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Synthesis and Anti‐HIV‐1 Integrase Activitiy of Cyano Pyrimidinones
Author(s) -
Ramajayam R.,
Mahera Nilesh B.,
Neamati Nouri,
Yadav Mange Ram,
Giridhar Rajani
Publication year - 2009
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200900066
Subject(s) - pyrimidinones , integrase , chemistry , recombinant dna , enzyme , integrase inhibitor , human immunodeficiency virus (hiv) , virology , stereochemistry , biochemistry , biology , viral load , antiretroviral therapy , gene
A series of 2‐phenethyl/benzylthio‐6‐oxo‐4‐phenyl‐1,6‐dihydropyrimidine‐5‐carbonitrile were synthesized and tested against recombinant HIV‐1 integrase in an enzyme assay. 2‐(Phenethylthio)‐4‐(4‐chlorophenyl)‐6‐oxo‐1,6‐dihydropyrimidine‐5‐carbonitrile 4m and 2‐(phenethylthio)‐4‐(3‐chlorophenyl)‐6‐oxo‐1,6‐dihydropyrimidine‐5‐carbonitrile 4o showed significant inhibition against integrase in the assay (strand transfer: IC 50 values of 16 and 17 μM, respectively).