Synthetic Drugs : N-Pyridoyl di-abd tri-peptide derivatives as possible synthetic tuberculostats

Abstract

The thesis entitled “SYNTHETIC DRUGS: N?PYRIDOYL DI? AND TRI?PEPTIDE DERIVATIVES AS POSSIBLE SYNTHETIC TUBERCULOSTATS” is divided into two chapters. The first chapter deals with a brief review of some of the antituberculosis drugs currently used for the treatment of tuberculosis, along with a few other derivatives exhibiting pronounced activity. Chapter 2 deals with the candidate’s work on N?pyridoyl peptide derivatives, discussed under the following subheadings: (a) Isonicotinoyl dipeptide derivatives (b) Nicotinoyl dipeptide derivatives (c) Nicotinoyl tripeptide derivatives (d) Picolinoyl dipeptide derivatives (e) Dimedone derivatives The syntheses and in vitro screening of these compounds against M. tuberculosis H37Rv are discussed. A brief account of amino acids and peptides exhibiting antibacterial activity is also presented in this chapter. Polymorphism is observed in the case of N?nicotinoyl?DL?methionyl?DL?methionine and picolinoylglycine. In the preparation of nicotinic acid ethyl ester, an improved yield is obtained by a modification of the reported procedure. Finally, the discussion of the results of pharmacological screening of the compounds synthesised by the candidate during the investigation is presented under the heading “Conclusions.” A few of these compounds (Nos. 1 through 75 except 73) have been submitted for antimicrobial screening to Smith Kline and French Laboratories, Philadelphia, and the result is awaited. A part of this work has been presented at the Indian Chemical Society Symposium, held at Bombay during the last week of December 1963, and the same has been published in the Journal of the Indian Chemical Society.