Abstract:
BACKGROUND:Fluoroquinolones, the synthetic antibacterial agents are being successfully utilized against bacterial infections, since the time immemorial. Despite of enormous useful features, these drugs are associated with some limitations also. Large number of efforts has been made by various scientists to improve pharmacokinetic properties of these drugs and hence, to overcome the limitations associated with them. OBJECTIVES:The aim of this paper is to introduce a novel scheme for synthesis of prodrug with improved pharmacokinetic properties i.e., lipophilicity and consequently, modified bioavailability of norfloxacin. METHODS:Fatty acid hydrazide of selected fatty acid was synthesized followed by preparation of 5-formyl salicylamide. N-Mannich base of norfloxacin was synthesized by reacting norfloxacin with 5-formyl salicylamide. The prodrug was obtained by covalently coupling this N-Mannich base of norfloxacin with fatty acid hydrazide. The synthesized lipid based prodrug was evaluated for partition coefficient by shake flask method and screened for antimicrobial activity against selected strains. Drug content determination and in vitro dissolution studies utilizing HPLC were also carried out. RESULTS:The synthesized prodrug was found to exhibit improved partition coefficient (1.15) when compared with parent drug, norfloxacin (0.46). The results of antimicrobial evaluation indicate promising antibacterial and antifungal activity. CONCLUSION:The synthesized prodrug proved to be a good antimicrobial substance due to improved lipophilicity and would be expected to be used as a suitable candidate for exploration of possible utilities in treatment of bacterial infections in forthcoming time.
journal_name
Curr Drug Delivjournal_title
Current drug deliveryauthors
Sharma PC,Piplani M,Rajak Hdoi
10.2174/1567201813666161018153852subject
Has Abstractpub_date
2018-02-14 00:00:00pages
219-226issue
2eissn
1567-2018issn
1875-5704pii
CDD-EPUB-79064journal_volume
15pub_type
杂志文章abstract::The objective of this study was to investigate the influence of drug type on the release of drug from PEO matrix tablets accompanied with the impact of vitamin E succinate as antioxidant. The result showed that the presence of vitamin E promoted a stable release rate of soluble drug propranolol HCl from aged PEO matri...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201812666150326113052
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journal_title:Current drug delivery
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doi:10.2174/1567201816666181119112410
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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doi:10.2174/1567201815666181024112252
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journal_title:Current drug delivery
pub_type: 杂志文章
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
pub_type: 杂志文章,评审
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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更新日期:2012-09-01 00:00:00
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journal_title:Current drug delivery
pub_type: 杂志文章,评审
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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更新日期:2016-01-01 00:00:00
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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更新日期:2020-08-17 00:00:00
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
pub_type: 杂志文章,评审
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更新日期:2005-07-01 00:00:00
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journal_title:Current drug delivery
pub_type: 杂志文章
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journal_title:Current drug delivery
pub_type: 杂志文章
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更新日期:2013-12-01 00:00:00
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
pub_type: 杂志文章
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journal_title:Current drug delivery
pub_type: 杂志文章
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更新日期:2016-01-01 00:00:00