Click chemistry decoration of amino sterols as promising strategy to developed new leishmanicidal drugs

Antitubercular activity of 1,2,3-triazolyl fatty acid derivatives

“…The collection of triazolyl fatty esters 1 - 25 was obtained with an 80 % average yield after purification (Table 1). The products were characterized by 1D-, 2D- NMR experiments, IR and HRMS, displaying a 1,4-substitution pattern as was expected based our previous experience[18, 37] and by several other reports. [42, 43]…”

“…Another key advantage that turns then in an attractive connection unit is that they are stable to metabolic degradation and capable of hydrogen bonding, which can be favorable in the binding of biomolecular targets and can improve the solubility. [17] Over the years, many examples of biologically active 1,2,3-triazole-containing molecules have been reported, including antiparasite,[18, 19] antifungal, [20] anticancer,[21] antiviral,[22, 23] and against many bacterial species. [24, 25] The synthesis of collections of 1,2,3-trizoles to develop new chemical entities toward M. tuberculosis has not been an exception.…”

Antitrypanosomal and antileishmanial activity of prenyl-1,2,3-triazoles

“…Isoprenyl 1,2,3-triazoles have shown promising and varied biological activities (Figure 2) such as antimicrobials, 9 antibiofilms, 10,11 antioxidants, 9 and antiparasitics. 12 Additionally they also displayed activity as geranylgeranyl transferase II, 13 geranylgeranyldiphosphate synthase, 14,15 farnesyltransferase, Ras and Rab geranylgeranyl transferase inhibitors. In the same way, it is used as a precursor for the construction of analogues and metabolites, for example FPP, 16 glycolipids 17 and pharmacological drugs.…”

“…Based on previous precedents where complex prenyl 1,2,3-triazolyl steroids 12 have shown promising antitrypanosomal activities we wanted to explored simplified version of those compounds. Looking for new chemical entities with antitrypanosomal activity, we wanted to investigate if simple prenylated 1,2,3-triazoles could displayed antiparasitic activity.…”

A minimalistic approach to develop new anti-apicomplexa polyamines analogs

“…In this opportunity, a different methodology for the synthesis was required. A one-pot procedure was selected, where two consecutive reductive aminations occurred using sodium triacetoxy borohydride, acetic acid in DCM art room temperature [25,26]. Ten new products were prepared (Scheme 2) with 22% global yield (Table 1).…”