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Synthesis and NHE1 inhibitory activity of ligustrazine derivatives 被引量：2

Synthesis and NHE1 inhibitory activity of ligustrazine derivatives
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摘要 A series of novel derivatives of ligustrazine linked with substituted benzoyl guanidine were synthesized. These compounds have not been reported in literature, and their chemical structures were confirmed by IR, ^1H NMR and MS. The results of NHE1 inhibitory activity test showed that compounds I2, I3, I4, I6, and I7 possess more potent NHE1 inhibitory activity than cariporide. A series of novel derivatives of ligustrazine linked with substituted benzoyl guanidine were synthesized. These compounds have not been reported in literature, and their chemical structures were confirmed by IR, ^1H NMR and MS. The results of NHE1 inhibitory activity test showed that compounds I2, I3, I4, I6, and I7 possess more potent NHE1 inhibitory activity than cariporide.
作者 Mei Ren Yun Gen Xu Na Wen Da Yong Zhang Wei Yi Hua
机构地区 Center of Drug Discovery Department of Pharmacology
出处 《Chinese Chemical Letters》 SCIE CAS CSCD 2007年第5期539-541,共3页 中国化学快报（英文版）
关键词 Na^＋/H^＋ exchanger inhibitors Ligustrazine derivatives Benzoyl guanidine derivatives SYNTHESIS Na^＋/H^＋ exchanger inhibitors Ligustrazine derivatives Benzoyl guanidine derivatives Synthesis
分类号 R284.3 [医药卫生—中药学]
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参考文献8

  • 1[1]X.C.Cheng,X.Y.Liu,W.F.Xu,Drugs Future 30 (10) (2005) 1059.
  • 2[2]Z.G.Wu,J.Wuhan Inst.Chem.Technol.25 (1) (2003) 28.
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  • 6[6]Typical procedure for the synthesis of 4a-g:The mixture of compound 2 (10 mmol),compound 3 (10 mmol) and Na2CO3 (5 mmol) in 50 mL acetone was refluxed for 48 h (check by TLC) and filtrated,and the solvent was evaporated in vacuo.Typical procedure for the synthesis of I1-7:A mixture of guanidine (3.5 mmol) and 3 mL isopropyl was stirred at 70 ℃,to it was added dropwise a solution of compound 4 (0.35 mmol) dissolved in 2 mL isopropyl.The mixture was refluxed for 30 min (checked by TLC).Adjust the pH to 2 by hydrochloride,filtered,and the filtrate was evaporated in vacuo.The final product was purified by silica gel column chromatography (eluent:dichloromethane:methanol = 20:1-10:1).
  • 7[7]D.Rosskopf,E.Morgenstern,W.Scholz,et al.Hypertension 9 (3) (1991) 231.
  • 8[8]Selected spectroscopic data:I4:mp 175-176 ℃,yield:52.1%; IR (KBr,cm-1) 3380,3189,2921.1706 (vC=O),1657 (vC=N),1595,1551(vC=C),1265 (vC-O-C); 1H NMR (500 MHz,DMSO-d6,δ ppm):2.50 (s,6H,-CH3),2.59 (s,3H,-CH3),5.29 (s,2H,-CH2-O),7.20 (d,1H,J = 8.8 Hz,ArH),7.65 (bs,2H,NH),8.06 (dd,1H,J1 = 2.0 Hz,J2 = 8.8 Hz,ArH),8.32 (d,1H,J = 2.0 Hz,ArH); MS(ESI(+)70 V,m/z):394.0([M+H]+,base peak).Anal.Caled.for C16H18BrN5O2·HCl·H2O:C 43.02,H 4.74,N 15.68,found:C 42.87,H 4.82,N 15.57.

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Chinese Chemical Letters
2007年 第5期

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