Abstract
A literature survey has shown that some simple peptides and their derivatives and also some amino acid derivatives have pharmacological activities of interest. The thesis describes the preparation and characterisation of amino acid and thence of peptide derivatives of Aspirin, acetylsalicylic acid, and then of Alclofenac, 4-allyloxy-3-chlorophenylacetic acid. Acetylsalicyloyl-(DL)-alanine, and some amino acid and dipeptide derivatives (and one tripeptide derivative) of Alclofenac were prepared. The compounds have been submitted for pharmacological testing. The results obtained todate indicate that Alclofenac-(DL)-alanine methyl ester and Alclofenac-(DL)-alanyl-(DL)-alanine methyl ester are bioactive compounds. They inhibit the release of histamine from rat peritoneal mast cells in vitro. Further, Alclofenac-glycine and its hydrogenated form, 3-chloro-4-n-propoxyphenylacetyl-glycine, show as much anti-inflammatory activity in vivo as does Alclofenac. Derivatives are named arbitrarily as, e.g. Alclofenac-glycine etc where the first part of such composite names refers strictly to the acyl radical derived from the acid, Alclofenac.