The synthesis of some penicillins with potential antihistaminic activit .


Research type: Research Paper

Authors: Omer, Salah Eldin Ali .

Abstract: As part of a programme aimed at synthesizing penicillins with standard antihistaminics as side chain, the present thesis is concerned with the synthesis of selected standard antihistaminics into which a carboxylate function was introduced and coupled to 6-aminopenicillanic acid. the work in this thesis is included in three chapters: The first chapter deals with a literature of the evolution of penicillin B-lactam antibiotics and penicillin allergy as a major problem. Also the objective to overcome this problem is given. The experimental work is described in chapter. 2. It includes detailed experimental procedures that lead to the synthesis and isolation of two penicillin salts: [1] 6-[-a-(2-dimerhylaminoethoxy) -a,a-diphenyl] acetamido] -penicillanic acid sodium salt. [2] 6-1[a-(4-methylpiperazyl)-a,a-diphenyl] acetamidol-penicillanic acid sodium salt. Identity and purity tests have also been describe including spectral analysis, thin layer chromatography and elemental analytical results. Also micobological data is given. Trials were also performed to synthesize the two carboxylic acid salts: [3] sodium-a-[2-(B-dimethylaminoethyl) aminopyridine] phenylacetate. [4] sodium-aphenyl-a-(B-dimethylaminoethyl)2-pyridyl-acetate. These salts could not be obtained successfully to be coupled to 6-amincopenicillanic acid to produce the required penicillins. A general scheme of work representing the synthetic procedures together with the intermediates and final products precedes the experimental section. In chapter 3, the results obtained and the observations are discussed. In addition a short literature survey of some synthetic procedures related to the present work, together with reaction mechanisms is included .