The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1,5-Dibromopentane( cas:111-24-0 ) is researched.Computed Properties of C5H10Br2.Liang, Yan; He, Dian; Zhou, Deshun; Li, Junshuai; Tang, Lei; Wang, Zhen published the article 《Synthesis, Antibacterial and Pharmacokinetic Evaluation of Novel Derivatives of Harmine N9-Cinnamic Acid》 about this compound( cas:111-24-0 ) in Molecules. Keywords: harmine cinnamic acid derivative antibacterial pharmacokinetic evaluation; antibacterial activity; harmine; pharmacokinetics; synthesis. Let’s learn more about this compound (cas:111-24-0).
A series of 16 new derivatives of harmine N9-Cinnamic acid were synthesized and fully characterized using NMR and MS. The in vitro antibacterial evaluation revealed that most of the synthesized harmine derivatives displayed better antibacterial activities against Gram-pos. strains (S. aureus, S. albus and MRSA) than Gram-neg. strains (E. coli and PA). In particular, compound 3c showed the strongest bactericidal activity with a min. inhibitory concentration of 13.67 μg/mL. MTT assay showed that compound 3c displayed weaker cytotoxicity than harmine with IC50 of 340.30, 94.86 and 161.67 μmol/L against WI-38, MCF-7 and HepG2 cell lines, resp. The pharmacokinetic study revealed that the distribution and elimination of 3c in vivo were rapid in rats with an oral bioavailability of 6.9%.
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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis