Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.


In continuation of our efforts toward identification and optimization ...
In continuation of our efforts toward identification and optimization for novel non-nucleoside reverse transcriptase inhibitors (NNRTIs) project, we have employed a structure-based bioisosterism strategy, with which, a new series of diarylpyridazine (DAPD) derivatives were synthesized and evaluated for their anti-HIV-1 (human immunodeficiency virus type 1) activity. Most of the title compounds displayed excellent anti-HIV-1 activitiy at submicromolar concentrations ranged from 34nM to 5.08μM. The most promising compound 8g inhibited HIV-1 IIIB in MT-4 cells with low EC(50) value (0.034μM), which was higher than the reference drugs nevirapine and delavirdine. The structure activity relationships (SARs) were discussed and rationalized by docking simulations.




new topics/pols set partial results complete validated


No results available for this paper.

Entry validated by:

Using Polbase tables:


Tables may be sorted by clicking on any of the column titles. A second click reverses the sort order. <Ctrl> + click on the column titles to sort by more than one column (e.g. family then name).


It is also possible to filter the table by typing into the search box above the table. This will instantly hide lines from the table that do not contain your search text.