Morita-Baylis-Hillman adducts: biological activities and potentialities to the discovery of new cheaper drugs.

This review aims to present by the first time the Morita-Baylis-Hillman adducts (MBHA) as a new class of bioactive compounds and highlight its potentialities to the discovery of new cheaper and efficient drugs. Now, most these compounds can be prepared fast and on a single synthetic step (one-pot reaction) in high yields and using ecofriendly synthetic protocols. We highlight here the aromatic MBHA, which have shown diverse biological activities as anti-Leishmania chagasi and Leishmania amazonensis (parasites that cause cutaneous and visceral leishmaniasis), anti-Trypanosoma cruzi (parasite that cause Chagas disease), anti-Plasmodium falciparum and Plasmodium berghei (parasites that cause malaria), lethal against Biomphalaria glabrata (the snail transmitter of schistosomiasis), antibacterial, antifungal, herbicide and actives against some human tumor cell lines. Understanding of the biological mechanisms of action of this new class of molecules is still in the infancy stage. However, we report here which has been described to date on the possibilities of biological mechanisms of action, and we present new analyzes based on literature in this area. The academic and industrial interest in selecting green and cheaper experiments to the drugs development has been the prime mover of the growth on the subject.

A randomised controlled clinical trial on the safety of co-administration of albendazole, ivermectin and praziquantel in infected schoolchildren in Uganda.

Integrated chemotherapy of neglected tropical diseases (NTD) through mass drug administration given as a single dose would increase treatment coverage and cost-effectiveness. This study reports on the safety of a combination of albendazole, ivermectin and praziquantel in the treatment of lymphatic filariasis (LF), schistosomiasis and soil-transmitted helminthiasis (STH) in infected children. In this randomised, controlled, single-blinded clinical trial conducted in 235 primary school children aged 5-18 years in Yumbe District in Northern Uganda, the triple combination therapy was compared with the current NTD programme regimen. Liver function testing was performed for all children who received combined therapy. The study included 48 children with LF alone, 60 children with schistosomiasis (Schistosoma mansoni), 41 children with STH, 49 children with schistosomiasis + LF and 37 children with all three types of infection. Children were closely monitored by a paediatrician for any adverse reactions for 7 days. No serious adverse events were experienced. However, 4 of 18 children in the test group and 2 of 3 children in the control group who did not report any ill conditions before treatment developed adverse drug reactions. The combined and conventional therapies were found to be equally safe. The efficacies of both therapies were comparable and satisfactory. [ClinicalTrials.gov identifier: NCT01050517].

Cost-effectiveness of triple drug administration (TDA) with praziquantel, ivermectin and albendazole for the prevention of neglected tropical diseases in Nigeria.

Onchocerciasis, lymphatic filariasis (LF), schistosomiasis and soil transmitted, helminthiasis (STH) are all co-endemic in Nigeria. Annual mass drug administration (MDA) with ivermectin (for onchocerciasis), albendazole (for STH and with ivermectin for LF) and praziquantel (for schistosomiasis) is the WHO-recommended treatment strategy for preventive chemotherapy. Separate delivery rounds for distribution of these drugs have been the usual approach to MDA. All three drugs, however, have now been shown to be clinically and programmatically safe for co-administration with what has come to be known as triple drug administration (TDA). We examined the cost savings of converting from separate delivery rounds to TDA in two states in Nigeria. In 2008, eight local government areas received a single round of ivermectin with albendazole followed at least 1 week later by a single round of praziquantel to school-aged children. The following year, a single round was administered with TDA. The number of treated individuals was essentially unchanged during both years (1,301,864 in 2008 and 1,297,509 in 2009) and no change in adverse events was reported. The total programmatic costs for the MDA, not including drug and overhead costs, reduced by 41% from $123,624 to $72,870. Cost savings were limited in larger populations due to economies of scale. TDA is recommended for mature MDA.