Objective:This study involved synthesis of a new series of different five-membered heterocyclic derivatives, testing their antioxidant activity, and examining their potential in vitro antimicrobial agents. Methods: The synthesis of the derivatives involved a three-step process. Initially, succinyl chloride was reacted with methanol, followed by a reaction with 80% hydrazine hydrate through a nucleophilic addition-elimination mechanism, resulting in the formation of succinohydrazide (I). This compound was then employed as a precursor for the synthesis of Schiff bases (II), and (III) by reacting it with m-nitro benzaldehyde and p-nitro benzaldehyde. Following this, a ring closure reaction was applied using thioglycolic acid, glycolic acid, and glycine, resulting in the synthesis of different five-membered heterocyclic rings (IV–IX). Results and Discussion: The formation of the prepared derivatives was confirmed by FT-IR, 1H NMR, and 13C NMR spectroscopy. Comparative analysis with L-ascorbic acid as a standard revealed that all the prepared compounds exhibited excellent antioxidant activities. In terms of antimicrobial activity, the tested derivatives showed moderate activity against both positive and negative types of bacteria, when compared to the reference drug Ciprofloxacin. Additionally, the antifungal test showed moderate activity for all the tested compounds against a specific pathogenic fungus, with Clotrimazole being as the reference drug. The antimicrobial activity of the synthesized compounds was found to be dependent on the type of heterocyclic rings containing S, O, and N atoms. These atoms were observed to enhance antimicrobial activity by donating electrons and becoming active. Additionally, the presence of active functional groups such as C=O, NO2, and C=N contributed to this observed result. Conclusions: All of the synthesized compounds have demonstrated excellent antioxidant agents. Most of them have shown promising antimicrobial activity against certain bacteria strains, and effectiveness against a pathogenic fungus.
AASAH Enass J Waheed, Shatha MH Obaid, Research Journal of Pharmaceutical, Biological and Chemical Sciences, 2019 - Cited by 5
This work includes synthesis of new phenoxazine derivatives containing N-substituted phenoxazine starting from phenoxazine (1).10-nitrosyl phenoxazine was prepared through the reaction of phenoxazine with sodium nitrite to give compound (2), which reacted with zinc in acetic acid to give 10-amino phenoxazine (3). Condensation of compound (3) with benzoyl chloride, isovaleryl chloride and 4-bromophenacyl chloride gave 10-amido phenoxazine derivatives (4-6).
This work comprises the synthesis of new phenoxazine derivatives containing N-substituted phenoxazine starting from phenoxazine (1). Synthesis of ethyl acetate phenoxazine (2) through the reaction of phenoxazine with ethylchloroacetate, which reacted with hydrazine hydrate to give 10-aceto hydrazide phenoxazine (3), then reacted with formic acid to give 10-[N-formyl acetohydrazide] phenoxazine (4). Reaction of compound (4) with phosphorous pentaoxide or phosphorus pentasulphide to gave 10-[N-methylene-1,3,4-oxadiazole] phenoxazine (5) and 10-[N-methylene-1,3,4-thiadiazole] phenoxazine (6).
1-[4-(4-Acetyl-2-hydroxy-phenylazo)-phenyl]-ethanone (L1) and 1-[3-Hydroxy-4(4-nitro-phenylazo)-phenyl]-ethanone (L2) were readied by combination the diazonium salts of amines with 3-hydroxyacetophenone. (C.H.N) analyses, infrared spectra, UV–vis electronic absorption spectra, 1H and 13CNMR spectral mechanisms are use to identified of the ligands. Complexes of Ni+2 and Cu+2 were performed as well depicted. The formation of complexes has been identified by using atomic absorption of flame, elemental analysis, infrared spectra and UV-Vis spectral process as well conductivity and magnetic quantifications. Nature of compounds produced have been studied obeyed the mole ratio and continuous contrast methods, Beer's law followed during a concent
... Show MoreIn this work, a series of new maleimides linked to substituted benzothiazole moiety were synthesized. Synthesis of these new cyclic imides were performed via three steps, the first one involved preparation of a series of 2-aminobenzothiazole substituted with different substituents via reaction of different primary aromatic amines with ammonium thiocyanate and bromine in glacial acetic acid. The prepared 2- amino benzothiozoles were introduced in the second step in reaction with maleic anhydride producing a series of N-(substituted benzothiazole-2-yl) maleamic acids.The resulted maleamic acids were dehydrated in the third step via treatment with acetic anhydride and anhydrous sodium acetate to afford a series of the desirable N-(substitu
... Show MoreMetronidazole-MIPs were prepared by using (MDZ) as the template as well as allylchloride (AYC) or allylbromide (AYB) as monomer, used (TMPTA) tri-methylol propane tri-acrylate or ethylene glycol di-methyl acrylate (EGDMA) as cross-linker and initiator used (BP) benzyl peroxide. By using different plasticizers (di butyl Phthalate (DBPH), Nitrobenzene (NB), oleic acid (OA) and paraffin) for MDZ-MIP1 and (Di-butyl sebecate (DBS), Di-methyl acrylate (DMA), Tributylphosphate(TBP) and Tris(ethylhexyl phosphate (TEHP) ) for MDZ-MIP2. Membranes of MIPs were prepared in PVC matrix. The characterizations of each electrode were determined The Slope range from (55.083 - 43.711) mV/decade, Limit of Detection (8 X 10 -4- 2 X 10-6) and Linearity
... Show MoreBackground: Oral diseases persist to be a major health problem all over the world. Various bacteria and fungi are found to be the possible pathogensresponsible for the oral diseases. Moringa oleifera it is an extraordinary nutritious vegetable tree with many different uses. These leaves have high medicinal value. In the present study, antibacterial and antifungal activities of aqueous extracts of plant Moringa oleifera in comparison to chlorohexidene gluconate and deionized water were determined. Materials and methods: The leaves of plant of Moringa oleifera were collected from College of Pharmacy; Baghdad, Iraq. Tested microorganism (bacterial and fungal) was isolated from different clinical specimens. In-vitroantimicrobial activity was pe
... Show MoreMn(II), Co(II), Ni(II), Cu(II), and Cr(III) metal complexes with the ligand (L) [3-(2nitro benzylidene) amino-2-thioxoimidazolidin-4-one] have been prepared and characterized in their solid state using the elemental micro analysis (C.H.N.S), flame atomic absorption, UV-Vis spectroscopy, FT-IR, magnetic susceptibility measurements, and electrical molar conductivity. The ratio of metal to ligand [M:L] was got for all complexes in the ethanol by using the molar ratio method, which produced comparable results with those results obtained for the solid complexes. From the data of all techniques, octahedral geometry was proposed for Cr(III), Mn(II), and Co(II) complexes, while tetrahedral structure was proposed for Ni(II), Cu(II) complexes.
The present study was carried out to determine the bacterial isolates and study their antimicrobial susceptibility in case of burned wound infections. 70 burn wound swabs were taken from patients, who presented invasive burn wound infection from both sex and average age of 3-58 years, admitted to teaching medical Al- Kendi hospital from October 2007 to June 2008. Pseudomonas aeruginosa was found to be the most common isolate (48.9%) followed by Staphylococcus aureus (24.4%), Citrobacter braakii (13.3%), Enterobacter spp. (11.1%), Coagulase-negative Staphylococci (11.1%), Proteus vulgaris (6.66%), Corynebacterium spp. (6.66%), Micrococcus (6.66%), Proteus mirabilis (4.44%), Enterococcus faecalis (4.44%), E.coli (4.44%), Klebsiella spp. (2.22
... Show MoreA new series of Sulfamethoxazole derivatives was prepared and examined for antifibrinolytic and antimicrobial activities. Sulfamethoxazole derivatives bear heterocyclic moieties such as 1,3,4-thiadiazine {3}, pyrazolidine-3,5-diol {4} 6-hydroxy-1,3,4-thiadiazinane-2-thione {5} and [(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-yl)diazenyl] {8}. Their structures were elucidated by spectral methods (FT-IR, H1-NMR). Physical properties are also determined for all compound derivatives. Recently prepared compounds were tested for their antimicrobial activity in the laboratory. Each screened compound showed good tendency to moderate antimicrobial activity.