Stereochemistry | ACHIRAL |
Molecular Formula | C15H21N5O2 |
Molecular Weight | 303.3595 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC(CC2=C(N)N=C(N)N=C2)=CC(OC)=C1N(C)C
InChI
InChIKey=QBQMXWZTRRWPGK-UHFFFAOYSA-N
InChI=1S/C15H21N5O2/c1-20(2)13-11(21-3)6-9(7-12(13)22-4)5-10-8-18-15(17)19-14(10)16/h6-8H,5H2,1-4H3,(H4,16,17,18,19)
Aditoprim is a long-acting, selective, reversible inhibitor of dihydrofolate reductase with application as a broad-spectrum antibacterial agent in animals. Aditoprim is low toxic and not mutagenic.Many gram-positive and gram-negative bacteria are highly susceptible or susceptible to Aditoprim, especially Salmonella and Streptococcus, while H. parasuis and Klebsiella were moderately susceptible to Aditoprim. Phase II clinical study of Aditoprim on therapeutic effect on swine streptococcosis has demonstrated that Aditoprim is as active as compound sulfadiazine, which provides reasonable theoretical foundation for the clinical application of Aditoprim.
Approval Year
PubMed
Patents
Sample Use Guides
To evaluate the reproductive toxicity and teratogenic potential of aditoprim, different concentrations of aditoprim were administered to Wistar rats by feeding diets containing 0, 20, 100 and 1000 mg kg(-1) , respectively.
Route of Administration:
Oral
Salmonella and 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 were highly susceptible to Aditoprim (MIC or MIC50 ≤ 4 ug/mL). H. parasuis from swine, S. aureus, Aeromonas punctate, Mycobacterium tuberculosis, and S. agalactiae from fishes, and Klebsiella from calves and sheep showed moderate susceptibility (MIC or MIC50 = 8~16 ug/mL), whereas E. coli, A. pleuropneumonia, Pasteurella, S. aureus, and C. perfringens from swine, S. aureus and C. perfringens from chickens, and S. aureus from calves were resistant to Aditoprim (MIC or MIC50 ≥ 32 ug/mL). The values of MBC/MIC were from 1 to 4 for Aditoprim against sensitive bacteria, which indicated that Aditoprim had a good bactericidal activity.