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.
The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an
... Show MoreRecently, some prostate cancer patients have acquired resistance to the second -generation drugs (anzalutamide and apalutamide) prescribed for the treatment of this disease due to the emergence of the F876L mutation, which represents a challenge to modern medicine. In this study, a new series of 2-thiohydantoin derivatives were prepared through the reaction of different derivatives of maleimide (1c-4c) with isothiocyanate derivatives. The prepared compounds were diagnosed using FT-IR,1H-NMR ,13C-NMR, Mass spectra. The prepared series compounds has been studied against prostate cancer cells. The MTT assay was used to determine the activity of the prepared compounds against prostate cancer cells. The da
... Show MoreBackground: Enforcement of sustainable and green chemistry protocols has seen colossal surge in recent times, the development of an effective, eco-friendly, simple and novel methodologies towards the synthesis of valuable synthetic scaffolds and drug intermediates. Recent advances in technology have now a more efficient means of heating reactions that made microwave energy. Efforts to synthesize novel heterocyclic molecules of biological importance are in continuation. Microwave irradiation is well known to promote the synthesis of a variety of organic and inorganic compounds. The aim of current study was to conceivea mild base mediated preparation of novel Schiff base of 2-Acetylpheno with trimethoprim drug (H2TPBD) and its complexes w
... Show MoreMetallic nanoparticles are increasingly studied for their biomedical applications due to their unique physicochemical and catalytic properties. Here, a broccoli-mediated gold/platinum nanohybrid (Au@Pt NH) was synthesized using an ultrasound-assisted green method with an aqueous extract of Brassica oleracea var. italica for multifunctional biomedical evaluation. XRD and TEM confirmed a crystalline nanohybrid with an average crystallite size of 7.56 nm and a mean particle diameter of 13.08 ± 7.58 nm. The broccoli extract produced no inhibition zones, whereas Au@Pt NH inhibited Staphylococcus aureus (18 mm), Staphylococcus epidermidis (21 mm), Escherichia coli (18 mm), Klebsiella pneumoniae (20 mm), and Candida albicans (21 mm). In vivo,
... Show MoreSome new heterocyclic compounds containing, cyclohexenone, indazole, isoxazoline, pyrmidine and pyrazoline ring system were prepared from chalcones (1a,b). The starting chalcones (1a,b) were obtained by a base catalyzed condensation of appropriately substituted benzaldehydes and 2-acetylbenzofuran. The reaction of the prepared chalcones with ethylacetoacetate/hydrazine hydrate, hydroxylamine hydrochloride, urea, thiourea, hydrazine hydrate, phenyl hydrazine or hydrazide derivatives gave the mentioned heterocycles. All synthesized compounds have been characterized by physical and spectral methods.
Schiff base of chitosan with Para-Dimethyl aminobenzaldehyde /PVA-Ag Nanocomposite have been prepared as antimicrobial polymer. The prepared chitosan Schiff base and chitosan Schiff base / PVA-Ag nanocomposite were characterized by FT-IR, SEM analysis and biological activity. The nanocomposite showed good activity against different types of bacteria.
Two new ligands Na2[ H3B (BDIA)].0.05H2O (L1)(BDIA = 1-Boranyl-2,3-
Dihydro-1H-Indol-3-yl)]Acetic Acid and Na3[H2B(BDIA)2].0.3H2O.0.3CH3Ph (L2)
were synthesized by reaction of NaBH4 with indole -3- acetic acid (IAA) . The
coordination properties of ligands were studied with Co(II) , Ni(II) , Cu(II) and
Pt(IV) ions. Characterization and structural aspects of the prepared compounds were
elucidated by 1HNMR, FTIR electronic spectra, magnetic susceptibility, elemental
and metal analysis, thermal analysis (TG & DTG) and conductivity measurements.
The obtained data for metal complexes suggested square planar geometry for
copper complexes, octahedral geometry for nickel and platinium complexes and
tetrahedral geom
Darifenacin hydrobromide (DH) is the more recent uroselective M3 receptor antagonist for treating uncomplicated overactive bladder (OAB). This study was aimed to formulate DH as fast dissolving buccal films (FDBFs) using a solvent casting method to enhance patient’s compliance.
Films were prepared by using polyvinyl alcohol (PVA) as a film forming polymer. Different types and concentrations of superdisintegrants (croscarmellose sodium, sodium starch glycolate, indion 414) were used to select the best formula by studying the physicochemical properties of the films, disintegration time (DT) and percent drug release.
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... Show MoreNew heterocyclic compounds derived from 2-Morpholino-1,8-naphthyridine-4-carboxylic acid such as oxadiazolo, thiadiazolo – thione and triazolo-thione have been prepared and characterized on the basis of IR and 1H NMR spectra data. The hydrizide compound was utilized as a starting material for preparing of these compounds. The second part of this study involves the biological studies of some of these naphthyridine derivatives by using three different kinds of bacteria namely: Staphylococcus aureus, Pseudomonas aeruglnosa and Escherichia coli. The data indicated that some of these compounds have a good activity against the tested bacteria in comparison to antibiotics.
Carbazone Derivatives (CD) (semicarbazone, semithiocarbasone) are produced by the condensation reaction between a aldehyde (or ketone) with a carbazide derivatives (semicarbazide, semithiocarbazide). CD and their metal complexes existent a wide range of implementation that stretch from their ply in the medicinal and pharmaceutical area because of their major significant pharmacological characteristic such as anti-fungal,anti-bacterial, anti-cancer, anti-human immunodeficiency virus, anti-inflammation, anti-neoplastic,inhibition corrosion, antioxidation, antiradical. This paper reviews the definition, importance and various applications of carbazone derivatives with transitional meta