Abstract
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.
Abstract:
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
1.introduction
2.Materials and methods
3.Synthesis of tetrapeptide amide and ester of aspirin
4.Gastric – ulcer reducing property
5.Results and discussion
For downloading full text articles and issues in PDF, at free of cost , you have to fillup the hygeia registration form. At any time, you may request for the removal of your contact information from our website database.
For Correspondence:
E-mail:mmsekar7@.yahoo.co.in
M.Sekar* ,and JBalamani , Hygeia.J.D.Med. Vol 3 (2), October2011, pp.38-47.
© 2010 Hygeia journalfor drugs and medicines, all rights reserved. 2229 3590,0975 6221