Design, Synthesis and Hydrolysis Study of Gatifloxacin-NSAIDs as Mutual Prodrugs

Naser, Noor H.

doi:10.14233/ajchem.2018.20981

Cited by 4 publications

(2 citation statements)

References 9 publications

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“…When a link between carbon and oxygen forms, the ring is complete. Finally, the process may produce 2-amino1, 3, 4, and 5-substituted oxadiazole [17] .…”

Section: Chemistrymentioning

confidence: 99%

Design, synthesis of new gatifloxacin derivatives as antibacterial activity

Omran

2024

J. Res. Chem.

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Infectious disease-causing organisms are known as pathogens. They consist of viruses, fungi, bacteria, and parasites. Quinolones function by preventing either bacterial gyrase or topoisomerase IV from acting. A series of oxadiazole derivatives was added to the antibacterial fluoroquinolone gatifloxacin to increase bulkiness at the C7 piperazine ring. The present study employed 2D FT-IR and 1H-NMR spectroscopy, as well as physical and chemical parameters like melting points, to characterize the synthesized compounds. The antibacterial activity of the compounds was tested against Gram-negative bacteria, specifically Aeruginosa pseudomonas. The tested compounds demonstrated no inhibition of the bacteria used in the research. The final synthetic chemicals' affinity for the topoisomerase IV enzyme was demonstrated by docking research. The results of this investigation demonstrated that the gatifloxacin-derived compounds had no effect on the activity of the bacteria employed in the investigation.

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“…When a link between carbon and oxygen forms, the ring is complete. Finally, the process may produce 2-amino1, 3, 4, and 5-substituted oxadiazole [17] .…”

Section: Chemistrymentioning

confidence: 99%

Design, synthesis of new gatifloxacin derivatives as antibacterial activity

Omran

2024

J. Res. Chem.

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“…The free carboxylic group of the NSAID was condensed with another pharmacologically active drug. To name a few mutual prodrugs, Mefenamic acid-PGA to overcome poor solubility 12 , Etodolic and Thymol with reduced ulcerogenic activity 13 , Piroxican with Aceclofenac, Ibuprofen and Mefenamic acid to reduce gastric side effects 14 , esters of Mefenamic acid with thymol and sesamol with enhanced antiinflammatory activity and reduced gastric toxicity 15 , Mefenamic acid with a tocopherol and a tocopherol acetate to reduce the CNS toxicity and enhance therapeutic efficacy 16 , Galifloxacin -Paracetamol to enhance therapeutic action 17 , p-Aminosalicyclic acid and alkyl, alkoxy carbonyl to increase oral bioavailability 18 , xylitol-ibuprofen ester for enhanced water solubility 19 , Ibuprofensulphanilamide with an improved toxicity profile 20 . NSAIDs with 4-(1H-benzo[d] imidazole 2-yl)phenol (BZ) with better anti-inflammatory potential 21 , Febuxostat-NSAIDs with gastrointestinal safety profile 22 .…”

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confidence: 99%

Untitled

2023

IJPSR

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Inflammation and pain have all been successfully treated using nonsteroidal anti-inflammatory drugs. Today's nonsteroidal anti-inflammatory drugs (NSAIDs) are typically taken with restriction due to the gastric intolerance they create. The prodrug approach is quite effective in reducing the side effects caused by NSAIDs. Many nonsteroidal anti-inflammatory drug molecules have been modified in several ways so that they can be less hazardous to the stomach. Using the mutual prodrug concept, the side effects can be minimized by covalently bonding the NSAIDs to the second pharmacologically active carrier. The goal of the current study is to use the coupling approach to create mutual ester prodrugs of NSAIDs (MS and MP) in order to overcome the troubles, they cause, like gastrointestinal toxicity, ulcerogenic side effects, etc. The prodrugs were made by using a better reagent, EDAC 1-Ethyl-3-(3-Dimethylaminopropyl) carbodiimide hydrochloride, because it outperformed DCC (N, N′-Dicyclohexylcarbodiimide) as a coupling agent. The physiochemical properties were determined, and the structures of the synthesized prodrugs were confirmed and analyzed by UV, FT-IR, 1 HNMR, 13 CNMR Spectroscopy and Mass spectrometry. INTRODUCTION:The clinical importance of NSAIDs is enormous, but there's a robust risk that they might have negative effects on the abdomen. The ability of NSAIDs to restrict the activity of the enzyme cyclooxygenase (COX) involved in prostaglandin H 2 (PGH 2 ) production is correlated with their pharmacological effectiveness 1, 2 . It is generally known that COX has two isoforms, COX-I and COX-II, which are controlled in various ways. In the GIT, COX-I is expressed constitutively in the stomach to provide cytoprotection, and COX-II plays a major role in the biosynthesis of prostaglandin, which is expressed in inflammatory cell 3 .

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Mutual Prodrugs - Codrugs

Nudelman

2023

CMC

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This review encapsulates an extensive variety of substances identified as mutual prodrugs or codrugs, wherein two, or sometimes three, biologically active moieties are linked using an assortment of metabolically unstable bridging entities. Following the administration of the mutual prodrugs, these undergo a bridge cleavage releasing the active molecules, which then elicit their respective biological effects. In some cases, the released drugs act synergistically, other times the biological activity of only one of the drugs is elicited, and in such cases, the accompanying drug serves only as a carrier, which may have an affinity to the desired receptor. The most promising results are commonly observed when the two released drugs are efficacious at similar concentrations and particularly when the two drugs are effective against similar diseases. For instance, the best results are observed, when two analgesics, two anticancer agents, two drugs for the treatment of cardiac conditions, etc., are the substances comprising the codrug. Mutual prodrugs/codrugs described herein have been reported, primarily since the year 2000, as potential drugs for use against a plethora of diseases including pain, inflammation, cancer, bacterial infections, sickle cell anemia, Alzheimer’s disease, and others.

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Design, Synthesis and Hydrolysis Study of Gatifloxacin-NSAIDs as Mutual Prodrugs

Cited by 4 publications

References 9 publications

Design, synthesis of new gatifloxacin derivatives as antibacterial activity

Design, synthesis of new gatifloxacin derivatives as antibacterial activity

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Mutual Prodrugs - Codrugs

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