30070-99-6Relevant academic research and scientific papers
Towards the Development of Frustrated Lewis Pair (FLP) Catalyzed Hydrogenations of Tertiary and Secondary Carboxylic Amides
K?ring, Laura,Paradies, Jan,Sitte, Nikolai A.
, p. 1287 - 1300 (2022/01/20)
The development of the frustrated Lewis pair catalyzed hydrogenation of tertiary and secondary amides is reviewed. Detailed insight into our strategies in order to overcome challenges during the reaction development process is provided. Furthermore, the d
A minimalistic approach to develop new anti-apicomplexa polyamines analogs
Panozzo-Zénere, Esteban A.,Porta, Exequiel O.J.,Arrizabalaga, Gustavo,Fargnoli, Lucía,Khan, Shabana I.,Tekwani, Babu L.,Labadie, Guillermo R.
, p. 866 - 880 (2017/12/13)
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
MAIN CHAIN POLYAMINES
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Page/Page column 80, (2016/04/26)
Main chain polyamines comprise amine and ammonium groups along the polymer backbone. Main chain polyamines can be used as pharmaceutical agents and in pharmaceutical compositions. The main chain polyamines are particularly useful in the treatment or preve
Synthesis and evaluation of hexahydropyrimidines and diamines as novel hepatitis C virus inhibitors
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
, p. 315 - 325 (2013/11/19)
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.
Synthesis of an anion-binding amino acid
Chénard, Sylvain,Barberis, Claude,Otis, Fran?ois,Paquin, Jean-Fran?ois,Martel, Jonathan,Banville, Charles,Voyer, Normand
supporting information; experimental part, p. 409 - 411 (2012/02/02)
We achieved the synthesis of a derivative of phenylalanine with a diazamacrocycle on its side chain by macrocyclization of a dichloride on l-DOPA. We also report its incorporation into peptide structures by solid phase peptide synthesis which will lead to
Synthesis and antikinetoplastid activity of a series of N,N×-substituted diamines
Caminos, Andrea P.,Panozzo-Zenere, Esteban A.,Wilkinson, Shane R.,Tekwani, Babu L.,Labadie, Guillermo R.
supporting information; experimental part, p. 1712 - 1715 (2012/04/10)
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
Design, synthesis and biological activity of peptidomimetic analogs of insect allatostatins
Xie, Yong,Kai, Zhen Peng,Tobe, Stephen S.,Deng, Xi Le,Ling, Yun,Wu, Xiao Qin,Huang, Juan,Zhang, Li,Yang, Xin Ling
experimental part, p. 581 - 586 (2012/01/13)
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.
Synthesis and antitubercular activity of ferrocenyl diaminoalcohols and diamines
Andrianina Ralambomanana, Dimby,Razafimahefa-Ramilison, Dorothee,Rakotohova, Andry Clement,Maugein, Jeanne,Pelinski, Lydie
experimental part, p. 9546 - 9553 (2009/04/06)
A total of 21 ferrocenyl and benzyl diaminoalcohols and diamines were synthesized and evaluated against Mycobacterium tuberculosis H37Rv. Interestingly, ferrocenyl diamines exhibit better activities than ferrocenyl diaminoalcohols.
Discovery of new small molecules that influence neuroblast cell migration from the subventricular zone
Rolland, Amandine,Boquet, Isabelle,Norreel, Jean-Chretien,Moret, Vincent,Laras, Younes,Kraus, Jean-Louis
, p. 169 - 174 (2008/04/03)
Using SVZ (subventricular zone) tissue explants from one-day-old mice, we investigated the activity of new amino aromatic disulfide analogues and polyazamacrocycles on the migration of SVZ cells (neuroblasts). We found that among the tested analogues, non
Synthesis and antimycobacterial activity of ferrocenyl ethambutol analogues and ferrocenyl diamines
Razafimahefa, Dorothee,Ralambomanana, Dimby Andrianina,Hammouche, Lies,Pelinski, Lydie,Lauvagie, Sylvia,Bebear, Christiane,Brocard, Jacques,Maugein, Jeanne
, p. 2301 - 2303 (2007/10/03)
A new series of ferrocenyl diamino alcohols and diamines were synthesized and their inhibitory potencies were probed with Mycobacterium tuberculosis. Interestingly, ferrocenyl diamines 6a and b display significant activities against M. tuberculosis H37Rv.
