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1.
Int J Antimicrob Agents ; 55(4): 105906, 2020 Apr.
Article in English | MEDLINE | ID: mdl-31987883

ABSTRACT

Chagas disease, leishmaniasis and schistosomiasis are neglected diseases (NDs) and are a considerable global challenge. Despite the huge number of people infected, NDs do not create interest from pharmaceutical companies because the associated revenue is generally low. Most of the research on these diseases has been conducted in academic institutions. The chemotherapeutic armamentarium for NDs is scarce and inefficient and better drugs are needed. Researchers have found some promising potential drug candidates using medicinal chemistry and computational approaches. Most of these compounds are synthetic but some are from natural sources or are semi-synthetic. Drug repurposing or repositioning has also been greatly stimulated for NDs. This review considers some potential drug candidates and provides details of their design, discovery and activity.


Subject(s)
Anthelmintics/therapeutic use , Chagas Disease/drug therapy , Drug Discovery/methods , Drug Repositioning/methods , Leishmaniasis/drug therapy , Schistosomiasis/drug therapy , Animals , Antiprotozoal Agents/therapeutic use , Humans , Leishmania/drug effects , Neglected Diseases/drug therapy , Schistosoma/drug effects , Trypanosoma cruzi/drug effects
2.
Int J Pharm ; 573: 118814, 2020 Jan 05.
Article in English | MEDLINE | ID: mdl-31759101

ABSTRACT

Dendrimers are globular structures, presenting an initiator core, repetitive layers starting radially from the core and terminal groups on the surface, resembling tree architecture. These structures have been studied in many biological applications, as drug, DNA, RNA and proteins delivery, as well as imaging and radiocontrast agents. With reference to that, this review focused in providing examples of dendrimers used in nanomedicine. Although most studies emphasize cancer, there are others which reveal action in the neurosystem, reducing either neuroinflammation or protein aggregation. Dendrimers can carry bioactive compounds by covalent bond (dendrimer prodrug), or by ionic interaction or adsortion in the internal space of the nanostructure. Additionally, dendrimers can be associated with other polymers, as PEG (polyethylene glycol), and with targeting structures as aptamers, antibodies, folic acid and carbohydrates. Their products in preclinical/clinical trial and those in the market are also discussed, with a total of six derivatives in clinical trials and seven products available in the market.


Subject(s)
Dendrimers/administration & dosage , Dendrimers/chemistry , Nanomedicine/methods , Nanostructures/chemistry , Antineoplastic Agents/administration & dosage , Chemistry, Pharmaceutical , Clinical Trials as Topic , Contrast Media/administration & dosage , Contrast Media/chemistry , Humans , Nanostructures/administration & dosage , Neoplasms/diagnostic imaging , Neoplasms/drug therapy , Nervous System Diseases/diagnostic imaging , Nervous System Diseases/drug therapy , Nervous System Diseases/immunology , Polyethylene Glycols/chemistry , Prodrugs/administration & dosage , Prodrugs/chemistry , Protein Aggregation, Pathological/diagnostic imaging , Protein Aggregation, Pathological/drug therapy
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