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Pteridine derivatives with nitric oxide synthase inhibitor function

A compound, pteridine technology, applied in the field of pteridine derivatives, can solve problems such as lack of NOS isomerase inhibition selectivity

Inactive Publication Date: 2006-11-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Inhibitors mentioned above lack considerable selectivity for NOS isomerase inhibition

Method used

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  • Pteridine derivatives with nitric oxide synthase inhibitor function
  • Pteridine derivatives with nitric oxide synthase inhibitor function
  • Pteridine derivatives with nitric oxide synthase inhibitor function

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0081] 1. Compound preparation

[0082] 2-amino-4-[N-(ethyl p-aminobenzoate)-yl]-6-phenylpteridine ( 6 )

[0083] 0.68g (1.65mmol) compound A (wherein: NR 2 R 3 = HNC 6 h 4 COOC 2 h 5 ) was added into 15 mL of anhydrous methanol to dissolve it completely, and under the conditions of nitrogen protection, stirring and oil bath reflux, dropwise added a solution composed of benzoxime (C, R”=H) 0.37 g (2.48 mmol) and 6 mL of methanol , reflux reaction for 4 hours, stop heating, after cooling to room temperature, adjust the pH value to 7-8 with ammonia water, solid precipitates, put it in the refrigerator overnight, and filter to obtain the crude product, recrystallize from a mixture of ether and ethanol to obtain 0.22 g of orange-yellow solid 6 , Yield: 34.6%, m.p.275~277℃. 1 H-NMR δ: 9.32(s, 1H, 7-H), 9.23(s, 1H, 4-NH), 8.13-7.97(m, 6H, Ph-H), 7.55(m, 3H, Ph-H) , 6.06 (bs, 2H, 2-NH 2 ), 4.39 (q, J=6.9Hz, 2H, CH 2 ), 1.41(t, J=6.9Hz, 3H, CH 3 ).ESI-MS: 387.2[M+H] + .An...

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Abstract

The present invention relates to pteridine derivatives represented by general formula (I), which are inhibitors of NO synthase, especially inducible NO synthase, and are used to prepare drugs for preventing and treating diseases mediated by elevated levels of NO in the body . ∴

Description

technical field [0001] The present invention relates to the design and synthesis of pteridine derivatives capable of controlling excessive production of nitric oxide free radicals (NO·, abbreviated as NO) in the body, especially pteridine derivatives with the effect of inducible NO synthase inhibitors. Medicines for preventing and treating diseases mediated by elevated NO levels in the body can be prepared. [0002] This invention research work was funded by the National Natural Science Foundation of China (Project No. 39870822). Background of the invention [0003] NO is a bioactive molecule with low molecular weight and hydrophobic properties, which can freely pass through the cell membrane and act on target molecules in the cell. Theoretically, NO can reach any part of the cell and tissue, so it can regulate various cell functions and Produce a wide range of biological effects. NO is produced by endogenous nitric oxide synthase (NO Synthase, abbreviated as NOS). NOS use...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D475/08A61K31/519A61P7/00A61P29/00A61P37/06A61P3/10A61P9/00A61P25/08A61P25/06
Inventor 姚其正王秋娟吕刚周卫芬唐锋毛利姆
Owner CHINA PHARM UNIV
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