Pyridinium N-(2′-Azinyl)Aminides: Regioselective Synthesis of 2-Alkylaminoazines
摘要:
The regioselective alkylation of pyridinium-N-(2'-azinil)aminides with alkyl halides under mild conditions is described. The alkylation, combined with a reduction of the N-N bond, allows an easy preparation of 2-alkylaminoazines. (C) 2000 Elsevier Science Ltd. AU rights reserved.
ENHANCEMENT OF TIGECYCLINE POTENCY USING EFFLUX PUMP INHIBITORS
申请人:Glinka Tomasz
公开号:US20080076741A1
公开(公告)日:2008-03-27
Disclosed herein are Efflux Pump Inhibitor (EPI) compounds that can be co-administered with antimicrobial agents for the treatment of infections caused by drug resistant pathogens. The EPI compounds are soft drugs which exhibit a reduced propensity for tissue accumulation. It is demonstrated that the EPIs can be used to increase the potency, decrease bacterial resistance and development of bacterial resistance, and increase killing effectivness of tigecycline. Also disclosed are methods of treatment and pharmaceutical compositions for co-administering tigecylcine with an EPI.
METHODS AND COMPOSITIONS OF TARGETED DRUG DEVELOPMENT
申请人:Errico Joseph P.
公开号:US20110301193A1
公开(公告)日:2011-12-08
Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.
Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.
Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.