3176-72-5Relevant articles and documents
Design, synthesis, and evaluation of different scaffold derivatives against NS2B-NS3 protease of dengue virus
Ganji, Lata R.,Gandhi, Lekha,Musturi, Venkataramana,Kanyalkar, Meena A.
, p. 285 - 301 (2020/11/19)
The number of deaths or critical health issues is a threat in the infection caused by Dengue virus, which complicates the situation, as only symptomatic treatment is the current solution. In this regard we have targeted the dengue protease NS2B-NS3 that is responsible for the replication. The series was designed with the help of molecular modeling approach using docking protocols. The series comprised of different scaffolds viz. cinnamic acid analogs (CA1–CA11), chalcone (C1–C10) and their molecular hybrids (Lik1–Lik10), analogs of benzimidazole (BZ1-BZ5), mercaptobenzimidazole (BS1-BS4), and phenylsulfanylmethylbenzimidazole (PS1-PS4). Virtual screening of various natural phytoconstituents was employed to determine the interactions of designed analogs with the residues of catalytic triad in the active site of NS2B-NS3. We have further synthesized the selected leads. The synthesized analogs were evaluated for the cytotoxicity and NS2B-NS3 protease inhibition activity and compared with known anti-dengue natural phytoconstituent quercetin as the standard. CA2, BZ1, and BS2 were found to be more potent and efficacious than the standard quercetin as evident from the protease inhibition assay.
Straightforward synthesis of photoactive chalcogen functionalized benzimidazo[1,2-a] quinolines
Da Silva, Rodrigo Borges,Lange Coelho, Felipe,Rodembusch, Fabiano Severo,Schwab, Ricardo Samuel,Schneider, Juliana Maria Forain Miolo,Da Silveira Rampon, Daniel,Schneider, Paulo Henrique
supporting information, p. 11596 - 11603 (2019/07/31)
A series of new organochalcogen derivatives of benzimidazo[1,2-a]quinolines were synthesized in moderate to excellent yields and in short reaction times from chalcogen benzimidazoles, in a straightforward synthetic procedure, through transition-metal-free cascade reactions involving a sequential intermolecular aromatic nucleophilic substitution (SNAr), followed by an intramolecular Knoevenagel condensation. Both the sulfur and selenium derivatives presented similar photophysical properties, with absorption maxima located in the UV region (～355 nm) related to spin and symmetry allowed electronic p-p? transitions, and fluorescence emission located in the violet-blue region (～440 nm) with a relatively large Stokes shift (～90 nm). The fluorescence quantum yields were slightly influenced by the chalcogen, with the sulfur derivatives presenting higher values than the selenium analogues, probably due to the intersystem crossing allowed by the selenium atom. Moreover no clear evidence for charge transfer in either compound in the ground and excited states was observed.
Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents
Liu, Ting,Sun, Changyan,Xing, Xiumei,Jing, Lingling,Tan, Rui,Luo, Youfu,Huang, Wencai,Song, Hang,Li, Zicheng,Zhao, Yinglan
supporting information; experimental part, p. 3122 - 3125 (2012/06/17)
A novel class of acetylhydrazone derivatives (5a-x) containing 2-(phenylthiomethyl)-1H-benzo-[d]-imidazole moieties are synthesizer, and their antitumor activities against A549, HCT116, HepG2, PC-9, and A375 were determined by the MTT assay. Among them ar
