20734-66-1Relevant articles and documents
Identification of novel matrix metalloproteinase inhibitors by screening of phenol fragments library
Rubino, Maria Teresa,Maggi, Dariana,Laghezza, Antonio,Loiodice, Fulvio,Tortorella, Paolo
experimental part, p. 557 - 563 (2012/06/30)
In the last 20 years, a great variety of synthetic, low molecular weight MMP inhibitors (MMPIs) have been synthesized and tested, although none has reached clinical utility. Exploration of novel ZBGs and development of non-hydroxamate MMPI has become a focus in current research. It's well-known that polyphenols can produce beneficial effects on human health by their antioxidant properties as well as they have the ability to block gelatinase activity. In this work we tested a series of selected phenols as MMP inhibitors. The most interesting hit (B6) shows sub-micromolar activity against MMP-2 (IC50 0.59 ± 0.05 μM, LE = 1.07) and a fairly good selectivity spectrum. A screening of selected phenols against four matrix metalloproteinases is reported. Eight phenols showed a very interesting activity and selective profile. The most interesting hit (B6) presents a sub-micromolar activity against MMP-2 (IC50 0.59±0.05μM). Copyright
Benzimidazole compounds as bradykinin antagonists
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, (2008/06/13)
PCT No. PCT/JP95/01478 Sec. 371 Date Feb. 3, 1997 Sec. 102(e) Date Feb. 3, 1997 PCT Filed Jul. 25, 1995 PCT Pub. No. WO96/04251 PCT Pub. Date Feb. 15, 1996This invention relates to a heterocyclic compound of the formula: wherein a group of the formula: is a group of the formula: etc., X is O, S or N-R5, R1 is lower alkyl, etc., R5 is hydrogen, lower alkyl, etc., R2 is hydrogen, halogen, lower alkyl, etc., R3 is halogen, lower alkyl, etc., R4 is amino optionally having suitable substituent(s), and A is lower alkylene, and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.