Synthesis, pharmacological and biological screening of some novel pyrimidine derivatives

In the present study a new series of 4-substituted phenyl-6-(pyridin-2-yl)pyrimidin-2-ol ( 1 – 9 ) and 4-substituted phenyl-6-(pyridin-2-yl)pyrimidin-2-thiol ( 10 – 18 ) have been synthesized by cyclizing 3-substituted phenyl-1-(pyridin-2-yl)prop-2-en-1-one with urea/thiourea in the presence of NaOH...

Full description

Saved in:
Bibliographic Details
Published in:Medicinal chemistry research 2014-07, Vol.23 (7), p.3458-3467
Main Authors: Ishwar Bhat, K., Kumar, Abhishek, Nisar, Muhammed, Kumar, Pankaj
Format: Article
Language:English
Subjects:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Original Research
Pharmacology/Toxicology
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:In the present study a new series of 4-substituted phenyl-6-(pyridin-2-yl)pyrimidin-2-ol ( 1 – 9 ) and 4-substituted phenyl-6-(pyridin-2-yl)pyrimidin-2-thiol ( 10 – 18 ) have been synthesized by cyclizing 3-substituted phenyl-1-(pyridin-2-yl)prop-2-en-1-one with urea/thiourea in the presence of NaOH as base ( 1a – 18a ). 3-Substituted phenyl-1-(pyridin-2-yl)prop-2-en-1-one was prepared by condensing 2-acetylpyridine with substituted benzaldehyde in the presence of 20 % NaOH as base. The structures of the newly synthesized compounds were characterized by elemental analysis, IR, 1 H NMR, 13 C NMR, and mass spectroscopic studies. Newly synthesized compounds were screened for their anti-inflammatory, analgesic, cytotoxic, and antitubercular activities studies. Few of the compounds exhibited excellent anti-inflammatory activities compared to standard drug diclofenac sodium. Some compounds have shown moderate analgesic activities compared to standard drug pentazocine. Also, some compounds have exhibited moderate cytotoxic and antitubercular activities.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-014-0914-3