Hygeia journal for drugs and medicines


Synthesis and Ulcer reducing activity studies of some Peptide derivatives of Aspirin

Hygeia.JD.Med.Vol.3 (2),Oct.2011-March 2012, 38-47.


Article title: Synthesisand Ulcer reducing activity studies of some Peptide derivatives of Aspirin

 Authors. M.Sekar1*andJ. Balamani2

1.   Post Graduate and Research Department ofChemistry, Kongunadu Arts and Science College, Coimbatore-641 029, India.

2.  Post Graduate and Research Department of Chemistry, Sri Ramakrishna MissionVidyalaya College of Arts and Science, Coimbatore-641 020, India.                       

Articlehistory: Received: 15 December, 2010,revised: 24 May, 2011, accepted: 28 June, 2011, Available online: 1 October 2011.


 Tetrapeptidederivatives of Aspirin (1 to 4) were synthesized by the followingmethods. Aspirin was prepared by acetylation of salicylic acid using Ac2O/ AcOH. Aspirin was coupled with aminoacid amide and dipeptide amide using its  p-nitro phenyl (NP) ester. The ester (Aspirin – ONP) was prepared by treating p-nitro phenol andDCC in EtOAc and was precipitated by using EtOH. The synthesis of dipeptideamides were carried out in solution by stepwise elongation of the peptide chainfrom the C-terminal aminoacid by coupling one aminoacid at a time usingDCC/HOBt method. Boc-group was used from Nα protection of all aminoacids. The Boc-group cleavage was carried out using 50% TFA / CH2Cl2.The amidation of C-terminal aminoacid was carried out by treating thecorresponding Boc – aminoacid – ONp esters with dry NH3 in presenceof DCC and HOBt. Their gastric ulcer inducing property was studied byhistopathological method.

Keywords:  Aspirin – ONp, Boc – N3 (t-butylazido formate), HOBt (1-Hydroxy benzotriazole), DCC (N, N1 – Dicyclohexyl carbodiimide) and DCU (N, N1 – Dicyclohexyl urea).

Article outline


2.Materials and methods

3.Synthesis of tetrapeptide amide and ester of aspirin

4.Gastric – ulcer reducing property

5.Results and discussion

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For Correspondence: 

M.Sekar* ,and JBalamani , Hygeia.J.D.Med. Vol 3 (2), October2011, pp.38-47.

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