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1.
Molecules ; 25(6)2020 Mar 13.
Artículo en Inglés | MEDLINE | ID: mdl-32183140

RESUMEN

Malaria, affecting all continents, remains one of the life-threatening diseases introduced by parasites that are transmitted to humans through the bites of infected Anopheles mosquitoes. Although insecticides are currently used to reduce malaria transmission, their safety concern for living systems, as well as the environment, is a growing problem. Therefore, the discovery of novel, less toxic, and environmentally safe molecules to effectively combat the control of these vectors is in high demand. In order to identify new potential larvicidal agents, a series of 2-aryl-1,2-dihydroquinazolin-4-one derivatives were synthesized and evaluated for their larvicidal activity against Anopheles arabiensis. The in silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of the compounds were also investigated and most of the derivatives possessed a favorable ADMET profile. Computational modeling studies of the title compounds demonstrated a favorable binding interaction against the acetylcholinesterase enzyme molecular target. Thus, 2-aryl-1,2-dihydroquinazolin-4-ones were identified as a novel class of Anopheles arabiensis insecticides which can be used as lead molecules for the further development of more potent and safer larvicidal agents for treating malaria.


Asunto(s)
Anopheles/efectos de los fármacos , Simulación por Computador , Insecticidas/toxicidad , Malaria/parasitología , Mosquitos Vectores/efectos de los fármacos , Quinazolinas/toxicidad , Animales , Cristalografía por Rayos X , Insecticidas/síntesis química , Insecticidas/química , Larva/efectos de los fármacos , Modelos Moleculares , Conformación Molecular , Quinazolinas/síntesis química , Quinazolinas/química , Estereoisomerismo
2.
J Biomed Mater Res A ; 109(10): 2036-2064, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-33834610

RESUMEN

Electrospun technology becomes a valuable means of fabricating functional polymeric nanofibers with distinctive morphological properties for drug delivery applications. Nanofibers are prepared from the polymer solution, which allows the direct incorporation of therapeutics such as small drug molecules, genes, and proteins by merely mixing them into the polymeric solution. Due to their biocompatibility, adhesiveness, sterility, and efficiency in delivering diverse cargoes, electrospun nanofibers have gained much attention. This review discusses the capabilities of the electrospun nanofibers in delivering different therapeutics like small molecules, genes, and proteins to their desired target site for treating various ailments. The potential of nanofibers in administering through multiple administration routes and the associated challenges has also been expounded along with a cross-talk about the commercial products of nanofibers for biomedical applications.


Asunto(s)
Sistemas de Liberación de Medicamentos , Nanofibras/química , Ingeniería de Tejidos , Animales , Tecnología Biomédica , Vías de Administración de Medicamentos , Humanos , Nanotubos de Carbono/química
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