ChemInform Abstract: Synthesis and Immunomodulating Activity of Condensed N‐Aryl‐2‐cyano‐3‐ oxo‐3‐pyrazolylpropanamides.

Abstract

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On Dihydroorotate Dehydrogenases and Their Inhibitors and Uses

“…Recently, an attempt to replace the isoxazole ring with a 1,2,5-oxadiazole that led, by ring-opening, to the weak oxime-bearing inhibitor 37 pointed out the key role of the isoxazole ring . Quite large substituents, as seen in the structure of 38 , appeared to be also possible, since this unlikely analogue displayed an effect on an arthritis animal model …”

“…160 Quite large substituents, as seen in the structure of 38, appeared to be also possible, since this unlikely analogue displayed an effect on an arthritis animal model. 161 A structure-based study led to inhibitors of human DHODH related to teriflunomide (28), devoid of a nitrile function but retaining a ketone moiety as seen in compound 39 (Figure 5) or a bioisostere such as the phenol group of salicylate 40. 162 Interestingly, some structural similarities can been seen with a series of immunomodulators such as compound 41, 163 not to mention the ill-fated linomide (42) 164 or its backup laquinimod (43), 165,166 as well as heterocyclic-bearing analogues, 167 for which mechanisms of action have yet to be reported.…”