TY - JOUR
T1 - Synthesis, antitumor and antibacterial activities of certain substituted pyrimidines bearing benzofuran
AU - Babu, V.H.
AU - Kumar, P.S.
AU - Srinivasan, K.K.
AU - Bhat, G.V.
N1 - Cited By :9
Export Date: 10 November 2017
CODEN: IJSID
Correspondence Address: Babu, V. H.; Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, MAHE, Manipal-576104, India; email: harinadhababu_v@yahoo.com
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PY - 2004
Y1 - 2004
N2 - Benzofuran chalcones (2a-i) were prepared by the reaction of 2-acetylbenzofuran (1) with different aromatic aldehydes in the presence of a strong base. Cyclocondensation of benzofuran chalcones with guanidine hydrochloride, thiourea and urea resulted in the formation of various aminopyrimidines (3a-i), thiopyrimidines (4a-i) and hydroxy pyrimidines (5a-i), respectively. The structures of all the compounds (2,3,4,5 a-i) have been established on the basis of analytical and spectral data. All the compounds have been screened for antitumour and antimicrobial activities. Compounds 3b and 3d showed significant antitumour activity. While compounds 4d and 4h showed only moderate activity against Staphylococcus aureus at 500 μg/ml, compounds 4h, 4i, 5a, 5b, 5h and 5i showed promising activity against Candida albicans at 500 μg/ml concentrations.
AB - Benzofuran chalcones (2a-i) were prepared by the reaction of 2-acetylbenzofuran (1) with different aromatic aldehydes in the presence of a strong base. Cyclocondensation of benzofuran chalcones with guanidine hydrochloride, thiourea and urea resulted in the formation of various aminopyrimidines (3a-i), thiopyrimidines (4a-i) and hydroxy pyrimidines (5a-i), respectively. The structures of all the compounds (2,3,4,5 a-i) have been established on the basis of analytical and spectral data. All the compounds have been screened for antitumour and antimicrobial activities. Compounds 3b and 3d showed significant antitumour activity. While compounds 4d and 4h showed only moderate activity against Staphylococcus aureus at 500 μg/ml, compounds 4h, 4i, 5a, 5b, 5h and 5i showed promising activity against Candida albicans at 500 μg/ml concentrations.
M3 - Article
SN - 0250-474X
VL - 66
SP - 647
EP - 652
JO - Indian Journal of Pharmaceutical Sciences
JF - Indian Journal of Pharmaceutical Sciences
IS - 5
ER -