Promising Antileishmanial Activity Research Articles

Synthesis and antileishmanial profile of some novel terpenyl pyrimidines

Some novel terpenyl pyrimidine derivatives 2( a–d) and 6( a–b) have been synthesised from α/β-ionone keteneacetals 1 and 5. The terpenyl pyrimidine 2e has been synthesised from β-ionone 3 in two steps in quantitative yield. The pyrimidine derivatives were screened for in-vivo antilesihmanial activity. The compounds 2d, 2e, 6a and 6b showed promising in-vivo antileishmanial activity.

Aminomethylation reactions of nitrogen and sulfur five membered heterocyclic compounds

Five membered nitrogen and sulfur heterocyclic compounds such as isatins, benzimidazole, benzimidazolin-2-thione, benzoxazolinone-2, benzoxazolin-2-thione, benzotriazole, benzothiazolin-2-thione, 1,3,4-oxadiazolin-5-thione and 1,2,4-triazolin-5-thiones have been prepared and subjected to aminomethylation reactions in presence of formaldehyde and amines. Secondary as well as primary aromatic amines bearing different substituents have been successfully utilized in the aminomethylation reaction. The aminomethylated products have been tested for antibacterial, antifungal, antiviral, anticancer, antileishmanial and antifilarial activity. A number of such products have exhibited promising antifungal and antileishmanial activities.

Corrigendum: Archaeal Homologs of Eukaryotic Methylation Guide Small Nucleolar RNAs: Lessons from the Pyrococcus Genomes

The growing incidence of parasitic resistance against generic pentavalent antimonials, specifically for visceral disease in Indian subcontinent, is a serious issue in Leishmania control. Notwithstanding the two treatment alternatives, that is amphotericin B and miltefosine are being effectively used but their high cost and therapeutic complications limit their use in endemic areas. In the absence of a vaccine candidate, identification, and characterization of novel drugs and targets is a major requirement of leishmanial research. This review describes current drug regimens, putative drug targets, numerous natural products that have shown promising antileishmanial activity alongwith some key issues and strategies for future research to control leishmaniasis worldwide.

Ab initio quantum chemical analysis of stereoelectronic properties may explain in vitro antileishmanial activity of some macrocyclic bisbenzylisoquinoline alkaloids

Despite phenomenal progress made in the understanding of molecular biology of Leishmaniasis in the past few decades, no new therapeutic agent has come up for the treatment of the disease since the introduction of pentavalent antimonials almost half a century ago. Discovery of some macrocyclic bisbenzylisoquinolines from natural products has shown promising antileishmanial activity in recent years, but their mechanism of action is not known. The present theoretical investigation attempts to identify and assess the role of calculated stereoelectronic properties of five such bisbenzylisoquinolines toward their observed antileishmanial activity. The study is an ab initio quantum chemical (3-21G*/4-31G*-HF) analysis on the molecular electronic structure of gyrocarpine, daphnandrine, obaberine, pheanthine, and malekulatine. The ability to form a hole or cavity at the macrocyclic ring, preference for specific orientation of lone-pair electrons of the ether–oxygen atoms, the electrostatic potential profiles by these oxygen atoms, and similarity of the lowest unoccupied molecular orbital (LUMO) isosurface at the hole are found to be related to potent in vitro antileishmanial activity. ©1999 John Wiley & Sons, Inc. Int J Quant Chem 75: 995–1002, 1999

Expeditious enantioselective synthesis of carbocyclic nucleosides with antileishmanial activity

A short synthesis of the neplanocin A analogue 1, lacking the hydroxymethylene at C-4 of the parent naturally occurring carbocyclic nucleoside, is described. Moreover, the non toxic noraristeromycin 3, an intermediate in the synthetic scheme, was shown to exhibit a promising anti-leishmanial activity.