Potent Inhibitors of Secretory Phospholipase A2: Synthesis and Inhibitory Activities of Indolizine and Indene Derivatives was written by Hagishita, Sanji;Yamada, Masaaki;Shirahase, Kazuhiro;Okada, Toshihiko;Murakami, Yasushi;Ito, Yuji;Matsuura, Takaharu;Wada, Masaaki;Kato, Toshiyuki. And the article was included in Journal of Medicinal Chemistry in 1996.Category: pyridine-derivatives This article mentions the following:
Phospholipase A2 is an enzyme which hydrolyzes the sn-2 position of certain cellular phospholipids. The liberated lysophospholipid and arachidonic acid are precursors in the biosynthesis of various biol. active products. As human nonpancreatic secretory phospholipase A2 (sPLA2) is present in high levels in the blood of patients in several pathol. conditions, the potent sPLA2 inhibitors have been suggested to be useful drugs. Here the authors describe the synthesis, structure-activity relationship, and inhibitory activities of indolizine and indene derivatives 1-(Carbamoylmethyl)indolizine derivatives and 1-oxamoylindolizine derivatives exhibited very potent inhibitory activity. The former was unstable to air oxidation, but the latter exhibited an improvement both in stability and in potency. Some compounds approached the stoichiometric limit of the chromogenic assay. In the experiment, the researchers used many compounds, for example, 4-Methoxy-2-methylpyridine (cas: 24103-75-1Category: pyridine-derivatives).
4-Methoxy-2-methylpyridine (cas: 24103-75-1) belongs to pyridine derivatives. Pyridine has a conjugated system of six π electrons that are delocalized over the ring. The molecule is planar and, thus, follows the Hückel criteria for aromatic systems. One of the examples of pyridines is the well-known alkaloid lithoprimidine, which is an A3 adenosine receptor antagonist and N,N-dimethylaminopyridine (DMAP) analog, commonly used in organic synthesis.Category: pyridine-derivatives