Metioprim

Modify Date: 2024-01-11 00:52:10

Metioprim Structure
Metioprim structure
Common Name Metioprim
CAS Number 68902-57-8 Molecular Weight 306.38300
Density 1.31g/cm3 Boiling Point 563.3ºC at 760 mmHg
Molecular Formula C14H18N4O2S Melting Point N/A
MSDS N/A Flash Point 294.5ºC

 Use of Metioprim


Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria[1][2].

 Names

Name 5-[(3,5-dimethoxy-4-methylsulfanylphenyl)methyl]pyrimidine-2,4-diamine
Synonym More Synonyms

 Metioprim Biological Activity

Description Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria[1][2].
Related Catalog
In Vitro Metioprim 对部分厌氧菌有抑制作用,平均 MIC 值为 3.2 μg/mL[1]。 Metioprim (0-1.0 μM;0-8 h) 抑制细菌生长动力学,抑制大肠杆菌的 MIC 值为 0.7 μg/mL[2]。
In Vivo Metioprim (5 mg/kg or 10 mg/kg; 静脉注射; 单剂量) 在羊中的消除半衰期比猪的短 (23 min vs 169 min),它的主要代谢产物为蛋氨酸亚砜和甲氧磷磺酸[3]。 药代动力学分析[1] Animal Route Dose (mg/kg) C0 (μg/mL) A (μg/mL) α (1/min) t1/2α (min) B (μg/mL) β (1/min) t1/2β (min) VC (1/kg) Vp (1/kg) Vd,ss (1/kg) Clβ (mL/min/kg) Pigs i.v. 5 3.6 2.1 0.032 25 1.5 0.00415 169 1.45 0.74 2.19 10.0 Goats i.v. 10 12.2 6.4 0.220 4 5.6 0.03138 23 0.85 0.44 1.28 49
References

[1]. Wüst J, et al. Activity of brodimoprim and metioprim alone and in combination with sulfonamides against anaerobic bacteria. Antimicrob Agents Chemother. 1983 Mar;23(3):490-2.  

[2]. Seydel JK, et al. Bacterial growth kinetics of Escherichia coli and mycobacteria in the presence of brodimoprim and metioprim alone and in combination with sulfamerazine and dapsone (VI). Chemotherapy. 1983;29(4):249-61.  

[3]. Nielsen P, et al. Pharmacokinetics and metabolism of metioprim in pigs and goats. Pharmacol Toxicol. 1987 Nov;61(5):330-4.  

 Chemical & Physical Properties

Density 1.31g/cm3
Boiling Point 563.3ºC at 760 mmHg
Molecular Formula C14H18N4O2S
Molecular Weight 306.38300
Flash Point 294.5ºC
Exact Mass 306.11500
PSA 123.04000
LogP 1.83110
Index of Refraction 1.642

 Synonyms

Metioprim
He 909
Ro 12-6995
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