2-Amino-thiophene derivatives present antileishmanial activity mediated by apoptosis and immunomodulation in vitro was written by Rodrigues, Klinger Antonio da Franca;Dias, Cinthia Nobrega de Sousa;Neris, Patricia Lima do Nascimento;Rocha, Juliana da Camara;Scotti, Marcus Tullius;Scotti, Luciana;Mascarenhas, Sandra Rodrigues;Veras, Robson Cavalcante;Almeida de Medeiros, Isac;Keesen, Tatjana de Souza Lima;Bento de Oliveira, Tiago;Alves de Lima, Maria do Carmo;Balliano, Tatiane Luciano;Mendonca de Aquino, Thiago;Olimpio de Moura, Ricardo;Junior, Francisco Jaime Bezerra Mendonca;de Oliveira, Marcia Rosa. And the article was included in European Journal of Medicinal Chemistry in 2015.Recommanded Product: 2-Amino-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile This article mentions the following:
This study evaluated the effects of 2-amino-thiophene derivatives on the promastigote and amastigote forms of Leishmania amazonensis and their possible mechanisms of action. Initially, the authors evaluated the antileishmanial activity of ten 2-amino-thiophene derivatives on promastigote and axenic amastigote forms of Leishmania amazonensis and their cytotoxicity against murine macrophages and human red blood cells. Three promising compounds were selected for studies of the cell death process using flow cytometry anal. and a DNA fragmentation assay. The effects of the compounds were assessed on intramacrophagic amastigotes, and the modulation of cytokine and NO production was investigated. All thiophene derivatives showed antileishmanial activity against promastigotes and axenic amastigotes with less toxicity for murine macrophages and human red blood cells. The best values were obtained for compounds containing a lateral indole ring. Docking studies suggested that these compounds played an important role in inhibiting trypanothione reductase (TryR) activity. The selected compounds SB-200, SB-44, and SB-83 induced apoptosis in promastigotes involving phosphatidylserine externalization and DNA fragmentation in a pattern similar to that observed for the pos. control. Addnl., SB-200, SB-44, and SB-83 significantly reduced the infection index of macrophages by the parasites; for compounds SB-200 and SB-83 this reduction was associated with increased TNF-α, IL-12, and NO levels. This study demonstrated the effective and selective action of 2-amino-thiophene derivatives against L. amazonensis, resulting in apoptosis-like cell death and immunomodulation in vitro. The results suggest that they are promising compounds for the development of new leishmanicidal drugs. In the experiment, the researchers used many compounds, for example, 2-Amino-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile (cas: 70291-62-2Recommanded Product: 2-Amino-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile).
2-Amino-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile (cas: 70291-62-2) belongs to nitriles. The electronic structure of nitriles is very similar to that of an alkyne with the main difference being the presence of a set of lone pair electrons on the nitrogen. Some nitriles are manufactured by heating carboxylic acids with ammonia in the presence of catalysts. This process is used to make nitriles from natural fats and oils, the products being used as softening agents in synthetic rubbers, plastics, and textiles and for making amines.Recommanded Product: 2-Amino-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile
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