Heterocyclic systems, which are essential in medicinal chemistry due to their promising cytotoxic activity, are one of the most important families of organic molecules found in nature or produced in the laboratory. As a result of coupling N-(4-nitrophenyl)-3-oxo-butanamide (3) using thiourea, indole-3-carboxaldehyde, or piperonal, the pyrimidine derivatives (5a and 5b) were produced. Furthermore, pyrimidine 9 was synthesized by reacting thiophene-2-carboxaldehyde with ethyl cyanoacetate and urea with potassium carbonate as a catalyst. The chalcones 11a and 11b were synthesized by reacting equal molar quantities of 1-naphthaldehyde and 2-quinoline carboxaldehyde with 4-Bromo acetophenone and 4- fluoro acetophenone respectively. Pyrimidine 13 was synthesized by reacting chalcone 11a with guanidine hydrochloride in the presence of potassium hydroxide. Pyridine derivative 14 was prepared from the reaction of chalcone 11b with ethyl cyanoacetate and ammonium acetate in glacial acetic acid. In addition, the reaction of 4-methyl benzaldehyde and 4-fluoro acetophenone with ethyl cyanoacetate and ammonium acetate in n-butanol gave pyridine derivative 16. Spectral investigations (FT-IR, 1H, and 13C-NMR) and EI-MS spectra were used to determine the structure of the prepared compounds. The synthesized derivatives were tested in vitro for their potential cytotoxicity against two different human cancer cell types, MCF-7 (breast cancer cell) or HepG2 (liver cancer cell). Compounds 5a and 14 displayed cytotoxic activity versus HepG2 cell line with IC50 values of 43.84 and 57.14 µg /mL, respectively. Furthermore, the pyridine compound 14 demonstrated cytotoxic action versus MCF-7 with an IC50 value of 50.84 g/mL. The antibacterial and anti-parasitic properties of the synthesized derivatives have also been described.
ABSTRACT
Naproxen(NPX) imprinted liquid electrodes of polymers are built using polymerization precipitation. The molecularly imprinted (MIP) and non imprinted (NIP) polymers were synthesized using NPX as a template. In the polymerization precipitation involved, styrene(STY) was used as monomer, N,N-methylenediacrylamide (N,N-MDAM) as a cross-linker and benzoyl peroxide (BPO) as an initiator. The molecularly imprinted membranes and the non-imprinted membranes were prepared using acetophenone(AOPH) and di octylphathalate(DOP)as plasticizers in PVC matrix. The slopes and detection limits of the liquid electrodes ranged from)-18.1,-17.72 (mV/decade and )4.0 x 10-
... Show MoreThe ligand 2-[1-(1H-indol-3-yl)ethylimino) methyl]naphthalene-1-ol, derived from 1-hydroxy-2-naphthaldehyde and 2-(1H-indol-3-yl)ethylamine, was used to produce a new sequence of metal ions complexes. Thus ligand reactions with NiCl2.6H2O, PdCl2, FeCl3.6H2O and H2PtCl6.6H2O were sequentially made to collect mono-nuclear Ni(II), Pd(II), Fe (III), and Pt(IV). (IR or FTIR), Ultraviolet Reflective (UV–visible), Mass Spectra analysis, Bohr-magnetic (B.M.), metal content, chloride content and molar conductivity have been the defining features of the composites. The Fe(III) and Pt(IV) complexes have octahedral geometries, while the Ni(II) complex has tetra
... Show MoreThis article includes designed and synthesized for bent-shaped liquid crystal molecules starting from 5,5-diethylpyrimidine-2,4,6(1H,3H,5H)-trione and two moles of chloroacetylchloride in N, N-dimethyl formamide (DMF) and triethylamine (TEA) to product compound [I] ,then reacted the later compound with two moles of 4-hydroxybenzonitrile to yield nitrile compound [II]. Likewise, reaction 5,5-diethylpyrimidine-2,4,6(1H,3H,5H)-trione and two moles of ethylchloroacetate with fused sodium acetate in ethanol to create an ester compound [III], and then the later compound was reacted with two moles of hydrazine hydrate in ethanol to obtained hydrazide acid compound [IV]. After that, the compound [IV] reacted with two moles of ethyl acetoacetate in
... Show MoreThe present study deals with the synthesis of four different azo-azomethine derivatives; this is done by two steps; the first step is diazotization of sulfonamides (sulfanilamide, sulfacetamide, sulfamethoxazole, and sulfadiazine) separately, followed by the second step; the coupling reaction of diazotized compounds with isatin bis-Schiff base named 3-((4-nitrobenzylidene) hydrazono)indolin-2-one. The later one (bis-Schiff base) was synthesized by the reaction of 3-hydrazono-indolin-2-one with p-nitrobenzaldehyde. The chemical structures of newly synthesized compounds were approved on the basis of their FTIR, 1H-NMR, and CHNS elemental analysis data results. The synthesized azo compounds were tested in vitro for their antimicrobial potentia
... Show MoreSome metal ions (Mn+2, Co+2, Ni+2, Cu+2, Zn+2, Cd+2 and Hg+2) complexes of quinaldic acid (QuinH) and α-picoline (α-Pic) have been synthesized and characterized on the basis of their , FTIR, (U.V-Vis) spectroscopy, conductivity measurements, magnetic susceptibility and atomic absorption. From the results obtained the following general formula has suggested for the prepared complexes [M(Quin)2( α-Pic)2].XH2O where M+2 = (Mn, Co, Ni, Cu, Zn, Cd and Hg), X = 2, X = zero for (Co+2 and Hg+2) complexes, (Quin-) = quinaldate ion, (α-Pic) = α-picoline. The results showed that the deprotonated ligand (QuinH) by using (KOH) coordinated to metal ions as bidentate ligand through the oxygen atom of the carboxylate group (-COO-) and the nitrogen ato
... Show MoreSome metal ions (Mn+2, Co+2, Ni+2, Cu+2, Zn+2, Cd+2 and Hg+2) complexes of quinaldic acid (QuinH) and α-picoline (α-Pic) have been synthesized and characterized on the basis of their , FTIR, (U.V-Vis) spectroscopy, conductivity measurements, magnetic susceptibility and atomic absorption. From the results obtained the following general formula has suggested for the prepared complexes [M(Quin)2( α-Pic)2].XH2O where M+2 = (Mn, Co, Ni, Cu, Zn, Cd and Hg), X = 2, X = zero for (Co+2 and Hg+2) complexes, (Quin-) = quinaldate ion, (α-Pic) = α-picoline. The results showed that the deprotonated ligand (QuinH) by using (KOH) coordinated to metal ions as bidentate ligand through the oxygen atom of the carboxylate group (-COO-) and the nitrogen ato
... Show MoreObjective: Benzoxazole derivatives have antifungal, anticancer, antibacterial, and anticonvulsant function. Encouraged by this comment, we agreed to synthesize new Benzoxazole compounds connected to the bases of Schiff's. Methods: 2,4-diaminophenol (1) was prepared by the reaction of 2,4-dinitrophenol and sodium dithionate. Compound (1) reacted with either acetic acid to afford compound (2) or with formic acid to afford compound (3). The Schiff bases were preparation from the reaction condensing reaction of compound (2) or (3) and aromatic aldehydes or ketone; [p-nitrobenzaldehyde, p-hydroxybenzaldehyde, p-chlorobenzaldehyde, p-bromoacetophenone and terephthaldehyde]. Results: FTIR and 1H-NMR spectroscopy characterized all of the pr
... Show MoreIn this work, N-hydroxy phthalimide derivatives (NHPID) were synthesized from the nucleuphilic substitution reactions of (NHPI) with different halides (alkyl halides, sulfonyl halides, benzoyl halides and benzyl halides). The products were distinguished using FTIR spectrum and Nuclear magnetic resonsnce (1H-NMR and 13CNMR), in addition to other characteristic methods such as sodium fution for sulfur determination. followed by measuring antibacterial (with different types of gram positive/gram negative bacteria) and antifungal activities of these compounds.
With the study of synthesizing new organic compounds and exploring biological potency. Aryldiazenyl derivatives (2-5) were carried out by coupling of diazonium salt of 4-aminoacetophenone (1) and miscellaneous active methylene compounds such as: acetylacetone, ethyl cyanoacetate, dimedone or methyl acetoacetate. Moreover substituted 1,2,3-triazole (7-9) were synthesized by the cyclization of 1-(4-azidophenyl) ethanone (6); (which was obtained by coupling of diazonium salt (1) with sodium azid); with acetylacetone, methyl acetoacetate or methyl cyanoacetate, respectively. The structures of the prepared compounds were promoted by IR, H1NMR and UV/Visible spectra. Further, they were examined in vetro for antibacterial activity against five str
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