| Identification | Back Directory | [Name]
5-[(4-dimethylamino-3,5-dimethoxy-phenyl)methyl]pyrimidine-2,4-diamine | [CAS]
56066-63-8 | [Synonyms]
aditoprim
5-(4-(dimethylamino)-3,5-dimethoxybenzyl)pyrimidine-2,4-diamine
5-[[4-(Dimethylamino)-3,5-dimethoxyphenyl]methyl]-2,4-pyridinediamine
5-[(4-dimethylamino-3,5-dimethoxy-phenyl)methyl]pyrimidine-2,4-diamine
2,4-Pyrimidinediamine, 5-[[4-(dimethylamino)-3,5-dimethoxyphenyl]methyl]- | [Molecular Formula]
C15H21N5O2 | [MDL Number]
MFCD00864989 | [MOL File]
56066-63-8.mol | [Molecular Weight]
303.36 |
| Chemical Properties | Back Directory | [Boiling point ]
503.9±60.0 °C(Predicted) | [density ]
1.233±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
7.08±0.10(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics[1][2][3]. | [in vivo]
Aditoprime (Aditoprim) has longer elimination half-lives (3.3~14.8?h) and higher distribution volumes (4.6~10.4?L/kg) than those of Trimethoprim (TMP) in pig, calf, monkey, sheep and some other animal species, and a similar pattern is observed for Aditoprime where the distribution volume is about four times higher than that of TMP[1].
Aditoprime (10?-40 mg/kg; b.w.; intramuscularly) shows efficacy in infected swine (swine streptococcosis)[1]. | [References]
[1] Then RL, et al. Properties of aditoprim, a new antibacterial dihydrofolate reductase inhibitor. Zentralbl Veterinarmed B. 1988;35(2):114-120. DOI:10.1111/j.1439-0450.1988.tb00476.x
[2] Cheng G, et al. The antibacterial activities of aditoprim and its efficacy in the treatment of swine streptococcosis. Sci Rep. 2017;7:41370. Published 2017 Feb 1. DOI:10.1038/srep41370
[3] Wang X, et al. Two-generation reproduction and teratology studies of feeding aditoprim in Wistar rats. J Appl Toxicol. 2015;35(12):1531-1538. DOI:10.1002/jat.3121 |
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