2515-30-2Relevant articles and documents
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors
Viira, Birgit,Selyutina, Anastasia,García-Sosa, Alfonso T.,Karonen, Maarit,Sinkkonen, Jari,Merits, Andres,Maran, Uko
, p. 2519 - 2529 (2016/05/09)
A set of top-ranked compounds from a multi-objective in silico screen was experimentally tested for toxicity and the ability to inhibit the activity of HIV-1 reverse transcriptase (RT) in cell-free assay and in cell-based assay using HIV-1 based virus-like particles. Detailed analysis of a commercial sample that indicated specific inhibition of HIV-1 reverse transcription revealed that a minor component that was structurally similar to that of the main compound was responsible for the strongest inhibition. As a result, novel s-triazine derivatives were proposed, modelled, discovered, and synthesised, and their antiviral activity and cellular toxicity were tested. Compounds 18a and 18b were found to be efficient HIV-1 RT inhibitors, with an IC50 of 5.6 ± 1.1 μM and 0.16 ± 0.05 μM in a cell-based assay using infectious HIV-1, respectively. Compound 18b also had no detectable toxicity for different human cell lines. Their binding mode and interactions with the RT suggest that there was strong and adaptable binding in a tight (NNRTI) hydrophobic pocket. In summary, this iterative study produced structural clues and led to a group of non-toxic, novel compounds to inhibit HIV-RT with up to nanomolar potency.
4-Aminoquinoline-1,3,5-triazine: Design, synthesis, in vitro antimalarial activity and docking studies
Bhat, Hans Raj,Singh, Udaya Pratap,Gahtori, Prashant,Ghosh, Surajit Kumar,Gogoi, Kabita,Prakash, Anil,Singh, Ramendra K.
, p. 2654 - 2662 (2013/09/12)
A series of hybrid 4-aminoquinoline 1,3,5-triazine derivatives was synthesized and their chemical structure were confirmed by 1H-NMR, 13C-NMR, FT-IR and mass spectrometric analyses. In vitro antimalarial activity of these compounds was evaluated against chloroquine-sensitive (3D-7) and chloroquine resistant (RKL-2) strains of P. falciparum. Results showed that all compounds had considerable antimalarial activity against both the strains and further docking studies were performed on both wild type (1J3I.pdb) and quadruple mutant (N51I, C59R, S108 N, I164L, 3QG2.pdb) pf-DHFR-TS to quantify the structural parameter necessary for the activity.
Synthesis and antibacterial activity studies of some 2-(substitutedphenyl)- 3-bis2, 4-(4'-methylphenylamino)-s-triazine-6-ylaminobenzoylamino-5-H-4- thiazolidinone
Ahirwar, Mukesh Kumar,Shrivastava
, p. 988 - 992 (2012/07/28)
Some 4-thiazolidinone derivatives 6(a-l) have been prepared bearing s-triazine moiety by the condensation of Schiff bases from bis-2,4 (4'-methyl-phenylamino)-s-triazine-6-ylaminobenzoyl substituted benzylhydrazone 5(a-l) with thioglycolic acid. The structures of synthesized compounds have been characterized by IR, 1HNMR spectral studies. The synthesized compounds 6(a-l) have been screened for antibacterial activity.