Sulfamethoxazole (SMX) is the most significant antibiotic in the sulfonamide family. It was chosen as the representative of this category because of its widespread use. Starting with sulfamethoxazole, a new series of 2-Azetidinone (M1-M6) was synthesized, the structure of these new derivatives was confirmed using spectral methods, starting with the synthesis of Schiff’s bases by reflux of different aromatic benzaldehydes, separately, with Sulfamethoxazole in ethanol with few drops of acetic acid. The final compounds were obtained by ketene-imine synthesis of β-lactam using chloroacetyl chloride. The designed chemicals’ synthesis has been completed successfully. Physical parameters (melting points and Rf values), Fourier transform infrared (FT-IR) spectroscopy, and Proton nuclear magnetic resonance (1H-NMR) spectroscopy were used to establish the purity and characterization of these derivatives. When compared to standard antibiotics (Sulfamethoxazole, Ciprofloxacin, and Fluconazole), the preliminary antimicrobial activity tests on four different bacteria strains and one type of fungus demonstrated that the final compounds (M1-M6) have significant activity. Finally, the new derivatives (M3 and M5) are the most potent than the other ones and more active than the standard drugs.
4-amino-3-(4-(((4-hydroxy-3, 5dimethoxybenzyl) oxy) methyl) phenyl)-1, 2, 4-triazole-5-thione was synthesized by to method the first one from melt reaction of 4-(((4-hydroxy-3, 5-dimethoxybenzyl) oxy) methyl) benzoic acid with Thiocarbonyldihydrazide, the second method from convert the corresponded acid hydrazide to potassium 2-(4-(((4-hydroxy-3, 5-dimethoxybenzyl) oxy) methyl) benzoyl) hydrazinecarbodithioate salt then react with hydrazine hydrate. Newly Schiff base (7a-7f) were synthesized from reaction the 4-amino-1, 2, 4-triazol with substituted hydroxybenzaldehyde. The resulting compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS data. 2, 2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays
... Show MoreIn the present study, ( Schiff's bases 6a - 6e) and (new amids derivatives 6f - 6j) have been synthesized . The glutaroyl chloride(2) has been prepared by the reacting of glutaric acid and thionyl chloride in presence of (DMF) . The new compound bis(4-formylphenyl) glutarate (3) has been Synthesized from reaction of one mole of glutaroyl chloride and two moles of 4-hydroxybenzaldehyde . Compound 4,4'-(glutaroylbis(oxy))dibenzoic acid (4) was Synthesized from one mole of glutaroyl chloride and two moles of 4-hydroxybenzoic acid, while compound bis(4-(chlorocarbonyl)phenyl) glutarate (5) was prepared from 4,4'-(glutaroylbis(oxy))dibenzoic acid and Thionyl chloride . Then Schiff's bases 6a - 6e that prepared
... Show MoreNew 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 MoreObjective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the anticancer activities. Methods: Baclofen was initially reacted with aromatic aldehydes to create Schiff base derivatives (Ia–Ib), which were then closed in the next step using anhydrous acids to form oxazepine derivatives (IIa–IId). Results: The title compounds were synthesized successfully and identified using FT-IR, 1H NMR, and 13C NMR spectroscopy. Additionally, compound (IIc)’s (3-(4-chloro-phenyl)-4-[2-(4nitro-phenyl)-4,7-dioxo-4,7-dihydro-[1,3] oxazepin-3-yl]butyric acid) anticancer activity was assessed using MTT assay against FTC-133 (thyroid cancer) compared with WRL-68 (normal cell line). Discus
... Show MoreWe described herein the synthesized and characterized of new bent and liner core compounds containing thiazolidin-4-one ring[XI-XIII] and [XIV-XVI] respectively. These compounds synthesized by sequence reactions starting from reaction resorcinol or hydroquinone with chloracetyl chloride to yield compounds [I] and [II] ,then the later compounds reactant with 4-hydroxybenzylaldehyde to product dialdehyde compounds [III] and [IV] .The Schiff bases compounds[V-VII] and [VIII-X] synthesized from reaction the compound [III] or [IV] with different aromatic amines, while the bent and liner core mesogens containing thiazolidin-4-one ring [XI-XIII] and [XIV-XVI] synthesized from reaction Schiff bases compounds[V-VII] or [VIII-X] with thioglycolic aci
... Show MoreThe synthesis of new benzodiazepine, imidazole, isatin, maleimide, pyrimidine and 1,2,4-triazole derived from 2-amino-4-hydroxy-1,3,5-triazine, via its cyclocondensation reaction with different organic reagents, is described. FT-IR, 1H-NMR and as well as 13C-NMR spectra disclosed the structures of the precursors and heterocyclic derivatives formed.
Small ring heterocycles containing nitrogen and sulfur have been under investigation for a long time because of their important medicinal properties. Among the wide range of heterocycles explored to develop pharmaceutically important molecules, thiadiazoles had played an important role in medicinal chemistry. A survey of literature had shown that compounds having thiadiazole nucleus possess a broad range of biological activities such as anti-inflammatory (1), antibacterial (2), and antifungal activities (3). Thiazine-4-one and their derivatives are import classes of compounds in organic and medicinal chemistry. The thiazine-4-one ring system is a core structure in various synthetic pharmaceutical agents, displaying a broad spectrum of biolo
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