Structure activity relationship towards design of cryptosporidium specific thymidylate synthase inhibitors

Synthesis of azide congeners of preQ1 as potential substrates for tRNA guanine transglycosylase

“…While disappointed that our azide probes are not substrates for tRNA guanine transglycosylase, we feel that these can serve as valuable intermediates for click reactions with alkynes to provide a wide range of analogues incorporating substituted 1,2,3‐triazines as replacements for heterocycloalkyl or benzenoid moieties that are tethered to the 5‐alkyl‐2‐amino‐3,7‐dihydro‐4 H ‐pyrrolo[2,3‐ d ]pyrimidin‐4‐one scaffold. Potential applications to broad‐spectrum antiproliferative agents [ 19 ] or thymidylate synthase inhibitors [ 20 ] exemplify these possibilities.…”

Dihydrofolate reductase, thymidylate synthase, and serine hydroxy methyltransferase: successful targets against some infectious diseases

“…Hence, efforts are underway to find its potent and selective inhibitors. The selective inhibitor (2-amino-4-oxo-4,7-dihydro-pyrrolo[2,3-d]pyrimidin-methyl-phenyl- l -glutamic acid) for Ch TS was obtained, and X-ray structures with inhibitors were also resolved for human TS and Ch TS, which helped further in the selectivity of compounds [ 124 ]. In another study, a thiol-substituted 2-hydroxy-N-phenylbenzamide was found to show good activity against Ch DHFR-TS [ 22 ].…”