New thiophene-acridine compounds: Synthesis, antileishmanial activity, DNA binding, chemometric, and molecular docking studies was written by Serafim, Vanessa de Lima;Felix, Mayara Barbalho;Silva, Daiana Karla Frade;Rodrigues, Klinger Antonio da Franca;Andrade, Patricia Neris;Vitalino de Almeida, Sinara Monica;de Albuquerque dos Santos, Sanderssonilo;Ferreira de Oliveira, Jamerson;Alves de Lima, Maria do Carmo;Mendonca-Junior, Francisco Jaime Bezerra;Scotti, Marcus Tullius;Rosa de Oliveira, Marcia;Olimpio de Moura, Ricardo. And the article was included in Chemical Biology & Drug Design in 2018.Synthetic Route of C8H8N2S This article mentions the following:
In this study, we synthesized eight new compounds containing the 2-amino-cycloalkyl[b]thiophene and acridine moieties (ACT01 and ACS01-ACS07). None tested compounds presented human erythrocyte cytotoxicity. The new compounds presented antipromastigote activity, where ACS01 and ACS02 derivatives presented significant antileishmanial activity, with better performance than the reference drugs (tri and pentavalent antimonials), with resp. IC50 values of 9.60 ± 3.19 and 10.95 ± 3.96 μm. Addnl., these two derivatives were effective against antimony-resistant Leishmania (Leishmania) amazonensis strains. In addition, binding and fragmentation DNA assays were performed. It was observed that the antileishmanial activity of ACS01 is not associated with DNA fragmentation of the promastigote forms. However, it interacted with DNA with a binding constant of 104
2-Amino-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile (cas: 70291-62-2) belongs to nitriles. Nitriles are polar, as indicated by high dipole moments. As liquids, they have high relative permittivities, often in the 30s. Alkyl nitriles are sufficiently acidic to undergo deprotonation of the C-H bond adjacent to the CN group.Strong bases are required, such as lithium diisopropylamide and butyl lithium. The product is referred to as a nitrile anion. Synthetic Route of C8H8N2S
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts