Discovery of Inhibitors of Burkholderia pseudomallei Methionine Aminopeptidase with Antibacterial Activity
摘要:
Evaluation of a series of MetAP inhibitors in an in vitro enzyme activity assay led to the first identification of potent molecules that show significant growth inhibition against Burkholderia pseudomallei. Nitroxoline analogues show excellent inhibition potency in the BpMetAP1 enzyme activity assay with the lowest IC50 of 30 nM and inhibit the growth of B. pseudomallei and B. thailandensis at concentrations >= 31 mu M.
Labeled macrophage scavenger receptor antagonists for imaging cardiovascular diseases
申请人:Wilson Ian
公开号:US20060239915A1
公开(公告)日:2006-10-26
The present invention is in the field of diagnostic imaging. In one aspect, the invention relates to novel imaging agents comprising synthetic macrophage scavenger receptor A antagonists, said imaging agents being useful in the diagnostic imaging of cardiovascular disease. Also claimed in the present invention is a pharmaceutical composition comprising the novel imaging agents of the invention, said pharmaceutical composition being useful for the diagnostic imaging of cardiovascular disease in humans. Another aspect of the present invention is a kit useful in the preparation of the pharmaceutical composition of the invention. Furthermore, the use of the imaging agent of the invention for the diagnostic imaging of cardiovascular disease is also claimed.
Methods of Treating an Overweight or Obese Subject
申请人:Vath James E.
公开号:US20120010290A1
公开(公告)日:2012-01-12
The invention herein generally relates to methods of treating a subject having an overweight or obese condition, and overweight- or obesity-related conditions. In one embodiment, the invention herein provides a method of treating a subject having overweight or obese condition involving administering to the subject in need thereof, an amount of a pharmaceutical composition including a MetAP-2 inhibitory compound, or a salt, ester, or prodrug thereof, effective to result in weight loss in the subject.