الفهرس 
Tile : Design & synthesis of a novel Oxazolone & Imidazolone derivatives with expected biological activity
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Abstract
This thesis includes four chapters. The first one is an introduction to chemistry and pharmacology of oxazolone, triazinone and imidazolone ring systems reported to have anti-inflammatory & anti-tumor activity. The second chapter involves the objectives of the work based on structure activity relationship and molecular modelling study. It also demonstrates schemes for the preparation of the new derivatives. The third chapter represents the theoretical discussion of the experimental work for the preparation of starting materials Nicotinic acid (I) and 2-(nicotinamido)acetic acid (II), in addition to the target new oxazolones (IIIa-g), triazinones (IVa-g), sulphamoyl imidazolones (Va-n) and imidazolones (VIa-g).The fourth chapter is divided to three parts presenting the experimental work of the thesis. The first part is the synthetic approach that comprises the detailed methods for the preparation of the designed compounds in two schemes. Scheme 1: includes the preparation of starting compound nicotinic acid (I) followed by reaction with glycine affording 2-(nicotinamido)acetic acid (II). This was followed by Erlenmeyer reaction with different selected aldehydes using suitable solvents to afford five-membered heterocyclic compounds oxazolones (IIIa-g). These were further reacted with phenyl hydrazine to give six-membered heterocyclic compounds triazinones (IVa-g). Scheme 2: involves the synthesis of sulphamoyl imidazolones (Va-n) by reacting oxazolones (IIIa-g) with sulphanilamide and sulphamethoxazole. Furthermore, oxazolones (IIIa-g) derivatives were reacted with 2- aminopyridine to give compounds imidazolones (VIa-g).The structure of the new synthesized compounds was supported by elemental analyses as well as IR, 1H NMR, 13C NMR and mass spectral data and all reactions were monitored by TLC.The second part deals with the pharmacological evaluation of all newly synthesized compounds against both COX-1 and COX-2 enzymes in addition to antitumor activity evaluation of eight of the newly synthesized compounds by American National Cancer Institute (NCI