| 摘要 |
N-Phenyl-oxalamide derivatives (I) and their pharmaceutically acceptable salts. N-Phenyl-oxalamide derivatives of formula (I) and their pharmaceutically acceptable salts are new. [Image] R1>heterocyclyl; R2>hydrogen, lower alkyl or alkoxy, halo, hydroxy or cyano; R3>, R5> and R6>hydrogen, lower alkyl or alkoxy, halo or cyano; R4>hydrogen, lower (cyclo)alkyl, aryl or heterocyclyl; and R7> and R8>hydrogen or lower alkyl; or R4> and R8> together : heterocyclyl. Independent claims are also included for the following: (1) method for preparing (I); (2) intermediates (IV), similar to (I) but with NR4>R8> replaced by hydroxy; and (3) pharmaceutical composition containing (I), a carrier, diluent or adjuvant, optionally also additional therapeutic agents. ACTIVITY : Immunosuppressant; antiviral; antibacterial; antiparasitic; anti-inflammatory; anti-asthma; antiproliferative; cardiovascular; antitumor. MECHANISM OF ACTION : Inhibition of inosine monophosphate dehydrogenase (IMPD), which catalyzes the rate-determining step in de novo synthesis of guanine nucleotides. The compound tert-butyl [3-[[[3-methoxy-4-(5-oxazolyl)anilino]oxalyl]amino]benzyl] carbamate had ID50 for inhibition of IMPD of 0.036 MicroM. |
