New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
Abstract Despite the continuous research effort that has been made in recent years to find ways to treat the potentially life threatening Chagas disease (CD), this remains the third most important infectious disease in Latin America. CD is an important public health problem affecting 6–7 million people. Since the need to search for new drugs for the treatment of DC persists, in this article we present a panel of new polyamines based on the tripodal structure of tris(2-aminomethyl)amine (tren) that can be prepared at low cost with high yields. Moreover, these polyamines present the characteristic of being water-soluble and resistant to the acidic pH values of stomach, which would allow their…
In vitro evaluation of leishmanicidal properties of a new family of monodimensional coordination polymers based on diclofenac ligand
Some series of isostructural chains with general formula [M(diclof)(HO)]·(EtOH) have been obtained from reaction between diclofenac ligand (diclof) and first row transition salts (M = Mn (1),Ni (2) and Co (3)). These monodimensional coordination polymers have been characterized and their crystal structures have been solved by X-ray diffraction methods, elucidating isostructural compounds that are chains with water molecules acting as bridge between different metallic centers, while diclofenac ligands are coordinated to the octahedral coordination environment of the same. Magnetic studies of these complexes have revealed the existence of moderate ferromagnetic interactions among manganese, n…
Heterocyclic Diamines with Leishmanicidal Activity.
Leishmaniasis is one of the world's most neglected diseases with a worldwide prevalence of 12 million people. There are no effective human vaccines for its prevention, and outdated drugs hamper treatment. Therefore, research aimed at developing new therapeutic tools to fight leishmaniasis remains a crucial goal today. With this purpose in mind, here, we present 10 new compounds made up by linking alkylated ethylenediamine units to pyridine or quinoline heterocycles with promising in vitro and in vivo efficacy against promastigote and amastigote forms of Leishmania infantum, Leishmania donovani, and Leishmania braziliensis species. Three compounds (2, 4, and 5) showed a selectivity index muc…
Synthesis and in vitro leishmanicidal activity of novel [1,2,3]triazolo[1,5-a]pyridine salts
Leishmaniasis remains a significant worldwide problem; it is of great interest to develop new drugs to fight this disease. Recently we described some [1,2,3] triazolo[1,5-a] pyridine compounds with significant leishmanicidal activity. The importance of water solubility in drug action made us realise that we could transform non charged triazolopyridines into charged analogues that could increase the degree of water solubility. With this objective we report here the synthesis of novel [1,2,3] triazolo[1,5-a] pyridinium salts 2-7 from triazolopyridines 1, and the study of their in vitro leishmanicidal activity. The activity was tested on Leishmania infantum, Leishmania braziliensis and Leishma…
CCDC 1884201: Experimental Crystal Structure Determination
Related Article: Amalia García-García, José M. Méndez-Arriaga, Rubén Martín-Escolano, Javier Cepeda, Santiago Gómez-Ruiz, Alfonso Salinas-Castillo, José M. Seco, Manuel Sánchez-Moreno, Duane Choquesillo-Lazarte, Ana B. Ruiz-Muelle, Ignacio Fernández, Clotilde Marín, Antonio Rodríguez-Diéguez|2020|Polyhedron|184|114570|doi:10.1016/j.poly.2020.114570
CCDC 1884200: Experimental Crystal Structure Determination
Related Article: Amalia García-García, José M. Méndez-Arriaga, Rubén Martín-Escolano, Javier Cepeda, Santiago Gómez-Ruiz, Alfonso Salinas-Castillo, José M. Seco, Manuel Sánchez-Moreno, Duane Choquesillo-Lazarte, Ana B. Ruiz-Muelle, Ignacio Fernández, Clotilde Marín, Antonio Rodríguez-Diéguez|2020|Polyhedron|184|114570|doi:10.1016/j.poly.2020.114570