Antimicrobial cationic polymers having one or two cationic polycarbonate chains were prepared by organocatalyzed ring opening polymerization. One antimicrobial cationic polymer has a polymer chain consisting essentially of cationic carbonate repeat units linked to one or two end groups. The end groups can comprise a covalently bound form of biologically active compound such as cholesterol. Other antimicrobial cationic polymers have a random copolycarbonate chain comprising a minor mole fraction of hydrophobic repeat units bearing a covalently bound form of a vitamin E and/or vitamin D2. The cationic polymers exhibit high activity and selectivity against Gram-negative and Gram-positive microbes and fungi.
The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.
本申请描述了对治疗、预防和/或改善疾病有用的有机化合物。
[EN] BRYOSTATIN ANALOGS AND USE THEREOF AS ANTIVIRAL AGENTS<br/>[FR] ANALOGUES DE LA BRYOSTATINE ET UTILISATION DE CEUX-CI EN TANT QU'AGENTS ANTIVIRAUX
申请人:UNIV UTAH RES FOUND
公开号:WO2016025363A1
公开(公告)日:2016-02-18
Described herein are tricyclic macrolactones. The macrolactones have a high binding affinity for PKC. The compounds described herein can be used in a number of therapeutic applications including the treatment or prevention of viral infection. Also described herein are methods for producing macrolactones. The methods permit the high-yield synthesis of macrolactones in a low number of steps and with a high degree of substitution and specificity.
Palladium-Catalyzed Arylation of Unactivated γ-Methylene C(sp<sup>3</sup>)H and δ-CH Bonds with an Oxazoline-Carboxylate Auxiliary
作者:Peng-Xiang Ling、Sheng-Long Fang、Xue-Song Yin、Kai Chen、Bo-Zheng Sun、Bing-Feng Shi
DOI:10.1002/chem.201502621
日期:2015.11.23
A palladium‐catalyzed arylation of unactivated γ‐methylene C(sp3)H and remote δ‐CHbonds by using an oxazoline‐carboxylate directinggroup has been developed. Arylation occurs with a broad substrate scope and high tolerance of functional groups (i.e., halogen, nitro, cyano, ether, trifluoromethyl, amine, and ester). The oxazoline‐type auxiliary can be removed under acidic conditions.
VITAMIN FUNCTIONALIZED GEL-FORMING BLOCK COPOLYMERS FOR BIOMEDICAL APPLICATIONS
申请人:INTERNATIONAL BUSINESS MACHINES CORPORATION
公开号:US20180117162A1
公开(公告)日:2018-05-03
Gel-forming block copolymers were prepared comprising i) a central hydrophilic block consisting essentially of a divalent poly(ethylene oxide) chain and ii) two peripheral monocarbonate or polycarbonate hydrophobic blocks linked to the central block by linking groups bearing one or more hydrogen bond forming *—N(H)—* groups. The hydrophobic blocks comprise one or more vitamin-bearing subunits. The gel-forming block copolymers can be used to prepare various biodegradable and/or biocompatible hydrogel and organogel drug compositions, in particular antimicrobial and/or anti-tumor drug compositions. The hydrogel compositions have utility in depot injections for drug delivery. The hydrogen bonding *—N(H)—* group(s) provide longer in vivo lifetime of the hydrogel before degradation and a more prolonged and controlled release rate of a hydrophobic drug compared to similar hydrogels prepared from poly(ethylene glycol).