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PYRIDOXINE DERIVATIVE-BASED BETA-ADRENERGIC BLOCKING AGENTS

机译:基于吡ID醇衍生物的β-肾上腺素阻断剂

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to synthetic biologically active substances of the heterocyclic series, having high antiadrenergic activity, which are beta-substituted alcohols containing a pyridoxine fragment of general formula 1: , where: 1a R1+R2=-C(CH3)2-, R3=NHCH(CH3)2; 1b R1+R2=-C(CH3)2-, R3=NHC(CH3)3;1c R1+R2=-C(CH3)2-, R3=NHC12H25; 1d R1+R2=-C(CH3)2-, R3=NHC(CH3)2 CH2CH3; 1e R1+R2=-C(CH3)2-, R3=N(CH2CH2)2 O; 1f R1+R2=-C(CH3)2-, R3=N(CH2CH2)2 CH2; 1g R1+R2=-C(CH3)2-, R3=OCH(CH3)2; 1h R1+R2=-C(CH3)2-, R3=OCH2CH3; 1i R1=H, R2=H, R3=OH;1j R1+R2=-CH(CH3)-, R3=NHCH(CH3)2; 1k R1+R2=-CH(CH3)-, R3=NHC(CH3)3; 1l R1+R2=-CH(CH3)-, R3=NHC(CH3)2CH2CH3; 1m R1+R2=-CH(CH3)-, R3=N(CH2CH2)2O; 1n R1+R2=-CH(CH3)-, R3=N(CH2CH2)2CH2; 1o R1+R2=-CH(CH3)-, R3=OCH2CH3.;EFFECT: compounds of general formula 1 have high efficiency and duration of antiadrenergic properties with a short time for the onset of the effect and low toxicity.;2 dwg, 20 ex
机译:技术领域本发明涉及具有高抗肾上腺素能活性的杂环系列的合成生物活性物质,其是含有通式1的吡ido醇片段的β-取代的醇。<图像文件=“ 00000011.GIF” “ 29” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 63” />,其中:1a R 1 + R 2 =-C(CH 3 2-, R 3 = NHCH(CH 3 2 ; 1b R 1 + R 2 =-C(CH 3 2-, R 3 < / Sup> = NHC(CH 3 3 ; 1c R 1 + R 2 =-C(CH 3 2-, R 3 = NHC 12 H 25 ; 1d R 1 + R 2 =-C(CH 3 2-, R 3 < / Sup> = NHC(CH 3 2 CH 2 CH 3 ; 1e R 1 + R 2 =-C(CH 3 2-, R 3 < / Sup> = N(CH 2 CH 2 2 O; 1f R 1 + R 2 =-C(CH 3 2-, R 3 < / Sup> = N(CH 2 CH 2 2 CH 2 ; 1克R 1 + R 2 =-C(CH 3 2-, R 3 < / Sup> = OCH(CH 3 2 ; 1h R 1 + R 2 =-C(CH 3 2-, R 3 < / Sup> = OCH 2 CH 3 ; 1i R 1 = H,R 2 = H R 3 = OH; 1j R 1 + R 2 =-CH(CH 3 -,R 3 = NHCH(CH 3 2 ; 1k R 1 + R 2 =-CH(CH 3 -,R 3 = NHC(CH 3 3 ; 1l R 1 + R 2 =-CH(CH 3 -,R 3 = NHC(CH 3 2 CH 2 CH 3 ; 1m R 1 + R 2 =-CH(CH 3 -,R 3 = N(CH 2 CH 2 2 O; 1n R 1 + R 2 =-CH(CH 3 -,R 3 = N(CH 2 CH 2 2 CH 2 ; 1o R 1 + R 2 =-CH(CH 3 -,R 3 = OCH 2 CH 3 .;效果:通式1的化合物具有高效率和持续的抗肾上腺素能持续时间短,且起效时间短毒性。; 2 dwg,20 ex

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