Synthesis and Characterization of some New 2-Methyl-3-N-Substituted Imino - 5, 6-Tetramethylene Thieno [2, 3-D]-Pyrimidin (3h)–4-ones for Anti-bacterial and Antifungal screening
Journal Title: Hygeia:journal for drugs and medicines - Year 2015, Vol 7, Issue 1
Abstract
Plan: To synthesize some Schiff bases of 2-Methyl-3-N-amino-5, 6-disubtituted thieno [2, 3-d] - pyrimidin (3H)-4-ones for antibacterial and antifungal activities. Preface: Organic compounds containing thiophene and pyrimidine form a significant group of drugs and known for pharmacological activities having various therapeutic applications. The compounds containing Thieno(2,3-b) pyrimidine nucleus posses broad range of pharmacological activities namely antibacterial, antifungal, trichomicidal, anti-malarial, anti-inflammatory activity ,etc.Thus a new series of Thieno[2,3-d]- pyrimidinones have been synthesized by reacting the active 3-amino group with various substituted aryl aldehydes and screened for antibacterial and antifungal activity. Methodology: In our present investigation we have prepared the intermediate S-2 starting from cyclohexanone and ethyl cyano acetate, involving the elegant method described by Gewald et.al. This compound S-2 was treated with acetic anhydride followed by hydrazine hydrate to yield the parent compound RJ-2.This compound was derivatized to various Schiff bases by treating with various substituted aryl aldehydes. The synthesized title compounds were characterized by MP, TLC, UV and a few representative compounds by IR, NMR & Mass spectrum. The compounds were screened for antibacterial and antifungal activity. Outcome: The new title compounds possessing ‘electron withdrawing groups’ on the aldehydic phenyl ring (RJ-2d, RJ-2j, RJ-2f, RJ-2l) exhibited better antibacterial and antifungal activity compared to the compounds possessing ‘electron donating groups’(RJ-2e, RJ-2k, RJ-2m)
Authors and Affiliations
S Ramamurthy, E Jayachandran
Keywords
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- EP ID EP401493
- DOI 10.15254/H.J.D.Med.7.2015.142
- Views 49
- Downloads 0
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