Leishmaniasis is widely ignored in discussions on the priorities of tropical diseases, and the alreadyexisting drugs present high toxicity or teratogenicity, as well as reduced efficacy due to the emergence of resistant strains. Marine natural products have received increasing attention over the last few decades because of the isolation of metabolites found in many products, with structural pat...

Visceral leishmaniasis (VL) or Kala-azar is the most severe form of leishmaniasis and is uniformly fatal, if untreated. An estimated 500,000 new cases occur per year, 90% of which occur in the endemic areas of India, Bangladesh, Sudan Nepal and Brazil. More than 100,000 cases of VL occur in India alone every year and the state of Bihar accounts for more than 90% of these. Over the years new the...

The bioactivity guided fractionation of the dichloromethane extract of Mitracarpus frigidus afforded the pyranonaphthoquinone psychorubrin. This compound, hitherto unknown in the genus Mitracarpus, had its biological activity evaluated against one panel of bacteria and two fungi, three tumor cell lines (HL60, Jurkat and MCF-7) and four Leishmania species. Its identity was confirmed unambiguousl...

Following the promising antileishmanial results previously obtained in monoamidoxime series, a new series of derivatives was synthesized using manganese(III) acetate, Wittig reactions and Suzuki-Miyaura cross coupling reactions. Pharmacomodulation in R(1), R(2) or R(3) substituents on the amidoxime structure is shown to influence antiprotozoan activity in vitro: a monosubstituted phenyl group i...

Leishmaniasis is a vector-borne disease that affects several populations worldwide, against which there are no vaccines available and the chemotherapy is highly toxic. Depending on the species causing the infection, the disease is characterized by commitment of tissues, including the skin, mucous membranes, and internal organs. Despite the relevance of host inflammatory mediators on parasite bu...

Abstract Previous investigation of the potent antileishmanial properties antitubercular 7-substituted 2-nitroimidazo[2,1-b][1,3]oxazines with biaryl side chains led to our development a new clinical candidate for visceral leishmaniasis (DNDI-0690). Within collaborative backup program, racemic monoaryl lead (3) possessing comparable activity in mice but greater hERG liability formed starting poi...

The properties of benzimidazole and its derivatives have been studied over more than one hundred years. Benzimidazole derivatives are useful intermediates/subunits for the development of molecules of pharmaceutical or biological interest. Substituted benzimidazole derivatives have found applications in diverse therapeutic areas such as antiulcer, anticancer agents, and anthelmintic species to n...