This paper describes the development of a class of peptide-based inhibitors as novel antitrypanosomal and antimalarial agents. The inhibitors are based on a characteristic peptide sequence for the inhibition of the cysteine proteases rhodesain of Trypanosoma brucei rhodesiense and falcipain-2 of Plasmodium falciparum. We exploited the reactivity of novel unsaturated electrophilic functions such as vinyl-sulfones, -ketones, -esters, and -nitriles. The Michael acceptors inhibited both rhodesain and falcipain-2, at nanomolar and micromolar levels, respectively. In particular, the vinyl ketone 3b has emerged as a potent rhodesain inhibitor (k = 67 × 10 M min), endowed with a picomolar binding affinity (K = 38 pM), coupled with a single-digit micromolar activity against Trypanosoma brucei brucei (EC = 2.97 μM), thus being considered as a novel lead compound for the discovery of novel effective antitrypanosomal agents.

No abstract

Pharmaceutical products have become a necessary part of life. Several studies have demonstrated that indirect exposure of humans to pharmaceuticals through the water could cause negative effects. Raw sewage and wastewater effluents are the major sources of pharmaceuticals found in surface waters and drinking water. Therefore, it is important to consider and characterize the efficiency of pharmaceutical removal during wastewater and drinking-water treatment processes. Various treatment options have been investigated for the removal/reduction of drugs (e.g., antibiotics, NSAIDs, analgesics) using conventional or biological treatments, such as activated sludge processes or bio-filtration, respectively. The efficiency of these processes ranges from 20–90%. Comparatively, advanced wastewater treatment processes, such as reverse osmosis, ozonation and advanced oxidation technologies, can achieve higher removal rates for drugs. Pharmaceuticals and their metabolites undergo natural attenuation by adsorption and solar oxidation. Therefore, pharmaceuticals in water sources even at trace concentrations would have undergone removal through biological processes and, if applicable, combined adsorption and photocatalytic degradation wastewater treatment processes. This review provides an overview of the conventional and advanced technologies for the removal of pharmaceutical compounds from water sources. It also sheds light on the key points behind adsorption and photocatalysis.

No abstract

No abstract