1771650-41-9
Chemical Structure
BRD7929
- CAS No.: 1771650-41-9
- Formula:C33H38N4O2
- Molecular Weight:522.68
InChIKey: VKRCTZCBMKVHCK-RTOKGZNSSA-N
SMILES: CN(C)C[C@@H]1[C@H](C2=CC=C(C=C2)C#CC3=CC=CC=C3)[C@@]4([H])N1CCCCN(C4)C(NC5=CC=C(C=C5)OC)=O
Biological Activity: BRD7929 is an orally active phenylalanyl-tRNA synthetase (PheRS) inhibitor and parasiticide, with an IC50 value of 0.023 μM against Plasmodium falciparum PheRS. BRD7929 inhibits the aminoacylation activity of the target enzyme, blocking protein synthesis, DNA replication and parasite nuclear division. BRD7929 clears the asexual blood stage, liver stage and mature gametocyte stage of malaria parasite species, and prevents parasite transmission to mosquitoes. BRD7929 shows moderate cytotoxicity against mammalian cells and inhibits hERG ion channels. BRD7929 achieves cure of malaria in animal models. BRD7929 can be used in research related to cryptosporidiosis and malaria[1][2][3].
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BRD7929 | BRD7929 is an orally active phenylalanyl-tRNA synthetase (PheRS) inhibitor and parasiticide, with an IC50 value of 0.023 μM against Plasmodium falciparum PheRS. BRD7929 inhibits the aminoacylation activity of the target enzyme, blocking protein synthesis, DNA replication and parasite nuclear division. BRD7929 clears the asexual blood stage, liver stage and mature gametocyte stage of malaria parasite species, and prevents parasite transmission to mosquitoes. BRD7929 shows moderate cytotoxicity against mammalian cells and inhibits hERG ion channels. BRD7929 achieves cure of malaria in animal models. BRD7929 can be used in research related to cryptosporidiosis and malaria. | |||||||||||||||||||||
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References
- [1]. Funkhouser-Jones LJ, et al. Defining Stage-Specific Activity of Potent New Inhibitors of Cryptosporidium parvum Growth . mBio. 2020 Mar 03;11(2):e00052-20.
- [2]. Kato, N., et al. Diversity-oriented synthesis yields novel multistage antimalarial inhibitors. Nature 538, 344–349 (2016).
- [3]. Vinayak S, et al. Bicyclic azetidines kill the diarrheal pathogen Cryptosporidium in mice by inhibiting parasite phenylalanyl-tRNA synthetase. Sci Transl Med. 2020 Sep 30;12(563):eaba8412. [Content Brief]
