162439-40-9Relevant academic research and scientific papers
The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors
Steinman, Douglas H.,Curtin, Michael L.,Garland, Robert B.,Davidsen, Steven K.,Heyman, H. Robin,Holms, James H.,Albert, Daniel H.,Magoc, Terry J.,Nagy, Ildiko B.,Marcotte, Patrick A.,Li, Junling,Morgan, Douglas W.,Hutchins, Charles,Summers, James B.
, p. 2087 - 2092 (2007/10/03)
A series of succinate-derived hydroxamic acids incorporating a macrocyclic ring were designed, synthesized, and evaluated as inhibitors of matrix metalloproteinases. The inhibitors were designed based on the published X-ray crystal structure of batimastat (1) complexed with human neutrophil collagenase (MMP-8). The synthesized compounds were shown to inhibit selected MMPs in vitro with low nanomolar potency.
HYDROXAMIC ACID AND CARBOXYLIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND USE THEREOF
-
, (2008/06/13)
This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.
Inhibition of matrix metalloproteinases by hydroxamates containing heteroatom-based modifications of the P1' group
Gowravaram,Tomczuk,Johnson,Delecki,Cook,Ghose,Mathiowetz,Spurlino,Rubin,Smith,Pulvino,Wahl
, p. 2570 - 2581 (2007/10/02)
In this study, structure-based drug design of matrix metalloproteinase inhibitors [human fibroblast collagenase (HFC), human fibroblast stromelysin (HFS), and human neutrophil collagenase (HNC)] was utilized in the development of potent hydroxamates which
