66735-17-9Relevant academic research and scientific papers
Synthesis, characterization and antitumor potential of cinnamoyl urea derivatives
Chaudhary, Rakhi,Shuaib, Mohd,Hashim, S. Riaz,Mishra, Prem Shankar
, p. 410 - 414 (2016/01/20)
Cinnamoyl ureas have been identified as novel compounds with their various biological activities. Some novel cinnamoyl ureas were synthesized successfully by these substitutions, at the phenyl ring, at α,β -unsaturated carbon and the substitution at the c
The Development of a Stereoselective Method for the Synthesis of Tetrasubstituted Derivatives of α,β-Unsaturated Carboxylic Acids
Rzymkowski, Jan,Pi?tek, Anna
, p. 665 - 673 (2016/09/21)
Alkenes possessing four different carbon-linked substituents are the main structural motif of many biologically active compounds. The derivatives of (2E)-3-(3-methoxyphenyl)-2-methylpent-2-enoic acid ((E)-2c) are suitable precursors for the synthesis of Tapentadol, a novel centrally acting analgesic. It was found that the Ni-carbometallation reaction of disubstituted alkyne 8 with CO2and an Et2Zn allows for efficient and practical preparation of (E)-2c as a single (E)-regioisomer in 89% of isolated yield. The influence of the size of the aliphatic substituent of alkyne and the steric hindrance of the organozinc reagent on stereochemical course of the carbometallation reaction was evaluated. Finally, air-stable Ni(dme)Cl2was proposed as an alternative to widely used Ni(cod)2catalyst.
Indene-1-acetamide sPLA2 inhibitors
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, (2008/06/13)
Indene-1-acetamide compounds of the general formula (I) below; inhibit sPLA2mediated release of fatty acids and are useful for treatment of conditions such as septic shock.
Potent inhibitors of secretory phospholipase A2: Synthesis and inhibitory activities of indolizine and indene derivatives
Hagishita, Sanji,Yamada, Masaaki,Shirahase, Kazuhiro,Okada, Toshihiko,Murakami, Yasushi,Ito, Yuji,Matsuura, Takaharu,Wada, Masaaki,Kato, Toshiyuki,Ueno, Masahiko,Chikazawa, Yukiko,Yamada, Katsutoshi,Ono, Takashi,Teshirogi, Isao,Ohtani, Mitsuaki
, p. 3636 - 3658 (2007/10/03)
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 biologically active products. As human nonpancreatic sPLA2 is present in high levels in the blood of patients in several pathological conditions, the potent sPLA2 inhibitors have been suggested to be useful drugs. Here we 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.
