D. Kardile, N. Kalyane
2010
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Journal
International Journal of Applied Biology and P
Abstract
The purpose of this research was to development of new potent bioactive molecule with less toxic, safer and easy available. Modern therapeutic is based on scientific observation supported by systematic assessment of activity of drug is simulated and clinical condition. The integrity of the drug molecule, optimization of biological effect, uniform and consistent availability of drug from the dosage. Present work deals with the preparation of thiomorpholie derivatives by nucleophilic substitution reaction. Thiomorpholine (I) and P-chlorobenzonitrile (II) on reflux gives 4– thiomorpholin–4ylbenzonitrile (III) then this upon hydrolysis by using sodium hydroxide and methanol gives corresponding 4–thiomorpholin–4ylbenzoic acid (IV).This acid on treatment with thionyl chloride gives corresponding 4–thiomorpholin–4ylbenzoyl chloride (V).This is treated with hydrazine hydrate gives 4–thiomorpholin–4ylbenzohydrazide (VI) then this hydrazide is treated with various substituted heterocyclic compound to form thiomorpholine derivatives. Aromatic and Heterocyclic derivatives were synthesized to increase Log P value by increasing microbial intracellular concentration and to decrease microbial resistance. The newly synthesized compounds were tested for its antimicrobial activity. The structures of newly synthesized compounds were established on the basis of elemental analysis, IR, 1H NMR and mass spectral data.