Selection of the most promising 2-substituted quinoline as antileishmanial candidate for clinical trials

Vieira, Nashira Campos; Herrenknecht, Christine; Vacus, Joël; Fournet, Alain; Bories, Christian; Figadère, Bruno; Espindola, Laïla Salmen; Loiseau, Philippe M.

doi:10.1016/j.biopha.2008.09.002

Cited by 38 publications

(19 citation statements)

References 17 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Thus, this core is an interesting constituent for new drugs design. Anti-mycobacterial, anti-microbial, anti-convulsant, anti-inflamatory, anti-tumoral, cardiovascular but also leishmanicidal and trypanocidal, are some biological activities exhibited by compounds having this heteroaromatic ring [7][8][9][10][11][12][13][14][15]. On the other hand, hydrazones constitute an important type of biologically active compounds which have high ability to elicit an leishmanicidal and trypanocidal activity [16][17][18]; thus for example, the 4-benzyloxy N´,N´-diethylbenzohydrazone (figure 1a) is one of the synthetic benzyloxy protected hydrazone series with an Inhibitory Concentration (IC 50 ) of 6.25 µg/mL (21µM) against (L) major promastigotes [19].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, leishmanicidal, trypanocidal and cytotoxic activity of quinoline-hydrazone hybrids

Coa

Castrillón

Cardona

et al. 2015

European Journal of Medicinal Chemistry

View full text Add to dashboard Cite

Registro de acceso restringido Este recurso no está disponible en acceso abierto por política de la editorial. No obstante, se puede acceder al texto completo desde la Universitat Jaume I o si el usuario cuenta con suscripción. Registre d'accés restringit Aquest recurs no està disponible en accés obert per política de l'editorial. No obstant això, es pot accedir al text complet des de la Universitat Jaume I o si l'usuari compta amb subscripció. Restricted access item This item isn't open access because of publisher's policy. The full--text version is only available from Jaume I University or if the user has a running suscription to the publisher's contents.

show abstract

Section: Introductionmentioning

confidence: 99%

Synthesis, leishmanicidal, trypanocidal and cytotoxic activity of quinoline-hydrazone hybrids

Coa

Castrillón

Cardona

et al. 2015

European Journal of Medicinal Chemistry

View full text Add to dashboard Cite

show abstract

“…The susceptibility of 4 cryopreserved isolates (S 1 , S 3 , S 4 , and S 6 ; Table) to AmpB and to miltefosine was studied in the in vitro promastigote and axenic amastigote form by determining the concentrations inhibiting parasite growth by 50% ( 1 , 2 ). The 50% inhibitory concentration (IC 50 ) was determined in parallel for the following reference L. donovani lines: a wild-type L. donovani LV9 (MHOM/ET/67/HU3) line (LV9 WT), a wild-type L. donovani DD8 (MHOM/IN/80/DD8) line (DD8 WT), a laboratory miltefosine-resistant line obtained from LV9 WT (LV9 miltefosine-R, resistant to 90 μmol/L miltefosine), and the laboratory AmB-resistant line obtained from DD8 WT (DD8 AmB-R, resistant to 1.4 μmol/L AmB) on promastigote and axenic amastigote forms ( 3 , 4 ).…”

mentioning

confidence: 99%

LeishmaniaResistance to Miltefosine Associated with Genetic Marker

Cojean¹,

Houzé²,

Haouchine³

et al. 2012

Emerg. Infect. Dis.

Self Cite

View full text Add to dashboard Cite

“…Activity of 2-substituted quinoline alkaloids was subsequently reported in the L.donovani – BALB/c mouse model with 2-n-propylquinoline showing significant activity after oral administration and chimanine D after subcutaneous administration 74 . Among more than one hundred 2-substituted quinolones, 2-n-propylquinoline was found to be the most stable and safe compound in various conditions 75 . As this compound was in oily state, a 2-npropylquinoline formulation as camphorsulfonic salt ( Fig:4) was prepared and characterised.…”

Section: Investigational Drugsmentioning

confidence: 99%

Investigational drugs for visceral leishmaniasis

Sundar

Chakravarty

2014

Expert Opinion on Investigational Drugs

View full text Add to dashboard Cite

Introduction The armamentarium of antileishmanials is small. It is further being threatened by development of resistance and decreasing sensitivity to the available drugs. Development of newer drugs are sorely needed. Areas covered Literature search on investigational drugs for visceral leishmaniasis (VL) was done on PubMed. Those candidates with at least in vitro and in vivo activity against leishmania species causing VL were reviewed. Among the investigational drugs the nitroimidazole compound fexinidazole is the one of the few drugs which has reached phase II trials. Although the (S)-PA-824 is in phase II trials for the treatment of tuberculosis its R enantiomer has shown good antileishmanial activity. Development of sitamaquin, which has completed phase II studies has been stopped for VL due to its low efficacy. Many novel delivery system and oral formulations of Amphotericin B which are cheap and less toxic are in investigational stages, and will go a long way in improving the treatment of VL. Expert opinion Very few new drugs have reached the clinical stage in the treatment of this neglected tropical disease. Thus, there is an urgent need for support from public private partnerships to ensure that drug candidates are promptly taken forward into development.

show abstract

Selection of the most promising 2-substituted quinoline as antileishmanial candidate for clinical trials

Cited by 38 publications

References 17 publications

Synthesis, leishmanicidal, trypanocidal and cytotoxic activity of quinoline-hydrazone hybrids

Synthesis, leishmanicidal, trypanocidal and cytotoxic activity of quinoline-hydrazone hybrids

LeishmaniaResistance to Miltefosine Associated with Genetic Marker

Investigational drugs for visceral leishmaniasis

Contact Info

Product

Resources

About