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[PDF] Heterocyclic chemistry - PDF Drive

ABSTRACT: Peptide deformylase (PDF) is a mononuclear metal ion protein that is responsible for removing the N-formyl group of nascent proteins found in bacteria and chloroplasts in order for them to become mature proteins. From literature it was found that heterocyclic derivatives containing hydroxamic acid and hydroxyl amine exhibit good antibacterial and PDF inhibitory activity. Heterocycles bearing nitrogen, sulphur, oxygen and thiazole moieties constitute the core structure of a number of biologically interesting compounds. Recently 1,3,4 oxadiazole and 1,3,4 –triazole derivatives received significant attention owing to their diverse range of biological properties particularly being antifungal, antitubercular, antibacterial, antiviral, anticancer and antioxidant. Ethyl-cyano- acetate when treated with sodium hydrate and THF give acetate derivatives, which on further treatment with hydrazine hydrate and various reagent afforded heterocyclic hydroxylamine derivatives

Several lead inhibitors have demonstrated in vivo efficacy and an excellent safety profile. From literature it was also found that heterocyclic derivatives containing hydroxamic acid and hydroxyl amine exhibit good antibacterial and PDF inhibitory activity. PDF inhibitor synthesis have shown to posses potent antibacterial activity structural features have been used in the present work for designing novel antibacterial compounds. The SAR of various PDFIs synthesized revealed some specific characters essential for antibacterial activity.6

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The synthesis of heterocyclic compounds: Some …

Chapter-I contains many observations from the literature regarding the various types of heterocyclic compounds.

Heterocyclic derivatives is very important for PDF inhibitory activity and hence retained as a major functional group as per the literature, substituted aliphatic chain , with hydroxylamine, so that some conclusion drawn at the end of work.

Recent developments and current situation of solid phase heterocyclic synthesis are discussed focussing on cyclization of heterocyclic compounds. Solid phase synthesis is regarded as a basic technology for supporting combinatorial synthesis and automated synthesis. Heterocyclic compounds have been found in many biologically active substances and further investigation of solid phase heterocyclic chemistry is desired.

Heterocyclic Chemistry - PDF Drive

The present work aimed at synthesizing novel antibacterial agents based on PDF inhibitory and antibacterial activity. Literature survey revealed that heterocyclic containing hydroxylamine derivatives play important role in reported PDF inhibitors and potent antibacterial agent. Based on this, a series of compounds containing different substituted Oxadiazole and Triazole derivatives containing hydroxylamine were successfully synthesized. The characterized compounds were taken for antibacterial as well as antioxidant activity was performed. The compounds were purified and characterized by physical constant, IR and NMR.

Heterocycles also play an important role in the design and discovery of new physiologically and pharmacologically active compounds.

The synthesized compounds were subjected to antibacterial and antioxidant activity. Antibacterial activity of all the synthesized heterocyclic and hydroxyl amine derivatives were screened against both gram positive and gram negative bacteria by cup plate method (agar well diffusion technique). Streptomycin was used as standard drug.

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SYNTHESIS OF THE HETEROCYCLIC HYDROXAMIC ACID …

Peptide deformylase (PDF) is a mononuclear metal ion protein that is responsible for removing the N-formyl group of nascent proteins found in bacteria and chloroplasts in order for them to become mature proteins. From literature it was found that heterocyclic derivatives containing hydroxamic acid and hydroxyl amine exhibit good antibacterial and PDF inhibitory activity. Heterocycles bearing nitrogen, sulphur, oxygen and thiazole moieties constitute the core structure of a number of biologically interesting compounds. Recently 1,3,4 oxadiazole and 1,3,4 –triazole derivatives received significant attention owing to their diverse range of biological properties particularly being antifungal, antitubercular, antibacterial, antiviral, anticancer and antioxidant. Ethyl-cyano- acetate when treated with sodium hydrate and THF give acetate derivatives, which on further treatment with hydrazine hydrate and various reagent afforded heterocyclic hydroxylamine derivatives

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