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A drug-like molecule could be considered as a congregation of small fragments which are chemically linked to each other and the biological effect of such molecule is due to the contribution of these small fragments working together. This molecular unit has been constructed gradually through a multi-step synthesis route. Assessment of the biological activity of all the intermediary compounds of a multi-step synthesis process helps to track down the emergence of biological activity alongside the synthesis process and the results provide valuable clues about the SAR of the compounds. Furthermore unanticipated findings may be encountered if such approach is exercised. A two-step synthesis route was employed to make a few 2-aminopyrimidines from their corresponding enamine precursors. Both aminopyrimidines and enamines were subjected to antiproliferative and antimicrobial tests. Hit compounds with acceptable activities were found in both aminopyrimidine and enamine series. With respect to antimicrobial activity, enamine series were found more promising. This experiment sets an example for the applicability of our new approach called "Synthesis route-based hit identification" as a tool in medicinal chemistry to increase the hit rate in drug discovery processes.

international journal of drug discovery

INTRODUCING "SYNTHESIS ROUTE-BASED HIT IDENTIFICATION APPROACH" AS A TOOL IN MEDICINAL CHEMISTRY AND ITS APPLICATION IN INVESTIGATING THE ANTIPROLIFERATIVE AND ANTIMICROBIAL EFFECTS OF 2- AMINOPYRIMIDINE DERIVATIVES