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5355-16-8

5355-16-8 structure
5355-16-8 structure
  • Name: Diaveridine
  • Chemical Name: diaveridine
  • CAS Number: 5355-16-8
  • Molecular Formula: C13H16N4O2
  • Molecular Weight: 260.292
  • Catalog: API Antiparasitic drug Anthelmintic
  • Create Date: 2018-02-03 08:00:00
  • Modify Date: 2024-01-02 19:18:47
  • Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
Name diaveridine
Synonyms Diaveridinum [INN-Latin]
Diaveridinum
DIAVERIDINE
2,4-Diamino-5-veratrylpyrimidine
5-(3,4-Dimethoxybenzyl)-2,4-pyrimidinediamine
2,4-diamino-5-(3,4-dimethoxy-benzyl)-pyrimidine
MFCD00057349
5-(3,4-dimethoxy-benzyl)-pyrimidine-2,4-diamine
5-[(3,4-dimethoxyphenyl)methyl]pyrimidine-2,4-diamine
Diaveridin
BW 49-210
Diaveridina
5-Veratryl-pyrimidin-2,4-diyldiamin
EINECS 226-333-3
Description Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
Related Catalog
Target

Ki: 11.5 nM (DHFR) [1] Bacterial[2]
In Vitro Diaveridine is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent[1]. Treatments with Diaveridine for 90 min have a strong bactericidal effect on S. typhimurium TA1535, and no bacterial growth is observed at 10μg/mL or more. Without metabolic activation, treatment with Diaveridine for 48 h, but not 24 h, causes a dose-dependent, significant increase in the frequency of aberrant metaphases. At 100 μg/mL, 60% of the metaphases contain chromosome aberrations[2].
In Vivo The sperm abnormality of the Diaveridine (DVD) treatment groups at all dose levels (Diaveridine, 128 to 512 mg/kg) shows no significant differences compare with the negative control group. There are no significant differences of micronucleus between the negative control group and the Diaveridine treatment groups (Diaveridine, 128 to 512 mg/kg). The chromosome aberration of the Diaveridine treatment groups at all dose levels and the negative control group are significantly lower than those in the positive control group treated with cyclophosphamide (P<0.05), indicating that Diaveridine at the doses studied does not cause abnormal chromosome aberration. The results demonstrate that the Diaveridine administration does not produce significant changes in the ratio of organ-to-body weight, compare with the negative control group in the end period of the study[3].
Cell Assay Cells are cultured at 37°C in a humidified atmosphere of 5% CO2 in air. The growth medium is Eagle’s MEM supplemented with 10% fetal bovine serum. In the experiment without metabolic activation, the cells are treated for 24 or 48 h continuously without a medium change. In the experiment with metabolic activation, the cells are pulse treated with test compounds (including Diaveridine) at varying doses for 6 h and incubated for 18 h in fresh culture medium. Breakage type chromatid aberrations, exchange type chromatid aberrations, breakage type chromosome aberrations, and exchange type chromosome aberrations are scored. Gaps are also counted. Mitotic index is determined from scoring 2000 cells[2].
Animal Admin 3]Fifty male ICR mice, weighing 25 to 35 g, are assigned to five groups randomly with 10 mice in each group. Mice in the experiment groups receive Diaveridine (DVD) via IG at ed 128 mg/kg (low doses), 256 mg/kg (medium doses), and 512 mg/kg (high doses) body weight for 5 consecutive days, respectively. Mice in negative and positive control groups receive IG 1% CMC-Na solvent and 40 mg/kg body weight of cyclophosphamide, respectively. The testing groups are administered 0.2 mL/10 g Diaveridine (mixed with 1% of CMC-Na, to obtain the concentration of 2 mg/mL.) body weight, once a day, for 5 days. The behavioral changes are recorded on the daily basis[3].
References

[1]. Sirichaiwat C et al. Target guided synthesis of 5-benzyl-2,4-diamonopyrimidines: their antimalarial activities and binding affinities to wild type and mutant dihydrofolate reductases from Plasmodium falciparum. J Med Chem 47:345-54 (2004).

[2]. Ono T, et al. The genotoxicity of diaveridine and trimethoprim. Environ Toxicol Pharmacol. 1997 Sep;3(4):297-306.

[3]. Wang J, et al. Acute, mutagenicity, teratogenicity and subchronic oral toxicity studies of diaveridine in rodents. Environ Toxicol Pharmacol. 2015 Sep;40(2):660-70.
Density 1.3±0.1 g/cm3
Boiling Point 506.1±60.0 °C at 760 mmHg
Melting Point 232 - 236ºC
Molecular Formula C13H16N4O2
Molecular Weight 260.292
Flash Point 259.9±32.9 °C
Exact Mass 260.127319
PSA 96.28000
LogP 1.09
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.626
Storage condition 2-8°C

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UV8142000
CHEMICAL NAME :
2,4-Pyrimidinediamine, 5-((3,4-dimethoxyphenyl)methyl)-
CAS REGISTRY NUMBER :
5355-16-8
BEILSTEIN REFERENCE NO. :
0258464
LAST UPDATED :
199612
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C13-H16-N4-O2
MOLECULAR WEIGHT :
260.33

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3679 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
6028 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value

MUTATION DATA

TYPE OF TEST :
Mutation in microorganisms
TEST SYSTEM :
Bacteria - Salmonella typhimurium
DOSE/DURATION :
5 ug/plate
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 261,149,1991
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xi:Irritant;
Risk Phrases R36/37/38
Safety Phrases S26-S36
RIDADR NONH for all modes of transport
WGK Germany 2
RTECS UV8142000
HS Code 2933599090
91-16-7 structure

91-16-7
7440-44-0 structure

7440-44-0
54236-98-5 structure

54236-98-5

~91%

5355-16-8 structure

5355-16-8
Literature: Hoffmann-La Roche Inc. Patent: US4143227 A1, 1979 ;
30077-75-9 structure

30077-75-9
50-01-1 structure

50-01-1

~96%

5355-16-8 structure

5355-16-8
Literature: Hachtel; Haller; Seydel Arzneimittel-Forschung/Drug Research, 1988 , vol. 38, # 12 p. 1778 - 1783
91959-82-9 structure

91959-82-9

~%

5355-16-8 structure

5355-16-8
Literature: Journal of the American Chemical Society, , vol. 73, p. 3758,3760 US2624732 , ;
120-14-9 structure

120-14-9

~%

5355-16-8 structure

5355-16-8
Literature: Arzneimittel-Forschung/Drug Research, , vol. 38, # 12 p. 1778 - 1783
30077-88-4 structure

30077-88-4

~%

5355-16-8 structure

5355-16-8
Literature: Arzneimittel-Forschung/Drug Research, , vol. 38, # 12 p. 1778 - 1783
HS Code 2933599090
Summary 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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