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Literature summary for 1.1.1.205 extracted from

  • Gorla, S.K.; Kavitha, M.; Zhang, M.; Chin, J.E.; Liu, X.; Striepen, B.; Makowska-Grzyska, M.; Kim, Y.; Joachimiak, A.; Hedstrom, L.; Cuny, G.D.
    Optimization of benzoxazole-based inhibitors of Cryptosporidium parvum inosine 5-monophosphate dehydrogenase (2013), J. Med. Chem., 56, 4028-4043.
    View publication on PubMedView publication on EuropePMC
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Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Cryptosporidium parvum

Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-[(1-naphthyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide competitive versus NAD+ Cryptosporidium parvum
(2S)-2-[(3,4-dichlorophenyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide competitive versus NAD+, displays excellent IMPDH inhibitory activity and moderate stability in mouse liver microsomes Cryptosporidium parvum
2-[(3,4-dichlorophenyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide racemic variant, competitive versus NAD+. Compound displays good antiparasitic activity in a Toxoplasma gondii strain that relies on Cryptosporidium parvum IMPDH, EC50 20 nM. No toxicity is observed against four mammalian cells lines Cryptosporidium parvum

Organism

Organism UniProt Comment Textmining
Cryptosporidium parvum Q8T6T2
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000005
-
 pH 8.0, 25°C Cryptosporidium parvum (2S)-2-[(3,4-dichlorophenyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
0.000002
-
 pH 8.0, 25°C Cryptosporidium parvum 2-[(3,4-dichlorophenyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
0.000014
-
 pH 8.0, 25°C Cryptosporidium parvum (2S)-2-[(1-naphthyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide