Synthesis and Anti‐HIV‐1 Integrase Activitiy of Cyano Pyrimidinones | Zendy

Ramajayam R. | Zendy; Mahera Nilesh B. | Zendy; Neamati Nouri | Zendy; Yadav Mange Ram | Zendy; Giridhar Rajani | Zendy

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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).

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