56066-63-8

56066-63-8 structure

Name: Aditoprime
Chemical Name: 5-[[4-(dimethylamino)-3,5-dimethoxyphenyl]methyl]pyrimidine-2,4-diamine
CAS Number: 56066-63-8
Molecular Formula: C₁₅H₂₁N₅O₂
Molecular Weight: 303.36000
Catalog: Signaling Pathways Anti-infection Bacterial
Create Date: 2018-06-10 01:40:10
Modify Date: 2024-01-06 19:05:59
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].

Name	5-[[4-(dimethylamino)-3,5-dimethoxyphenyl]methyl]pyrimidine-2,4-diamine
Synonyms	Aditoprima Aditoprim Aditoprime

Description	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].
Related Catalog	Research Areas >> Infection Signaling Pathways >> Cell Cycle/DNA Damage >> Antifolate Signaling Pathways >> Anti-infection >> Bacterial
In Vitro	Aditoprime has the same antibacterial spectrum as TMP. Salmonellaand Streptococcus from swine, E. coli and Salmonella from chickens, E. coli, Streptococcus, Mannheimia, and Pasteurella from calves, Streptococcus and Mannheimia from sheep, and E. coli, Flavobacterium columnare, A. baumannii and Y. ruckeri from fishes are highly susceptible to Aditoprime (MIC or MIC50 ≤ 4 μg/mL)[1].
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. [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. [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.

Density	1.233g/cm3
Boiling Point	503.9ºC at 760 mmHg
Molecular Formula	C₁₅H₂₁N₅O₂
Molecular Weight	303.36000
Flash Point	258.5ºC
Exact Mass	303.17000
PSA	100.98000
LogP	1.17520
Index of Refraction	1.633

Hazard Codes	Xi

56066-62-7

124-46-9

56066-63-8

Literature: Hoffmann-La Roche Inc. Patent: US4515948 A1, 1985 ;

Precursor 2
56066-62-7 124-46-9
DownStream 0

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134104-43-1	131615-57-1
1013805-59-8	6906-52-1
930439-75-1	923150-38-3
16350-97-3	1018584-77-4