68535-56-8Relevant articles and documents
VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF
-
Paragraph 0247-0248, (2020/01/24)
Disclosed herein are small molecule Vascular Adhesion Protein- 1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.
3-Heterocycle-phenyl N-alkylcarbamates as FAAH inhibitors: Design, synthesis and 3D-QSAR studies
Kaesnaenen, Heikki,Myllymaeki, Mikko J.,Minkkilae, Anna,Kataja, Antti O.,Saario, Susanna M.,Nevalainen, Tapio,Koskinen, Ari M. P.,Poso, Antti
scheme or table, p. 213 - 231 (2010/11/18)
Carbamates are a well-established class of fatty acid amide hydrolase (FAAH) inhibitors. Here we describe the synthesis of meta-substituted phenolic N-alkyl/aryl carbamates and their in vitro FAAH inhibitory activities. The most potent compound, 3-(oxazol-2yl)phenyl cyclohexylcarbamate (2a), inhibited FAAH with a sub-nanomolar IC50 value (IC50=0.74 nM). Additionally, we developed and validated three-dimensional quantitative structure-activity relationships (QSAR) models of FAAH inhibition combining the newly disclosed carbamates with our previously published inhibitors to give a total set of 99 compounds. Prior to 3D-QSAR modeling, the degree of correlation between FAAH inhibition and in silico reactivity was also established. Both 3D-QSAR methods used, CoMSIA and GRID/GOLPE, produced statistically significant models with coefficient of correlation for external prediction (R2 PRED) values of 0.732 and 0.760, respectively. These models could be of high value in further FAAH inhibitor design.
Discovery of novel and potent aryl diamines as leukotriene A4 hydrolase inhibitors
Khim, Seock-Kyu,Bauman, John,Evans, Jarred,Freeman, Beverly,King, Beverly,Kirkland, Thomas,Kochanny, Monica,Lentz, Dao,Liang, Amy,Mendoza, Lisa,Phillips, Gary,Tseng, Jih-Lie,Wei, Robert G.,Ye, Hong,Yu, Limei,Parkinson, John,Guilford, William J.
scheme or table, p. 3895 - 3898 (2009/04/07)
The synthesis and biological evaluation of a series of aryl diamines as inhibitors of LTA4-h inhibitors are described. The optimization which led to the identification of the optimal para-substitution on the diphenyl ether moiety and diamine spacer is discussed. The resulting compounds such as 3l have excellent enzyme and cellular potency as well as desirable pharmacokinetic properties.
Diamine derivatives as inhibitors of leukotriene A4 hydrolase
-
Page/Page column 69, (2010/11/27)
This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9
BIARYL SUBSTITUTED HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION
-
Page/Page column 79, (2008/06/13)
The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders. The compounds have general formula Ψ: An example is
Di-heterocyclic compounds and their use as antiviral agents
-
, (2008/06/13)
Compounds of the formulas: STR1 wherein Het is an oxazole or oxazine moiety; X is O, S or SO, n is an integer from 3 to 9, Y is an aliphatic bridge; and the various R groups represent hydrogen or various substituents as described herein, are useful as antiviral agents, especially against picornaviruses. N-(Chloroalkyl)amide intermediates for the compounds of Formula I are also active as antiviral agents. Related compounds outside the scope of the above formulas are also disclosed.
Synthesis and analgesic-antiinflammatory activity of some 4- and 5-substituted heteroarylsalicylic acids
Jones,Fordice,Greenwald,Hannah,Jacobs,Ruyle,Walford,Shen
, p. 1100 - 1104 (2007/10/05)
We have made a series of 4- and 5-aryl- and 4- and 5-heteroarylsalicylic acid derivatives with the objective of reducing gastric irritation and increasing potency. Here we describe a series of 4- and 5-heterocyclic salicylic acids and their antiinflammatory-analgesic potencies measured in comparison to aspirin. An improvement of the therapeutic index over aspirin of 100 was achieved; however, the heterocyclic salicylic acids lacked antipyretic activity. Some physicochemical parameters which may bear on the antiinflammatory activity of these compounds are discussed.