Title : Antiprotozoal activity of spiro-γ-lactone compounds
Abstract:
Antiprotozoal activity refers to the ability of a substance to inhibitor or kill protozoan parasites like Giardia, Trichomonas, Trypanosoma, Leishmania, and Plasmodium which are single-called organisms responsible for many disease. Substances are tested against common parasites including Trypanosoma brucei (sleeping sickness), Trypanosoma cruzi (Chagas disease), Leishmania spp. (leishmaniasis), Plasmodium falciparum (malaria), and Entamoeba histolytica. Effectively, plants may show antiprotozoal activity due to : flavonoids, terpenoids, alkaloids, spiro-γ-lactones and phenolic compounds. In recent years, the pharmaceutical industry is the economic sector that brought together research, manufacturing, and also marketing activities of drugs for human or veterinary medicine especially those obtained from natural sources. Indeed, medicinal chemistry plays a major role in finding and confirming the relationship between the chemical structures of molecules isolated from medicinal plants and their biological activities. Medicinal chemistry plays a major role in finding and confirming the relationship between the chemical structures of molecules isolated from medicinal plants and their biological activities.Small-ring heterocycles constitute valuable scaffolds in medicinal chemistry for generating biologically active derivatives.Remarkably, data indicate that at least 85% of all bioactive compounds incorporate a heterocyclic moiety into their structure. From a medicinal perspective, the incorporation of a spiro fragment significantly impacts the properties of the drug candidate. Introducing a spirocyclic moiety often leads to increased potency and selectivity, as observed in comparisons between spirocycles and their non-spiro counterparts. Furthermore, several examples illustrate that a spirocycle can alter the stability, physicochemical, and pharmacokinetic properties of the structure. In the present work, we are interested in the evaluation of biological activity such as antiprotozoal of two spiro-lactones using PASS online server. The latter predicts over 4000 kinds of biological activity, including pharmacological effects, mechanisms of action, toxic and adverse effects, interaction with metabolic enzymes and transporters, influence on gene expression. PASS Online server calculates two probabilities for the cmopound to be active and inactive (Pa and Pi respectively). Generally, Pa and Pi values vary from 0.000 to 1.000. This study demonstrates that the spiro-lactones showed good antiprotozoal activity.
