N2-arylformyl-4-ammonia/amidopteridine compound capable of regulating nitrous oxide synthase acitivity

A technology of aroyl and compound, applied in the field of N2-aroyl-4-amine/amino-pteridine derivatives

Inactive Publication Date: 2009-05-20
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, so far there are no drugs that increase NO levels by activating / promoting the action of NOS

Method used

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  • N2-arylformyl-4-ammonia/amidopteridine compound capable of regulating nitrous oxide synthase acitivity
  • N2-arylformyl-4-ammonia/amidopteridine compound capable of regulating nitrous oxide synthase acitivity
  • N2-arylformyl-4-ammonia/amidopteridine compound capable of regulating nitrous oxide synthase acitivity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0042] 1 Compound preparation

[0043] 1.1 Intermediate 2,6-diamino-4-diethylaminopyrimidine (III-1)

[0044] Add 2,6-diamino-4-chloro-5-p-chlorobenzopyrimidine (5.00g, 17.7mmol) into 20ml of DMF, then add diethylamine (10g, 0.137mol), heat to 70°C and stir the reaction 5h, then poured into ice water, a yellow solid precipitated, filtered, washed with water, and dried to obtain 4.01g of yellow powder 2,6-diamino-4-diethylamino-5-p-chlorobenzopyrimidine, yield: 71%, m.p: 148~150℃, compared with literature (Frohlich LG, Kotsonis P, Traub H, et al. Inhibition of neuronal nitricoxide synthase by 4-amino pteridine derivatives: Structure-activity relationship of antagonists of (6R)-5, 6 , 7, 8-tetrahydrobiopterin cofactor. J Med Chem, 1999, 42: 4108-4121) the results were consistent.

[0045] 2,6-diamino-4-diethylamino-5-p-chlorophenylazopyrimidine (1.28g, 4mmol) was added to 20ml of ethanol, 15ml of 5% HCl solution and the mixed solution, and the temperature was raised to 70°C ,...

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Abstract

The invention relates to a method for designing and synthesizing N2-fragrant formyl-4-amido / amido-pteridines derivation with Nitric Oxide Synthase, which has the structure of (I), wherein R1 and R2 at least has one fragrant formyl. The pteridines compound can adjust the activity of NOS and can prepare for the drug.

Description

technical field [0001] The present invention relates to the design and synthesis of a class of Nitric Oxide Synthase (Nitric Oxide Synthase, abbreviated as NOS) activity that can regulate 2 - Aroyl-4-amino / amino-pteridine derivatives, used for the preparation of various diseases caused by the deficiency and reduction or excessive production of nitric oxide (Nitric Oxide, abbreviated as NO) in the body drug. Background technique [0002] Nitric oxide free radical (NO, abbreviated as NO) as an important messenger molecule and effector molecule in organisms was discovered and confirmed in the late 1980s (Hibbs JB, Taintor RR, Vavrin Z.Macrophage cytotoxicity -role for L-arginine deiminase and iminonitrogen oxidation to nitrite. Science, 1987, 235: 473-476.; Palmer RMJ, Ferige AG, Moncada S. Nitric oxide release accounts for the biological activity of endothelium-derived relaxing factor. Nature, 1987 , 327:524-526.), NO is produced in the body with a suitable rhythm and intens...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D475/08A61K31/519A61P29/00A61P11/06A61P9/12A61P9/10
Inventor 姚其正唐锋李小亮华维一
Owner CHINA PHARM UNIV
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