Pafuramidine
Modify Date: 2024-01-05 08:13:48
Pafuramidine structure
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Common Name | Pafuramidine | ||
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| CAS Number | 186953-56-0 | Molecular Weight | 364.39800 | |
| Density | 1.25 | Boiling Point | N/A | |
| Molecular Formula | C20H20N4O3 | Melting Point | 192.5-193ºC | |
| MSDS | N/A | Flash Point | N/A | |
Use of PafuramidinePafuramidine (DB289) is an orally bioavailable prodrug of furamidine, which has clinical activity against Pneumocystis pneumonia.IC50 Value: 4.5 nM (In vitro inhibitory activity against Trypanosoma brucei rhodesiense) [4]Target: AntiparasiticDB289 (pafuramidine maleate; 2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) is a prodrug of DB75 (furamidine dihydrochloride; 2,5-bis(4-guanylphenyl)furan dihydrochloride), an aromatic dication related to pentamidine that has demonstrated good efficacy against African trypanosomiasis, Pneumocystis carinii pneumonia, and malaria, but lacks adequate oral availability. in vitro: The results of this investigation suggest that DB75 inhibits mitochondrial function. Yeast cells relying upon mitochondrial metabolism for energy production are especially sensitive to DB75 [1].in vivo: Clearance of DB289 approximated the liver plasma flow and its large volume of distribution was consistent with extensive tissue binding. Plasma protein binding of DB289 was 97 to 99% in four animal species and humans, but that of DB75 was noticeably less and more species- and concentration-dependent [2]. Despite excellent oral activity against early-stage sleeping sickness, oral administration of DB289 exhibited limited efficacy in mouse models of late-stage disease [3].Clinical trial: DB289, a novel orally active prodrug of DB75, is undergoing phase IIb clinical trials for early-stage human African trypanosomiasis, Pneumocystis jiroveci carinii pneumonia, and malaria [1]. |
| Name | N'-methoxy-4-[5-[4-[(Z)-N'-methoxycarbamimidoyl]phenyl]furan-2-yl]benzenecarboximidamide |
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| Synonym | More Synonyms |
| Description | Pafuramidine (DB289) is an orally bioavailable prodrug of furamidine, which has clinical activity against Pneumocystis pneumonia.IC50 Value: 4.5 nM (In vitro inhibitory activity against Trypanosoma brucei rhodesiense) [4]Target: AntiparasiticDB289 (pafuramidine maleate; 2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) is a prodrug of DB75 (furamidine dihydrochloride; 2,5-bis(4-guanylphenyl)furan dihydrochloride), an aromatic dication related to pentamidine that has demonstrated good efficacy against African trypanosomiasis, Pneumocystis carinii pneumonia, and malaria, but lacks adequate oral availability. in vitro: The results of this investigation suggest that DB75 inhibits mitochondrial function. Yeast cells relying upon mitochondrial metabolism for energy production are especially sensitive to DB75 [1].in vivo: Clearance of DB289 approximated the liver plasma flow and its large volume of distribution was consistent with extensive tissue binding. Plasma protein binding of DB289 was 97 to 99% in four animal species and humans, but that of DB75 was noticeably less and more species- and concentration-dependent [2]. Despite excellent oral activity against early-stage sleeping sickness, oral administration of DB289 exhibited limited efficacy in mouse models of late-stage disease [3].Clinical trial: DB289, a novel orally active prodrug of DB75, is undergoing phase IIb clinical trials for early-stage human African trypanosomiasis, Pneumocystis jiroveci carinii pneumonia, and malaria [1]. |
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| Related Catalog | |
| References |
[4]. In vitro inhibitory activity against Trypanosoma brucei rhodesiense - BioAssay Summary. |
| Density | 1.25 |
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| Melting Point | 192.5-193ºC |
| Molecular Formula | C20H20N4O3 |
| Molecular Weight | 364.39800 |
| Exact Mass | 364.15400 |
| PSA | 108.36000 |
| LogP | 4.54760 |
| Storage condition | 2-8℃ |
| UNII-H1VG379J2X |
| Pafuramidine |