332132-39-5
Chemical Structure
E5700
- CAS No.: 332132-39-5
- Formula:C26H31N3O3
- Molecular Weight:433.54
IUPAC Name: (R)-3-((2-benzyl-6-((3R,4S)-3-hydroxy-4-methoxypyrrolidin-1-yl)pyridin-3-yl)ethynyl)quinuclidin-3-ol
InChIKey: NDEOTZXSBKCQLS-RMTZWNOUSA-N
SMILES: O[C@@]1(CN2CCC1CC2)C#CC3=CC=C(N=C3CC4=CC=CC=C4)N5C[C@H]([C@H](C5)OC)O
Biological Activity: E5700 is an orally active squalene synthase inhibitor, antimalarial agent and antifungal agent with an IC50 of 0.49 nM (without PPi) against squalene synthase from T. cruzi epimastigotes. E5700 shows antiparasitic activities against Trypanosoma cruzi. E5700 inhibits the growth and alters the lipid prolife and the ultrastructure of a multiple agent-resistant C. tropicalis strain. E5700 is a potent and selective inhibitor of the growth of Leishmania amazonensis[1][2][3].
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E5700 | E5700 is an orally active squalene synthase inhibitor, antimalarial agent and antifungal agent with an IC50 of 0.49 nM (without PPi) against squalene synthase from T. cruzi epimastigotes. E5700 shows antiparasitic activities against Trypanosoma cruzi. E5700 inhibits the growth and alters the lipid prolife and the ultrastructure of a multiple agent-resistant C. tropicalis strain. E5700 is a potent and selective inhibitor of the growth of Leishmania amazonensis. | |||||||||||||||||||||
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- [1]. Urbina JA, et al. In vitro and in vivo activities of E5700 and ER-119884, two novel orally active squalene synthase inhibitors, against Trypanosoma cruzi. Antimicrob Agents Chemother. 2004 Jul;48(7):2379-87. [Content Brief]
- [2]. Ishida K, et al. Two squalene synthase inhibitors, E5700 and ER-119884, interfere with cellular proliferation and induce ultrastructural and lipid profile alterations in a Candida tropicalis strain resistant to fluconazole, itraconazole, and amphotericin B. J Infect Chemother. 2011 Aug;17(4):563-70. [Content Brief]
- [3]. Fernandes Rodrigues JC, et al. In vitro activities of ER-119884 and E5700, two potent squalene synthase inhibitors, against Leishmania amazonensis: antiproliferative, biochemical, and ultrastructural effects. Antimicrob Agents Chemother. 2008 Nov;52(11):4098-114. [Content Brief]
Keywords
