321344-24-5Relevant academic research and scientific papers
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: Part 2
Nakao, Akira,Ohkawa, Nobuyuki,Nagasaki, Takayoshi,Kagari, Takashi,Doi, Hiromi,Shimozato, Takaichi,Ushiyama, Shigeru,Aoki, Kazumasa
, p. 2435 - 2437 (2010)
We previously reported a novel pyrrole derivative 1 which possesses a tetrahydropyridine group at the β-position with a proinflammatory cytokine TNFα production inhibitor. Herein, we report the synthesis and biological activity of N- and α-position substituted tetrahydropyridine derivatives. In this series, we found that compound 3o showed good inhibitory activity in vitro (inhibition of lipopolysaccharide (LPS)-induced TNFα production in human whole blood, IC50 = 0.44 μM) and compound 3i demonstrated potent inhibitory activity in vivo (inhibition of LPS-induced TNFα production in mice, ID50 = 1.42 mg/kg). Crown Copyright
Heteroaryl-substituted pyrrole derivates, their preparation and their therapeutic uses
-
Page 310, (2010/01/31)
Compounds of formula (I): [wherein: A is a pyrrole ring; R1 is an optionally substituted phenyl or naphthyl group; R2 is an optionally substituted pyridyl or pyrimidinyl group; R3 represents a group of the formula -X-R4, wherein X is a single bond or an alkenylene group, and R4 is an optionally substituted nitrogen-containing heterocyclyl group; selected from the group consisting of 8-azabicyclo[3.2.1]octenyl, 9-azabicyclo[3.3.1]nonenyl and quinuclidinenyl groups, PROVIDED THAT said substituents R1 and R3 are bonded to the two atoms of said pyrrole ring which are adjacent to the atom of the pyrrole ring to which said substituent R2 is bonded] have excellent inhibitory activity against the production of inflammatory cytokines.
Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses
-
, (2008/06/13)
Compounds of formula (I): [wherein: A is a pyrrole ring; R1 is an optionally substituted aryl or heteroaryl group; R2 is an optionally substituted nitrogen-containing heteroaryl group; R3 represents a group of the formula -X-R4, wherein X is a single bond or an optionally substituted alkylene, alkenylene or alkynylene group, and R4 is a substituted cycloalkyl group, a substituted aryl group, a substituted heterocyclyl group, an optionally substituted nitrogen-containing heterocyclyl group, a substituted heteroaryl group, an optionally substituted nitrogen-containing heteroaryl group, or -NRaRb, wherein each of Ra and Rb is a hydrogen atom or an alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl group; PROVIDED THAT said substituents R1 and R3 are bonded to the two atoms of said pyrrole ring which are adjacent to the atom of the pyrrole ring to which said substituent R2 is bonded] have excellent inhibitory activity against the production of inflammatory cytokines.
