PMID: 3215107Jan 1, 1988Paper

Gaps and perspectives of new fluoroquinolones

Drugs Under Experimental and Clinical Research
M Neuman, A Esanu

Abstract

The gaps in the present piperazinyl-substituted fluoroquinolones include: (a) gaps in their antibacterial spectrum, varying from one fluoroquinolone to another for streptococci-pneumococci-enterococci (SPE), some Gram-negative and Gram-positive anaerobes, Nocardia, Pseudomonas maltophilia, Ureaplasma urealyticum, slow-growing mycobacteria; (b) a pH dependence of their antibacterial activity (low activity at acidic pH for piperazinyl-substituted fluoroquinolones); (c) a rapid development of bacterial resistance for some bacteria (staphylococci, pseudomonas) in prolonged treatment of cystic fibrosis, intensive care units; (d) some gaps in the pharmacokinetic parameters such as incomplete oral bioavailability, short half-life, intensive biotransformation, unwanted interactions with other antibiotics or other drugs. The prospects for fluoroquinolones are trying to eliminate these gaps. The 7-piperazinyl or pyrrolidinyl, 1-cyclopropylfluoroquinolones have improved activity on SPE, anaerobes and pseudomonas-acinetobacter. Two categories can be distinguished: (i) with increased activity on SPE, but keeping also the activity on pseudomonas (A-62824, A-62254, A-65846, A-60969, AT-3295, AT-3765); (ii) with increased activity on SPE but w...Continue Reading

Related Concepts

Related Feeds

Blood Brain Barrier Regulation in Health & Disease

The blood brain barrier is essential in regulating the movement of molecules and substances in and out of the brain. Disruption to the blood brain barrier and changes in permeability allow pathogens and inflammatory molecules to cross the barrier and may play a part in the pathogenesis of neurodegenerative disorders. Here is the latest research in this field.

Antifungals

An antifungal, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis, cryptococcal meningitis, and others. Discover the latest research on antifungals here.

Antifungals (ASM)

An antifungal, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis, cryptococcal meningitis, and others. Discover the latest research on antifungals here.

CSF & Lymphatic System

This feed focuses on Cerebral Spinal Fluid (CSF) and the lymphatic system. Discover the latest papers using imaging techniques to track CSF outflow into the lymphatic system in animal models.

Blood Brain Barrier Chips

The blood brain barrier (BBB) is comprised of endothelial cells that regulate the influx and outflux of plasma concentrations. Lab-on-a-chip devices allow scientists to model diseases and mechanisms such as the passage of therapeutic antibodies across the BBB. Discover the latest research on BBB chips here.

Blood Brain Barrier

The blood brain barrier is a border that separates blood from cerebrospinal fluid. Discover the latest search on this highly selective semipermeable membrane here.