Eighteen new cyclic imides (maleimides) conncted to benzothiazole moiety through sulfonamide group were synthesized via multistep synthesis.The first step involved preparation of two maleamic acids N-phenylmaleamic acid and N-benzylmaleamic acid via reaction of maleic anhydride with aniline or benzyl amine.Dehydration of the prepared amic acids by treatment with acetic anhydride and anhydrous sodium acetate in the second step afforded N-phenylmaleimide and N- benzyl maleimide which in turn were treated with chlorosulfonic acid in the third step to afford 4-(N-maleimidyl) phenyl sulfonyl chloride and 4-(N-maleimidyl) benzyl sulfonyl chloride respectively.In the Fourth step of this work each one of the two prepared maleimidyl sulfonyl chlorides was introduced in reaction with nine substituted-2-amino benzothiazole compounds producing nine N-(4-(N-substituted benzothiazole -2-yl) sulfonamido phenyl) maleimides and nine N-(4-(N-substituted benzothiazole-2-yl)snlfonamido benzyl) maleimides.More over another new six sulfonamide phenyl and benzyl maleimides substituted with other heterocycles (pyridine and phenazone )were prepared via reaction of 4-(N-maleimidyl) phenyl and benzyl sulfonyl chlorides with heterocyclic amines including (2-amino pyridine,4-amino-pyridine,4-aminophenazone). Microbiological activity of the prepared compounds against two typs of bacteria(staphylococcus aureus and klebsiella pneumonia) and (candida albicans) fungi were evaluated and the results showed that these compounds have good antibacterial and good antifungal activities.
New Fourteen compounds were synthesized in four steps. The first step included synthesis of 2-biphenyl fused ring of imidazo(1,2- a)pyrimidine from the reaction of 2-aminopyrimidine and biphenyl phenacyl bromide . The second step was introduced aldehyde group from the reaction of 2-biphenyl fused rings of imidazo(1,2-a)pyrimidine with POCl3 in presence of DMF and CHCl3. 3-Carbaladehyde derivatives of fused imidazo/pyrimidine was reacted with different aromatic amines to afford new Schiff bases. These new 3- imines derivatives was reduced by using sodiumborohydride to yield another new 3-aminomethyl-2-biphenyl imidazo (1,2-a)pyrimidine derivatives in moderate yield .Some new prepared compounds were identified by melting point, FT- IR , 13C-
... Show MoreThe synthesis of the bisaldehyde ligand 2-(1,1-dimethyl-1,3-dihydro-2H-benzo[e]indol-2-ylidene)malonaldehyde (B) and its coordinated compounds with Cr(III), Mn(II), Fe(II), Co(II), Ni(II) and Cu(II) ions are reported. The synthetic route of B was completed by adopting the Vilsmeier-Haack reaction. This was based on the mixing of 1,1,2-trimethyl-1H-benzo[e]indole with phosphoryl trichloride and N, N-dimethylformamide (anhydrous) that gave the aminomethylenemalondialdehyde. The use of POCl3 and DMF was aimed to give the Vilsmeier-Haack intermediate, which was kept at 5°C and then heated with stirring at 85°C. The addition of an aqueous NaOH solution (35%) to the reaction mixture resulted in the isolation of B. The monomeric coordinated comp
... Show MoreThis study reports the formation, characterisation and biological evaluation of a Schiff base ligand and its corresponding metal complexes. The Schiff base ligand (HL) was prepared through a condensation reaction involving isonicotinohydrazide and N'-((1R,2R,4R,5S, E)-2,4-bis(4-chlorophenyl)-3-azabi cyclo[3.3.1]nonan-9-ylidene) isonicotinohydrazide (M) in EtOH solvent and (3-5) drops of conc. HCl. The interaction of HL with selected metal chlorides including Mn(+2), Co(+2), Ni(+2), Cu(+2) and Zn(+2) in a 2:1 (L:M) mole ratio resulted in the synthesis of complexes with the general formula [M(HL)Cl2] (where: M = Mn(+2),Co(+2) and Ni(+2)) and [M`(HL)Cl2] (where M` = Cu(+2) and Zn(+2)). The characterisation of the prepared compounds w
... Show MoreThe aim of this research is to prepare a set of complexes with the general formula [M(HMB)n] , where M=VO (II) , Cr(III) and Cu(II) while n=2,3,2 respectively resulting from the reaction of anew ligand [N'-(2-hydroxy-3-methoxybenzyl)-4-methylbenzohydrazide] (HMB) derived from the reaction of the tow substances (4-methylbenzohydrazide and 2-hydroxy-3-methoxy benzaldehyde) with metal ions. The prepared compounds were identified by several spectroscopic methods such as Infrared, Nuclear Magnetic Resonance and Electronic Spectra. From the results of the measurements, it was suggested that the prepared complexes have different geometries such as square planar (Cu), square pyramidal (VO) and octahedral (Cr). DFT simulations backed up
... Show MoreTransition metal complexes of Co(II) and Ni(II) with azo dye 3,5-dimethyl-2-(4-nitrophenylazo)-phenol derived from 4-nitoaniline and3,5-dimethylphenol were synthesized. Characterization of these compounds has been done on the basis of elemental analysis,electronic data, FT-IR,UV-Vis and 1 HNMR, as well as magnetic susceptibility and conductivity measurements. The nature of thecomplexes formed were studies following the mole ratio and continuous variation methods, Beer ' s law obeyed over a concentrationrange (1x10 -4 - 3x10 -4 M). High molar absorbtivity of the complex solutions were observed. From the analytical data, thestoichiomerty of the complexes has been found to be 1:2 (Metal:ligand). On the basis of physicochemical data tetrahedral
... Show MoreSynthesis, Characterization And Biological Evaluation of Schiff Base And Ligand Metal Complexes of Some Drug Substances
Schiff bases (Sh1-Sh3) have been synthesized (p-aminophenol) was condensed with different aromatic aldehyde in ethanol inthe presence of glacial acetic acid as catalyst. These Schiff bases on treatment with monochloroacetyl choride gave 3-chloro-1-(4-hydroxyphenyl)-4-(substituted)azetidin-2-one(Az4-Az6), with αmercaptoacetic acid gave 3-(4-hydroxyphenyl)-2-( substituted)thiazolidin-4-one (Th7-Th9) and with anthranilic acid gave 3-(4-hydroxyphenyl)-2(substituted)-2,3-dihydroquinazolin-4(1H)-one (Qu10-Qu12). The purity of the derivatives was confirmed by TLC. The some compoundsidentify by (FT-IR and1H, 13C-NMR) data. Some of derivatives were evaluated activity against several microbesto determine ability to inhibit bacterial in some h
... Show MoreSchiff bases (SBs) based on amino acid derivative stand for multipurpose ligands that formed by condensing amino acids with carbonyl groups. They are significant in pharmaceutical and medical areas due to their widespread biological actions such as antiseptic, antifungal, along with antitumor actions. Transition metallic complexes resulting from SB ligands with biological activity were extensively experimented in the literature. In this article, we review, in details, about synthesizing and biological performances of SBs along with its complexes.