16061-96-4Relevant articles and documents
A convenient practical synthesis of alkyl and aryl oxime esters
Santosh Kumar, S. Chandrappa,Vijendra Kumar, Nanjundaswamy,Srinivas, Pullabhatla,Bettadaiah, Bheemanakere Kempaiah
, p. 1847 - 1852 (2014/07/22)
A facile access to the synthesis of alkyl and aryl oxime esters of ketoximes and aldoximes in high yields (90-97%) is reported. The reactions were performed using N-[3-(methylamino)propyl]-N′-ethylcarbodiimide hydrochloride (EDCI) reagent in the presence of 4-(dimethylamino)pyridine (DMAP) as a catalyst at room temperature. The isolation and purification of products is very simple and in cases where product is solid, column chromatography is avoided. Georg Thieme Verlag Stuttgart New York.
Potent inhibitors of lipoprotein-associated phospholipase A2: Benzaldehyde O-heterocycle-4-carbonyloxime
Jeong, Hyung Jae,Park, Yong-Dae,Park, Ho-Yong,Jeong, Il Yun,Jeong, Tae-Sook,Lee, Woo Song
, p. 5576 - 5579 (2007/10/03)
A series of multi-substituted oximes were prepared and their potencies for inhibiting lipoprotein-associated phospholipase A2 (Lp-PLA2) activity were evaluated in vitro. Among them, compounds 3a, 3b, and 3m were identified to display a micromolar potency for inhibiting Lp-PLA2 in whole human plasma and isolated human LDL. Based on these results, structure-activity relationship was studied on modification of three parts of R1, R2, and R3 to identify a potent pharmacophore for Lp-PLA2. In an attempt to introduce various functional groups at R2 and R3, we discovered that replacement of less lipophilic groups led to an increase of inhibitory activity. Among the tested oxime derivatives, cyano- and morpholino-substituted analogue 4f at R2 and R3 had the highest potency with an IC50 value of 0.05 μM in whole human plasma.
(E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors
Jeong, Tae-Sook,Kim, Mi Jeong,Yu, Hana,Kim, Kyung Soon,Choi, Joong-Kwon,Kim, Sung-Soo,Lee, Woo Song
, p. 1525 - 1527 (2007/10/03)
A series of (E)-phenyl- and -heteroaryl-substituted O-benzoyl- (or acyl)oximes 3a-n were synthesized for evaluating their human lipoprotein-associated phospholiphase A2 (Lp-PLA2) inhibitory activities. The less lipophilic derivatives 3a-c showed the most potent in vitro inhibitory activity on human Lp-PLA2.
