40332-16-9Relevant articles and documents
Molecular modeling, synthesis and biological evaluation of N-heteroaryl compounds as reverse transcriptase inhibitors against HIV-1
Singh, Anuradha,Yadav, Dipti,Yadav, Madhu,Dhamanage, Ashwini,Kulkarni, Smita,Singh, Ramendra K.
, p. 336 - 347 (2015)
Different N-heteroaryl compounds bearing pyrimidine and benzimidazole moieties have been designed in silico using Discovery studio 2.5 software, synthesized and evaluated for their inhibitory activity as reverse transcriptase inhibitors against HIV-1 replication using laboratory adapted strains HIV-1IIIB (X4, subtype B) and HIV-1Ada5 (R5, subtype B), and the primary isolates HIV-1UG070 (X4, subtype D) and HIV-1VB59 (R5, subtype C). Cell-based assay showed that compounds were active at 1.394 μM concentrations (Selectivity Index: 1.29-38.39). The studies on structure-activity relationship clearly suggested anti-HIV activity of pyrimidine and benzimidazole derivatives and these findings were consistent with the in vitro cell-based experimental data. The results of molecular modeling and docking confirmed that all compounds assumed a butterfly-like conformation and showed H-bond, 'π-π' and 'π-+' and hydrophobic interactions within flexible non-nucleoside inhibitor binding pocket of HIV-1 reverse transcriptase, similar to known non-nucleoside reverse transcriptase inhibitors, such as nevirapine. In view of the results obtained, it can be said that the chemical skeletons of N, N′-bis-(pyridin-2-yl)-succinamide (14 and 15) and 1, 4-bis-benzoimidazol-1-yl-butane-1, 4-dione (16 and 17) may be used for developing potent inhibitors of HIV-1 replication, with suitable structure/pharmacophore modifications.
Analgesic and anti-inflammatory activity of new analogs of HC-030031: A TRPA1 channel antagonist
Kazek, Grzegorz,?lusarczyk, Marietta,Bry?a, Adrian,Ch?o-Rzepa, Gra?yna,Zygmunt, Ma?gorzata
, p. 113 - 119 (2020/04/09)
One of our study direction is research in the group of compounds affecting the TRPA1 ion channel (Transient receptor potential cation channel, subfamily A, member 1) which can perform an important function in pain (including neuropathic pain) and inflamma
Ramoplanin derivatives possessing antibacterial activity
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Page/Page column 57, (2010/11/23)
Novel ramoplanin derivatives are disclosed. These ramoplanin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against gram positive bacteria, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.