Design, synthesis and pharmacological evaluation of a series of 5-carbethoxy-4-chloro-6-(substituted amino)pyrimidines as potential analgesic and anti-flammatory agents with very low ulcerogenic potential.

A series of 5-carbethoxy-4-chloro-6-(substituted amino)pyrimidines was designed on the basis of its good 3-dimensional structural similarity with mefenamic acid (CAS 61-68-7), a well known anti-inflammatory drug. Synthesis of some 5-carbethoxy-4-chloro-6-(substitutedamino)pyrimidines has been achieved by cyclization of N-(cyanovinyl)formamidine intermediate in the presence of dry HCl. Target compounds were evaluated for their analgesic and anti-inflammatory potential by known experimental models. Some of the compounds emerged as more potent analgesic and anti-inflammatory agents than the standard drug diclofenac sodium (CAS 15307-79-6). A very low ulcer index was observed with the most potent compound.