27170-93-0Relevant academic research and scientific papers
N-(arylaminoethyl) benzoxazolone compound as well as preparation method and application thereof
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Paragraph 0082-0084, (2021/01/12)
The invention provides an N-(arylaminoethyl) benzoxazolone compound for crop bacteriostasis as well as a preparation method and an application thereof. The compound is prepared by reacting an arylamine compound with N-(2-bromoethyl) benzoxazolone, and the
Design, synthesis and biological evaluation of bivalent benzoxazolone and benzothiazolone ligands as potential anti-inflammatory/analgesic agents
Abdelazeem, Ahmed H.,Khan, Shabana I.,White, Stephen W.,Sufka, Kenneth J.,McCurdy, Christopher R.
, p. 3248 - 3259 (2015/08/03)
Abstract Benzoxazolone and benzothiazolone were used as template blocks to develop two series of dimers as anti-inflammatory and analgesic agents based on the concept of bivalent ligands. The first series (I) involved varying the carbon chain lengths extending from the piperazine core to the nitrogen atom of the dibenzo[d]oxazol-2(3H)-one or dibenzo[d]thiazol-2(3H)-one. The second series (II) was designed by changing the attachment point. All compounds were screened for their in vitro anti-inflammatory activity in terms of the inhibition of inducible nitric oxide synthase (iNOS) and nuclear factor kappa B (NF-κB). Seventeen compounds inhibited both targets. Eleven of them exhibited IC50 values below 3 μM while five compounds showed IC50 values of 1 μM or below. Most of the compounds were found to be devoid of cytotoxicity against mammalian kidney and solid tumors cell lines up to 25 μg/mL. In vivo anti-inflammatory and antinociceptive studies revealed that compounds 3j, 5t and 8b have significant anti-inflammatory and analgesic activity comparable to that of indomethacin and ketorolac, respectively.
HIGHLY SELECTIVE SIGMA RECEPTOR LIGANDS
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Page/Page column 22, (2009/04/25)
A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula ( I ) in which R1 can be a radical of an optionally substituted C-4 to C-7 N
Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity
Mésangeau, Christophe,Narayanan, Sanju,Green, Andrea M.,Shaikh, Jamaluddin,Kaushal, Nidhi,Viard, Eddy,Xu, Yan-Tong,Fishback, James A.,Poupaert, Jacques H.,Matsumoto, Rae R.,McCurdy, Christopher R.
, p. 1482 - 1486 (2008/09/20)
Cocaine's toxicity can be mitigated by blocking its interaction with sigma-1 receptors. The involvement of sigma-2 receptors remains unclear. To investigate their potential role, we have designed compounds through a convergent synthesis utilizing a highly selective sigma-1 ligand and elements of a selective sigma-2 ligand. Among the synthesized compounds was produced a subnanomolar sigma-2 ligand with an 11-fold preference over sigma-1 receptors. These compounds may be useful in developing effective pharmacotherapies for cocaine toxicity.
