Metioprim

Names

[ Name ]:
Metioprim

[Synonym ]:
Metioprim
He 909
Ro 12-6995

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]:

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

[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

Related Compounds

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