In this study, new oxazolidinone and thiazolidinone derivatives were synthesized through a three-step process. In the first step, o-aminothiophenol was reacted with p-aminobenzoic acid in hydrochloric acid to produce an amine containing a thiazole ring, achieving a product yield of 80%. The second step involves synthesizing Schiff bases (E1-E4) by reacting 4-(benzo[d]thiazol-2-yl)aniline with various aromatic aldehydes in the presence of glacial acetic acid. This reaction yields products of 76% to 90%. In the third step, the Schiff derivatives (E1-E4) are reacted with glycolic acid and thioglycolic acid to obtain the desired products. Oxazolidinone derivatives (N1-T1) were produced with rates ranging from 66% to 74%, while thiazolidinone derivatives (N2-T2) exhibited production rates between 63% and 80%. The synthesized compounds were characterized using FT-IR, 13C-NMR, and 1H-NMR spectroscopy. Additionally, all the prepared compounds were evaluated for their antioxidant potential through the DPPH free radical scavenging method. Among the tested compounds (N2-S2-T1-T2-Q2), all demonstrated antioxidant activity. When compared to L-ascorbic acid as a reference, compound Q2 was found to be the most effective inhibitor of the oxidation process. Some of these compounds were examined for their antimicrobial properties against two types of Gram-positive bacteria (Staphylococcus aureus, Staphylococcus epidermidis), two types of Gram-negative bacteria (Escherichia coli, Klebsiella sp.), and one type of fungus (Candida albicans). The study found that most of the compounds exhibited moderate effectiveness, with compounds Q2 and Q1 showing the best results as anti-microbial agents
A set newly complexes with the general formula [M(L)Cl2] are resulting from the reaction of a new schiff base ligand [Ethyl (6R,7R)-7-((E)-2-((2-ethoxy-2- oxoethoxy)imino)-2-(2-(((E)-4-nitrobenzylidene) amino) thiazol -4- yl) acetamido) -8- oxo -3- vinyl -5- thia -1-aza bicyclo [4. 2.0] oct -2- ene -2- carboxylate] (L). This ligand was derived from the reaction of the two substances 4-nitrobenzaldehyde and precursor (P). Reaction the ligand with metal ions M= Mn(II), Co(II), Ni(II), Cu(II) and Cd(II) afforded new complexes which are characterized by FT-IR and Electronic Spectra. These measurements indicate that the complexes have a tetrahedral geometry. The Penicillin-Binding Protein 3 (PBP3) of Staphylococcus aureus and the target protein
... Show MoreIn this study, the ethanolic extracts of Moringa peregrinaseeds (MPSE) were evaluated for their antiparasitic, insecticidal, herbicidal, anti-leukemic, and anti-pancreatic lipase activities. The MPSE showed moderate antileishmanial activity against Leishmania major with an IC50 of 71.7±0.46 μg/mL, compared to 10±0.05 μg/mL and 4±0.05 μg/mL for pentamidine and amphotericin B, respectively. The extract demonstrated moderate insecticidal activity with 41% mortality in Rhyzopertha dominicaand 15.7% in Tribolium castaneum. MPSE exhibitedpotent herbicidal activity against Lemna minorat 1000 μg/mL. Additionally, MPSE inhibited the proliferation of leukemia K562 cells with an IC50 of 25 μg/mL and porcine pancrea
... Show MoreWith the aim of developing potential antimicrobials, a series of novel Ciprofloxacin methylene isatin derivatives incorporating different aromatic aldehydes were synthesized and characterized by FTIR, 1H NMR, Mass spectroscopy and bases of elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique. A majority of compounds were showing activity against several of the microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds is discussed. From comparisons of the compounds, 3c was determined to be the most active compound.
A new series of ?-D-glucose as Schiff bases derivatives is synthesized and characterized with studying their bioactivity. Hydroxyl groups at C (1,2&5,6) sugar moiety are converted into acetal form through a reaction with dry acetone using phosphoric acid and anhydrous zinc chloride as catalysts producing 1,2:5,6-di-O-isopropyledine ?-D-glucofuranose(I). The five memberd ring acetal of C(5,6) is hydrolyzed with acetic acid (65%)and a reaction of the new product with sodium periodate is carried on to get an aldehyde moiety which is used to produce a new series of Schiff bases through reacting with different amino compounds such as 4-amino antipyrene . The suggested chemical structures of the prepared compounds are confirmed by using UV., FT
... Show MoreA new series of ?-D-glucose as Schiff bases derivatives is synthesized and characterized with studying their bioactivity. Hydroxyl groups at C (1,2&5,6) sugar moiety are converted into acetal form through a reaction with dry acetone using phosphoric acid and anhydrous zinc chloride as catalysts producing 1,2:5,6-di-O-isopropyledine ?-D-glucofuranose(I). The five memberd ring acetal of C(5,6) is hydrolyzed with acetic acid (65%)and a reaction of the new product with sodium periodate is carried on to get an aldehyde moiety which is used to produce a new series of Schiff bases through reacting with different amino compounds such as 4-amino antipyrene . The suggested chemical structures of the prepared compounds are confirmed by u
... Show MoreThe synthesis, characterization and mesomorphic properties of two new series of triazine-core based liquid crystals have been investigated. The amino triazine derivatives were characterized by elemental analysis, Fourier transforms infrared (FTIR), 1HNMR and mass spectroscopy. The liquid crystalline properties of these compounds were examined by differential scanning calorimetry (DSC) and polarizing optical microscopy (POM). DSC and POM confirmed nematic (N) and columnar mesophase textures of the materials. The formation of mesomorphic properties was found to be dependent on the number of methylene unit in alkoxy side chains.
New Schiff bases derivatives [IV]a-e is prepared via condensation of Derythroascorbic acid with p-substituted aldehydes in dry benzene. To obtain these derivatives, the 5,6-O-isopropylidene-L-ascorbic acid[I] was chosen as starting material, compound prepared from the reaction of L-ascorbic acid as starting material. Compound[I] was prepared from the reaction of L-ascorbic acid with dry acetone in the presence of hydrogen chloride. The esterification of hydroxyl groups at C-2 and C-3 positions with excess ofethyl α –chloroacetate in the presence of sodium acetate produce acorresebonding ester [II] , which was condensed with hydrazine hydrate to give new hydrazide [III] . The new Schiff bases [IV]a-e were synthesized by reaction of acid h
... Show MoreAllosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.
A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR