New Fluoroquinolones: A Class of Potent Antibiotics

Abstract

The discovery of antibiotics opened a new era in the treatment against several pathogenic microorganisms that can disable or kill humans. The appearance of the fluoroquinolones (based on nalidixic acid, 4-quinolone-3-carboxylates), in the early 1980's, gave a new impetus in the treatment of infectious diseases. Despite these favourable properties, the earlier fluoroquinolones had limited potency against some clinically important organisms, especially Gram-positive pathogens so that the development of resistance to these organisms has become a serious problem. Thus the development of new fluoroquinolones with a better pharmacokinetic profile, potency, broad spectrum of activity, solubility, prolonged serum half-life and oral and parenteral routes of administration has been a major focus on recent research. The increasing interest in this class led me to review the promising new fluoroquinolones in clinical trials.

4-[(2-Chloroethyl)amino]quinolinium chloride monohydrate

“…For background information on the pharmacological activity of quinoline derivatives, see: Elslager et al (1969); Font et al (1997); Kaminsky & Meltzer (1968); Musiol et al (2006); Nakamura et al (1999); Palmer et al (1993); Ridley (2002); Sloboda et al (1991); Tanenbaum & Tuffanelli (1980); Warshakoon et al (2006). For recent studies on quinoline-based anti-malarials, see: Andrade et al (2007); Cunico et al (2006); da Silva et al (2003); de Souza et al (2005). For a related crystallographic study on a neutral species related to the title compound, see: Kaiser et al (2009).…”

“…It affects mainly those living in tropical and subtropical areas with an incidence of 500 million cases per year globally (Snow et al, 1999;Breman, 2001;World Health Organization, 1999). As part of our studies (de Souza et al, 2005;Andrade et al, 2007;da Silva et al, 2003;Cunico et al, 2006) of drugs for neglected diseases, various quinoline derivatives with potential antimalarial activities have been investigated. It was during this study that the the title salt hydrate, (I), was characterized.…”

Tuberculosis and the development of new tuberculostatic compounds in Far-Manguinhos (FIOCRUZ) in Rio de Janeiro

“…Nos últimos anos, fluoroquinolonas têm sido utilizadas com sucesso no tratamento da tuberculose, estando sob investigação como fármacos de primeira linha. [27][28][29][30][31][32][33] Assim sendo, em colaboração com o professor Mauro Vieira de Almeida da Universidade Federal de Juiz de Fora (MG), foi sintetizada e avaliada uma série de análogos lipofílicos da gati e moxifloxacino em que a atividade biológica depende do tamanho e da ramificação da cadeia alquílica empregada (Figura 3 e Esquema 1). 33 Outro trabalho realizado com essa classe de substâncias, em colaboração com a Dra.…”

Synthesis and antibacterial activity of novel fluoroquinolone analogs

“…Substantial efforts have been made to generate diversified quinolone libraries and the effects of various groups at this position were evaluated (Cecchetti et al, 1998;Zeng et al, 1998;Bambeke et al, 2005;Eggleston and Park, 1987;Zhanel et al, 2002). SAR revealed that secondary amino groups attached to position-7 of quinolone (De Souza, 2005;Giovanni et al, 2004) can provide efficient antimicrobial activity. The position-7 in quinolones can accommodate bulkier substituents and may be more tolerant to substitutions.…”