Ontology highlight
ABSTRACT:
SUBMITTER: Sun Z
PROVIDER: S-EPMC4281095 | biostudies-literature | 2014 Dec
REPOSITORIES: biostudies-literature
Sun Zhuming Z Khan Jihan J Makowska-Grzyska Magdalena M Zhang Minjia M Cho Joon Hyung JH Suebsuwong Chalada C Vo Pascal P Gollapalli Deviprasad R DR Kim Youngchang Y Joachimiak Andrzej A Hedstrom Lizbeth L Cuny Gregory D GD
Journal of medicinal chemistry 20141204 24
Cryptosporidium inosine 5'-monophosphate dehydrogenase (CpIMPDH) has emerged as a therapeutic target for treating Cryptosporidium parasites because it catalyzes a critical step in guanine nucleotide biosynthesis. A 4-oxo-[1]benzopyrano[4,3-c]pyrazole derivative was identified as a moderately potent (IC50 = 1.5 μM) inhibitor of CpIMPDH. We report a SAR study for this compound series resulting in 8k (IC50 = 20 ± 4 nM). In addition, an X-ray crystal structure of CpIMPDH·IMP·8k is also presented. ...[more]