Synthesis

ABSTRACTThe substituted 4-(bromomethyl)-N-(4-ethyl-6-methylpyrimidin-2-yl) benzamide derivatives 6a-k has been synthesis from reaction in between substituted 4-ethyl-6-methylpyrimidin-2-amine and 4-(bromomethyl)benzoyl bromide 5 in presence of KOH. Type of aldol condensation reaction in between aldehydes and ketones to form ?,?-Unsaturated carbonyl compounds3 this compound has been reacted with guanidine in presence of dry alcohol to convert 4-ethyl-6-methylpyrimidin-2-amine4.Chemical structures of all the new compounds were established by IR, 1H, 13C NMR, MS and elemental data. The compounds 6a-k were evaluated for their antibacterial activity against Gram-positive bacteria viz.  Bacillus subtilis, Bacillus sphaericus and Staphylococcus aureus, and three Gram-negative bacteria viz. Pseudomonas aeruginosa, Klebsiella aerogenes and Chromobacterium violaceum  and also evaluate their antifungal activity against Candida albicans (C.albicans)(ATCC 10231), Aspergillus fumigates(A.fumigatus) (HIC 6094), Trichophyton rubrum(T. rubrum) (IFO 9185), and Trichophyton mentagrophytes(T. mentagrophytes) (IFO 40996) Amongst them, compounds containing [3-hydrophenyl] moiety 6d, [3-chlorophenyl] moiety 6f and [4-nitrophenyl] moiety 6h showed significant antibacterial and antifungal activity, almost equal/more than the activity of the standard drugs Streptomycin and Amphotericin-B. Further, the compounds 6a-k were also screened for Most of these new compounds showed appreciable activity against test bacteria and fungi and emerged as potential molecules for further development. Keywords: Synthesis,4-(bromomethyl)-N-(4-ethyl-6-methylpyrimidin-2-yl) Benzamide, antibacterial activity, antifungal activity.  

Chalcones are commonly found in fruit, vegetables, nuts, seeds, stems and flowers. For centuries, preparations containing these compounds as the principal bioactive constituents have been used to treat human diseases. Increasingly, this class of natural products is becoming the subject of antimicrobial research, and many groups have isolated and identified the structures of chalcones. However, several high-quality investigations have examined the relationship between chalcone structure and antibacterial activity and these are in close agreement. In addition, numerous research groups have sought to elucidate the antibacterial mechanisms of action of selected chalcones. Hence a series of some new chalcones have been synthesized by condensation of 3-acetyl-thiophene with various aromatic aldehydes in 40% alkali. The synthesized compounds were identified by spectral data and screened for antimicrobial activity.  Some of these compounds showed moderate to considerable anti-microbial activity. Key words: Chalcone, Synthesis, antimicrobial activity.