- NOVEL ARGINASE INHIBITORS
-
The present invention relates to novel arginase inhibitors of formula (I). These novel compounds are useful in the treatment of diseases that are associated with arginase activity, such as asthma, allergic rhinitis and COPD (chronic obstructive pulmonary disease).
- -
-
Page/Page column 19
(2020/12/30)
-
- BENZAMIDE DERIVATIVES
-
Benzamides of the formula I wherein R1 and R2 each independently is hydrogen, halogen, lower alkyl, lower alkoxy, cyano, trifluoromethyl, sulfamoyl, mono(lower alkyl)sulfamoyl or di(lower alkyl)sulfamoyl or R1 and R2 on adjacent carbon atoms together are
- -
-
-
- New analogues of N-(2-aminoethyl)-4-chlorobenzamide (Ro 16-6491). Some of the most potent monoamine oxidase-B inactivators
-
A series of halo- and nitro-substituted analogues of N-(2- aminoethyl)benzamide has been synthesized. All of the compounds are competitive, time-dependent inhibitors of monoamine oxidase-B (MAO-B), but upon dialysis complete return of enzyme activity is observed for all compounds. Therefore, these are mechanism-based reversible inhibitors of MAO- B. The relative potencies of the compounds are rationalized in terms of steric and hydrophobic effects.
- Annan,Silverman
-
p. 3968 - 3970
(2007/10/02)
-
- Synthesis and evaluation of iodinated benzamide derivatives as selective and reversible monoamine oxidase B inhibitors
-
A new series of iodinated analogues of N-(2-aminoethyl)benzamide was synthesized and evaluated for inhibitory potency and specificity toward monoamine oxidase type-B (MAO-B). Among them, N-(2-aminoethyl)-2-chloro-4-iodobenzamide hydrochloride (2d) showed high inhibitory potency and selectivity against MAO-B. The type of MAO-B inhihition by 2d was non-competitive and the inhibition constant (K(i)) was 0.80 μM. Strong and selective in vivo MAO-B inhibition by 2d was also confirmed. The brain MAO-B inhibition by 2d was reversible and the enzyme activity completely returned to the control value 24 h after administration. Compound 2d was, therefore, considered to be a candidate for advanced development as a radioiodinated ligand that may be useful for functional MAO-B studies in the living brain using single photon emission computer tomography.
- Ohmomo,Murakami,Hirata,Sugimoto,Magata,Miyahara,Tanaka,Yokoyama
-
p. 1789 - 1792
(2007/10/02)
-