007/10/02)
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- TRANSAMIDATION REACTIONS USING β-LACTAMS. THE SYNTHESIS OF HOMALINE
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The synthesis of the plant product, homaline, by a translactamization process involving the β-lactam, (-)-4-phenyl-2-azetidinone, is described.
- Wasserman, Harry H.,Berger, Gregory D.,Cho, Kathleen R.
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p. 465 - 468
(2007/10/02)
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