Today there is a highly elevated demand for synthesis and screening of nature-like biopolymers an... more Today there is a highly elevated demand for synthesis and screening of nature-like biopolymers and their more stable modified derivatives like peptidomimetics because availability of huge amounts of genomic and proteomic data can contribute for research in this area. The design and synthesis of peptidomimetics are most important because of the dominant position peptide and protein-protein interactions play in molecular recognition and signaling, especially in living systems. The design of peptide mimetics can be viewed from several different perspectives and peptidomimetics can be categorized in a number of different ways. Study of the vast literature would suggest that medicinal and organic chemists, who deal with peptide mimics, utilize these methods in many different ways. This manuscript is an endeavor to discuss a variety of methodologies and strategies to develop and establish systematic tools for transformation of peptides into peptidomimetics or further into small drug-like ...
Journal of Enzyme Inhibition and Medicinal Chemistry, 2011
A series of six novel 1-ethyl-6-fluoro-7-[4-(1-alkyl-1,4-dihydropyridine-3-carbonyl)-piperazin-1-... more A series of six novel 1-ethyl-6-fluoro-7-[4-(1-alkyl-1,4-dihydropyridine-3-carbonyl)-piperazin-1-yl]-4-oxo-1,4dihydro-quinoline-3-carboxylates has been synthesized and evaluated for antibacterial activity. Norfloxacin was reacted with thionyl chloride, to yield norfloxacin acid chloride which was used immediately in next step by reacting with respective alcohols to furnish the corresponding esters i.e. 1-ethyl-6fluoro-1,4-dihydro-7-piperazin-1-yl-4-oxoquinoline-3carboxylates. Nicotinoyl chloride was prepared by adopting reported procedures and was reacted appropriately with previously synthesized esters to yield the amides. Amides were converted into the corresponding quaternary compounds by reacting with suitable alkyl halides. The quaternary compounds were reduced in the inert atmosphere to yield the title compounds. The structures of synthesized compounds were established on the basis of analytical and spectral studies. All the synthesized compounds were evaluated for antibacterial activity against five different strains of bacteria. Compounds exhibited moderate to significant minimum inhibitory concentration.
Hydrazone comprising compounds as promising anti-infective agents: chemistry and structure-property relationship, 2020
Despite the adverse effects of microbial hazards on public health, major pharmaceutical firms hav... more Despite the adverse effects of microbial hazards on public health, major pharmaceutical firms have left the field of anti-infective development and a dramatic reduction in the number of researcher's intricated in the quest for new specific anti-infective leads. In the non-existence of an efficient forum for antibiotics development and over usage in human beings and animals, bacteria have demoralized this potential by gradually establishing the resistance toward most of the antibiotics used. Thus, the production of novel and successful anti-infective drugs is urgently required to combat this resistance. Hydrazones and hy-drazides have mounted as a key-skeleton for the development of active drugs, due to their important biological and pharmacological profiles. Hydrazones are being manufactured as medicines by various investigators to fight against the ailments with maximal effects and minimal toxicity. This paper focuses on the outline of the literature results of recent years, incorporating the work on the anti-infective profile of hydrazone analogues. This review may also act as an excellent basis for the development of new derivatives of hydrazone as potential anti-infective mediators.
Today there is a highly elevated demand for synthesis and screening of nature-like biopolymers an... more Today there is a highly elevated demand for synthesis and screening of nature-like biopolymers and their more stable modified derivatives like peptidomimetics because availability of huge amounts of genomic and proteomic data can contribute for research in this area. The design and synthesis of peptidomimetics are most important because of the dominant position peptide and protein-protein interactions play in molecular recognition and signaling, especially in living systems. The design of peptide mimetics can be viewed from several different perspectives and peptidomimetics can be categorized in a number of different ways. Study of the vast literature would suggest that medicinal and organic chemists, who deal with peptide mimics, utilize these methods in many different ways. This manuscript is an endeavor to discuss a variety of methodologies and strategies to develop and establish systematic tools for transformation of peptides into peptidomimetics or further into small drug-like ...
Journal of Enzyme Inhibition and Medicinal Chemistry, 2011
A series of six novel 1-ethyl-6-fluoro-7-[4-(1-alkyl-1,4-dihydropyridine-3-carbonyl)-piperazin-1-... more A series of six novel 1-ethyl-6-fluoro-7-[4-(1-alkyl-1,4-dihydropyridine-3-carbonyl)-piperazin-1-yl]-4-oxo-1,4dihydro-quinoline-3-carboxylates has been synthesized and evaluated for antibacterial activity. Norfloxacin was reacted with thionyl chloride, to yield norfloxacin acid chloride which was used immediately in next step by reacting with respective alcohols to furnish the corresponding esters i.e. 1-ethyl-6fluoro-1,4-dihydro-7-piperazin-1-yl-4-oxoquinoline-3carboxylates. Nicotinoyl chloride was prepared by adopting reported procedures and was reacted appropriately with previously synthesized esters to yield the amides. Amides were converted into the corresponding quaternary compounds by reacting with suitable alkyl halides. The quaternary compounds were reduced in the inert atmosphere to yield the title compounds. The structures of synthesized compounds were established on the basis of analytical and spectral studies. All the synthesized compounds were evaluated for antibacterial activity against five different strains of bacteria. Compounds exhibited moderate to significant minimum inhibitory concentration.
Hydrazone comprising compounds as promising anti-infective agents: chemistry and structure-property relationship, 2020
Despite the adverse effects of microbial hazards on public health, major pharmaceutical firms hav... more Despite the adverse effects of microbial hazards on public health, major pharmaceutical firms have left the field of anti-infective development and a dramatic reduction in the number of researcher's intricated in the quest for new specific anti-infective leads. In the non-existence of an efficient forum for antibiotics development and over usage in human beings and animals, bacteria have demoralized this potential by gradually establishing the resistance toward most of the antibiotics used. Thus, the production of novel and successful anti-infective drugs is urgently required to combat this resistance. Hydrazones and hy-drazides have mounted as a key-skeleton for the development of active drugs, due to their important biological and pharmacological profiles. Hydrazones are being manufactured as medicines by various investigators to fight against the ailments with maximal effects and minimal toxicity. This paper focuses on the outline of the literature results of recent years, incorporating the work on the anti-infective profile of hydrazone analogues. This review may also act as an excellent basis for the development of new derivatives of hydrazone as potential anti-infective mediators.
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Papers by Prabodh Sharma