244272-07-9Relevant academic research and scientific papers
DISUBSTITUTED TRIAZINE DIMERS FOR TREATMENT AND/OR PREVENTION OF INFECTIOUS DISEASES
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, (2014/11/11)
The present invention relates to novel compounds (I) containing two disubstituted triazine rings covalently linked by an organic linker, thereby creating dimers. These compounds show activity against the causative infective agents of infectious diseases s
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds
Venkatraj, Muthusamy,Arin, Kevin K.,Heeres, Jan,Joossens, Jurgen,Diri, Bertrand,Lyssens, Sophie,Michiels, Johan,Cos, Paul,Lewi, Paul J.,Vanham, Guido,Maes, Louis,Van Der Veken, Pieter,Augustyns, Koen
, p. 5241 - 5248 (2014/12/11)
The presence of a structural recognition motif for the nucleoside P2 transporter in a library of pyrimidine and triazine non-nucleoside HIV-1 reverse transcriptase inhibitors, prompted for the evaluation of antitrypanosomal activity. It was demonstrated that the structure-activity relationship for anti-HIV and antitrypanosomal activity was different. Optimization in the diaryl triazine series led to 6-(mesityloxy)-N2-phenyl-1,3,5-triazine-2,4-diamine (69), a compound with potent in vitro and moderate in vivo antitrypanosomal activity.
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility
Bollini, Mariela,Cisneros, José A.,Spasov, Krasimir A.,Anderson, Karen S.,Jorgensen, William L.
, p. 5213 - 5216 (2013/09/12)
Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine and rilpivirine, while retaining high anti-viral activity. The solubility enhancements come from strategic placement of a morpholinylalkoxy substituent in the entrance channel of the NNRTI binding site. Compound 4d shows low-nanomolar activity similar to etravirine towards wild-type HIV-1 and key viral variants.
DISUBSTITUTED TRIAZINE DIMERS FOR TREATMENT AND/OR PREVENTION OF INFECTIOUS DISEASES
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, (2013/05/23)
The present invention relates to novel compounds (I) containing two disubstituted triazine rings covalently linked by an organic linker, thereby creating dimers. These compounds show activity against the causative infective agents of infectious diseases s
HIV replication inhibitors
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, (2008/06/13)
This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, provided that when Q is halo then Z is N; or when Q is polyh
Evolution of anti-HIV drug candidates. Part 2: Diaryltriazine (DATA) analogues
Ludovici, Donald W.,Kavash, Robert W.,Kukla, Michael J.,Ho, Chih Y.,Ye, Hong,De Corte, Bart L.,Andries, Koen,De Bethune, Marie-Pierre,Azijn, Hilde,Pauwels, Rudi,Moereels, Henry E.L.,Heeres, Jan,Koymans, Lucien M.H.,De Jonge, Marc R.,Van Aken, Koen J.A.,Daeyaert, Frederik F.D.,J. Lewi, Paul,Das, Kalyan,Arnold, Edward,Janssen, Paul A.J.
, p. 2229 - 2234 (2007/10/03)
A synthesis program directed toward improving the stability of imidoyl thiourea based non-nucleoside reverse transcriptase inhibitors (NNRTIs) led to the discovery of diaryltriazines (DATAs), a new class of potent NNRTIs. The synthesis and anti-HIV struct
