In this work, the preparation of some new oxazolidine and thiazolidine derivatives has been conducted. This was done over two steps; the first step included the synthesis of Schiff bases A1-A5 in 72-88% yields by the condensation of isonicotinic acid hydrazide and aldehydes. The second step includes the cyclization of derivatives A1-A5 with glycolic acid and thioglycolic acid to obtain the desired products, oxazolidine derivatives B1-B5 (44-60% yields) and thiazolidine derivatives C1-C5 (41-61% yields), respectively. The structure of the prepared compounds was characterized using FT-IR, 1H NMR, and 13C NMR spectroscopy. Some of the produced compounds were tested for antioxidant properties.
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 transfo
... Show MoreCoumarin derivatives have shown different biological activities, such as antifungal, antibacterial antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr
... Show MoreObjective: Schiff’s and Mannich bases of isatins are an important group of heterocyclic compounds which are of great importance in medicinal chemistry as antimicrobial agents. In the vision of these facts, new bis-Schiff bases and Mannich bases of isatins were synthesized. Methods: Three different bis-Schiff bases (3a-c) have been synthesized by reacting isatin, 5-fluoroisatin and 5-methoxy isatin with thiophene-2- carboxaldehyde using hydrazine hydrate to link between the carbonyl compounds, and then these bis- Schiff bases were condensed with two different secondary amines (piperidine and morpholine) separately, and formaldehyde to form the Mannich bases (4a-c and 5a-f), respectively. Results: The structures of the newly synthesized com
... Show MoreThree of imide intermediate products were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c) respectively in dry toluene with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the resulted products consider as
... Show MoreA new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity ag
... Show MoreHeterogeneous organic compounds play an important role in our daily life as they contribute in many medical and industrial fields and are in continuous development as a result of the preparation of new derivatives with different properties. From this premise, the goal of this work appears, which is preparation of (four, five, six, and seven) membered ring systems derived from furfural, by its reaction with different aromatic aldehydes, and record their antioxidant activity by using free radical scavenging method of DPPH radicals. The new ring systems are synthesized by reacting the prepared Schiff-bases with different ring closure agents (chloroacetyl chloride, mercaptoaceticacid, anthranilic acid, and phthalic anhydride), the prep
... 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 MoreIn this paper, some chalcone derivatives (C1, C2) were synthesized based on the reaction of equal amount of substituted acetophenone and substituted banzaldehyde in basic medium. Oxazine and thiazine derivatives were prepared from the reaction of chalcones (C1-C2) with urea and thiourea respectively in a basic medium. Pyrazole derivatives were prepared based on the reaction of chalcones with hydrazine mono hydrate or phenyl hydrazine in the presence of glacial acetic acid as a catalyst. The new synthesized compounds were identified using various physical techniques like1 H-NMR and FT-IR spectra.