1130-71-8Relevant academic research and scientific papers
Parallel synthesis and in vitro activity of novel anthranilic hydroxamate-based inhibitors of the prostaglandin H2 synthase peroxidase activity
Lee, Jean,Chubb, Anthony J.,Moman, Edelmiro,McLoughlin, Brian M.,Sharkey, Caroline T.,Kelly, John G.,Nolan, Kevin B.,Devocelle, Marc,Fitzgerald, Desmond J.
, p. 3678 - 3685 (2007/10/03)
Currently available non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin are directed at the cyclooxygenase (COX) site, but not the peroxidase (POX) activity of prostaglandin H2 synthase (PGHS). They are thus unable to inhibit the free-radical induced tissue injury associated with PGHS peroxidase activity, which can occur independently of the COX site. A lead compound, anthranilic hydroxamic acid (AHA) was found to have significant PGHS-POX inhibitory activity (IC50 = 72 μM). To define the critical parameters for PGHS-POX inhibition, we investigated 29 AHA derivatives, synthesised from their acid precursors, using solid phase synthesis. In vitro analysis demonstrated a ten-fold improvement in inhibition with 3,5-diiodoanthranilic hydroxamic acid (IC50 = 7 μM). The Royal Society of Chemistry 2005.
Facile Synthesis of Benzimidazol-2-one Derivatives by Modified Lossen Rearrangement
Eckstein, Zygmunt,Jadach, Tadeusz,Lipczynska-Kochany, Ewa
, p. 279 - 281 (2007/10/02)
A "formamide modification" has been applied to the Lossen rearrangement of several biologically important anthranilohydroxamic acids, some of them prepared for the first time.It has been found that a short heating at temperatures in the range 130-140 deg C converts these compounds into corresponding benzimidazol-2-ones with excellent yields.
