메뉴 건너뛰기




Volumn 17, Issue 5, 2007, Pages 1185-1188

Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2)

Author keywords

ADAMTS 5; Aggrecanase; Metalloprotease inhibitor; Thioxothiazolidinone; Zinc chelator

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; AGGRECANASE; AGGRECANASE 2; CHELATING AGENT; HYDANTOIN DERIVATIVE; HYDROXAMIC ACID DERIVATIVE; IMIDAZOLIDINE DERIVATIVE; METALLOPROTEINASE INHIBITOR; PROTEIN ADAMTS5; UNCLASSIFIED DRUG; ZINC;

EID: 33846919398     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.12.027     Document Type: Article
Times cited : (50)

References (16)
  • 6
    • 33846922459 scopus 로고    scopus 로고
    • note
    • ADAMTS-5 activity was determined using a Fluorescence Resonance Energy Transfer assay. Binding to target studies were conducted using a fluorescence polarization assay using a xanthene-ADAMTS-5 hydroxamic acid inhibitor.
  • 8
    • 33846896972 scopus 로고    scopus 로고
    • See the accompanying letter for the related 5-((1H-Pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one varient of this new class of ADAMTS-5 inhibitors: Gilbert, A. M.; Bursavich, M. G.; Lombardi, S.; Georgiadis, K. E.; Reifenberg, E.; Flannery, C. R; Morris, E. A. Bioorg. Med. Chem. Lett. 2007, doi:10.1016/j.bmcl.2006.12.020.
  • 13
    • 33846912647 scopus 로고    scopus 로고
    • note
    • All compounds were characterized by reversed phase-HPLC/MS spectroscopy. Selected compounds were also characterized by 1H NMR.
  • 14
    • 33846938692 scopus 로고    scopus 로고
    • note
    • Knoevenagel condensation afforded the Z isomer as shown. However 1H NMR spectroscopy studies demonstrated a time dependent Z to E isomeration in DMSO solution from the pure Z upto an 80:20 Z:E isomeric ratio.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.