在这项研究中,合成了一系列新颖的棉酚衍生物,并在体外对其抗HIV-1和抗H 5 N 1活性进行了筛选。用某些氨基酸取代棉酚的醛基,不仅可以降低细胞毒性,而且还可以增强对HIV-1和H 5 N 1的活性。与其他棉酚衍生物相比,化合物13 – 17对HIV-1和H 5 N 1的活性更强。同时,这些化合物还对H 5 N 1表现出更强的活性。比1-金刚烷胺。棉酚衍生物中缺少COONa基团会导致抗HIV-1活性的丧失,这表明该基团可能在介导抗病毒活性中起重要作用。添加时间分析表明,化合物13 – 17具有与T20相似的抗HIV-1作用机理。分子建模分析表明,化合物13 - 17可能适合的gp41的疏水口袋内通过氢键网络,疏水性接触性强的静电相互作用。
A Practical Synthesis of ω-Aminoalkanoic Acid Derivatives from Cycloalkanones
作者:Koc-Kan Ho、Doris C. O'Toole、Douglas M. Achan、Kitae T. Lim、Jeffery B. Press、Andrea Leone-Bay
DOI:10.1080/00397919608004580
日期:1996.7
A practical synthetic route to N-Boc protected or Boc-amino acid coupled omega-aminoalkanoic acids is reported and exemplified by the preparation of 8-(t-butoxycarbonylamino)caprylic acid 2 and (N-t-butoxycarbonylphenylalanyl)-8-aminocaprylic acid 3. The sequence does not involve column chromatography, hydrogenation, azide or bromine related rearrangements, and therefore is amenable to scale-up. Homologues of the omega-aminoalkanoic acid derivatives may also be prepared by using different cycloalkanones.
AMINE COMPOUNDS AND THEIR USE AS ZERO OR LOW VOC NEUTRALIZERS
申请人:ANGUS Chemical Company
公开号:EP2935477A1
公开(公告)日:2015-10-28
US6084112A
申请人:——
公开号:US6084112A
公开(公告)日:2000-07-04
[EN] METHOD FOR PREPARING omega -AMINOALKANOIC ACID DERIVATIVES FROM CYCLOALKANONES<br/>[FR] PROCEDE POUR PREPARER DES DERIVES D'ACIDES omega -AMINOALCANOIQUES A PARTIR DE CYCLOALCANONES
申请人:EMISPHERE TECHNOLOGIES, INC.
公开号:WO1997010197A1
公开(公告)日:1997-03-20
(EN) A convenient synthetic route to $g(v)-aminoalkanoic acids, $i(N)-Boc protected $g(v)-aminoalkanoic acids and Boc-amino acid coupled $g(v)-aminoalkanoic acids is disclosed. The method provides high purity compounds that generally do not require further purification.(FR) L'invention concerne un procédé de synthèse commode pour obtenir des acides $g(v)-aminoalcanoïques, des acides $g(v)-aminoalcanoïques protégées au niveau de l'azote par un groupe BOC et des acides $g(v)-aminoalcanoïques couplés à des acides aminés protégés par un groupe BOC. Le procédé fournit des composés très purs, ne nécessitant pas, généralement, de purification subséquente.
[EN] AMINE COMPOUNDS AND THEIR USE AS ZERO OR LOW VOC NEUTRALIZERS<br/>[FR] COMPOSÉS AMINE ET LEUR UTILISATION COMME AGENTS DE NEUTRALISATION À TENEUR NULLE OU FAIBLE EN COMPOSÉ ORGANIQUE VOLATIL (COV)
申请人:ANGUS CHEMICAL
公开号:WO2014099213A1
公开(公告)日:2014-06-26
Provided are compounds for use as neutralizing agents in aqueous formulations. The compounds are of the formula I: [Formula should be inserted here] wherein R, R', X, and M+ are as described herein.