Evaluation of in-vitro leishmanicidal activity of hydrazones of thiophene carboxaldehydes against promastigotes of Leishmania infantum and Leishmania tropica

Author:

Savornin B1,Madadi N E2,Delmas F1,Gasquet M1,Timon-David P1,Vanelle P2,Maldonado J2

Affiliation:

1. Laboratory of Parasitology, Faculté de Pharmacie, 27 Bd Jean Moulin, 13385 Marseille Cedex 5, France

2. Laboratory of Organic Chemistry, Faculté de Pharmacie, 27 Bd Jean Moulin, 13385 Marseille Cedex 5, France

Abstract

Abstract The lack of leishmanicidal drugs has prompted the synthesis and testing of new hydrazones of thiophene carboxaldehydes against three Leishmania strains. The compounds were obtained by condensation of appropriate hydrazines with thiophene 2-carboxaldehyde (series 7), thiophene 3-carboxaldehyde (series 2), and 5-nitrothiophene-2-carboxaldehyde (series 3). Leishmanicidal activity was assessed against promastigotes of Leishmania strains, grown in-vitro in nutrient broth medium complemented with fresh rabbit blood. The minimal inhibitory concentrations were evaluated against pentamidine, as a reference drug. Several compounds exhibited significant leishmanicidal activity, the best being ten times more active than pentamidine.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Reference7 articles.

1. Pharm;D'Arcy;Internat.,1983

2. Hybrid molecules: growth inhibition of Leishmania donovani promastigotes by thiosemicarbazones of 3-carboxy β-carbolines;Dodd;J. Med. Chem.,1989

3. Pharmacologie antiparasitaire d'aminals du nitro-5 thiophene carboxaldehyde-2;Gasquet;Bull. Soc. Fr. Parasit.,1989

4. Dérivés du furanne et du thiophène à propriétés antifongiques;Maldonado;Eur. J. Med. Chem.,1986

5. Isolement et culture des Corps de Leishman;Nicolle;Arch. Inst. Pasteur Tunis,1908

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