Singh K., Singh K., Wan B., Franzblau S., Chibale K., Balzarini J.
Organic Synthesis Laboratory, Department of Applied Chemical Sciences and Technology, Guru Nanak Dev University, Amritsar 143005, India; Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612-723, United States; Department of Chemistry, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa; Rega Institute for Medical Research, Katholieke Universiteit Leuven, 10 Minderbroedersstraat, B-3000 Leuven, Belgium
Singh, K., Organic Synthesis Laboratory, Department of Applied Chemical Sciences and Technology, Guru Nanak Dev University, Amritsar 143005, India; Singh, K., Organic Synthesis Laboratory, Department of Applied Chemical Sciences and Technology, Guru Nanak Dev University, Amritsar 143005, India; Wan, B., Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612-723, United States; Franzblau, S., Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612-723, United States; Chibale, K., Department of Chemistry, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa; Balzarini, J., Rega Institute for Medical Research, Katholieke Universiteit Leuven, 10 Minderbroedersstraat, B-3000 Leuven, Belgium
A series of pyrimidine derivatives bearing amine substituents at C-2 position were obtained from Biginelli 3,4-dihydropyrimidin-2(1H)-ones and the effect of structural variation on anti-TB activity against Mycobacterium tuberculosis H37Rv strain and antiviral activity in a series of cell cultures was evaluated. While the compounds were found to possess structure dependent cytostatic activity, these were not found to be efficient inhibitors of M. tuberculosis nor did they inhibit a broad variety of DNA or RNA viruses in cell culture. © 2011 Elsevier Masson SAS.
2 (2 hydroxyphenylamino) 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 (3 aminophenylamino) 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 (3 hydroxypropylamino) 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 (4 hydroxyphenylamino) 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 (piperidin 1 yl) 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 [2 (1h indol 3 yl) ethylamino] 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 amino 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 amino 4 methylpyrimidine 5 carboxylic acid ethyl ester; 2 benzylamino 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 benzylamino 4 methylpyrimidine 5 carboxylic acid ethyl ester; 2 butylamino 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 ethoxy 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 isopropylamino 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; 2 morpholino 4 methyl 6 phenylpyrimidine 5 carboxylic acid ethyl ester; pyrimidine derivative; pyrimidinone derivative; unclassified drug; animal cell; antiviral activity; article; bacterial strain; Biginelli reaction; cell culture; cell proliferation; controlled study; cytostasis; drug structure; drug synthesis; human; human cell; in vitro study; minimum inhibitory concentration; Mycobacterium tuberculosis; nonhuman; tuberculosis; Animals; Antitubercular Agents; Cell Proliferation; Drug Screening Assays, Antitumor; Hela Cells; Humans; Mice; Molecular Structure; Mycobacterium tuberculosis; Pyrimidines; Stereoisomerism; Structure-Activity Relationship; Tumor Cells, Cultured