Abstract: Chalcones were used to synthesis series of 2-pyrazoline derivatives and evaluated their antimicrobial and anti-inflammatory activities (E)-1,3-diphenylprop-2-en-1-one (1-5) were synthesized by Claisen-Schmidt Condensation method through the reaction of acetophenone with five various para substituted benzaldehyde in presence of KOH, the reaction monitoring by TLC and the result intermediates were checked by melting point and FT-IR Various 2-Pyrazoline derivatives were prepared by one pot reaction that involved the refluxing of (E)-1,3-diphenylprop-2-en-1-one (1–5) and Hydrazine monohydrate in the presence of glacial acetic acid for 24 hours at a temperature of (45–50) °C for a duration 24 hrs. pyrazoline II (1-5) was formed, then antioxidant compound (guaiacol) was added reflex for 24-48 hours, monitoring by TLC to ensure the reaction was completed. The final mixture was cooled in ice-water bathe until the formation of crystals were completed, added to crushed ice, kept in refrigerator overnight, filter, recrystallized and then dried to get 2-pyrazoline derivatives, IIIa, IIIb, IIIc, IIId and, IIIe. based on the spectral data 2-pyrazoline derivatives structures have been confirmed. The synthesized compounds were screened for their antimicrobial activity and anti-inflammatory.
In this research, cyclic compounds derived from 2- furfural mercaptan (oxazole, triazoles) were synthesized, and their biological efficacy was measured and compared with standard drugs. Also, their effectiveness as anti-oxidant was measured and compared with ascorbic acid as a standard substance. Some of the synthesized compounds were deduced with good efficacy. © 2021 Sami Publishing Company. All rights reserved
This search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [4-(1,3-dioxoisoindolin-2-yl)benzoic acid] was synthesized by reaction p-aminobenzoic acid and phthalic anhydride in presence of (gla. CH3COOH). Reaction of compound (V) with thionyl chloride produced [4-(1,3-dioxoisoindoli
... Show MoreTill now, isatin derivatives have received a lot of interest in organic and medicinal chemistry due to their significant biological and pharmacological activities. Schiff’s and Mannich bases of isatins are an effective group of heterocyclic derivatives that play a significant role in medicinal chemistry as antimicrobial agents. In light of these facts, new Schiff bases and Mannich bases of isatin were synthesized. The monomer Mannich bases; 3(a-e) have been synthesized by reacting isatin with different secondary amines, piperidine, morpholine, and pyrrolidine, dimethylamine, diphenylamine, separately, and formaldehyde, while the dimer (5) formed by using piperazine and formaldehyde which then react separately with Phenylhydrazine
... Show MoreThis work contain many steps starting from esterification of isophthalic acid to yield diester compound [I] which was converted to their acid hydrazide [II], then the later compound reacted with ethylacetoacetate to yield pyrazol-5-one compound [III]. Afterword added acetyl chloride to give the compound [IV], thereaction of this compound with theiosemicarbazide ledto produce a new carbothioamide compound [V], Which was reacted with ethyl chloro acetate to yield thethioxoimidazolidin compound [VI]. The condensation reaction of this compound with different substituted aldehyde give new alkene derivatives[VII]a-d. The synthesized compounds were characterized by melting points , FT-IR ,1H-NMR and Mass spectroscopy .
In this paper the new starting material 2-(5-chloro-1H-benzo[d]imidazole-2-yl) aniline (1) was synthesized by the condensation reaction of 4-chloro-o-phenylenediamine and anthranilic acid .The new Mannich base derivatives were synthesized using formaldehyde and different secondary amines to synthesize a new set of benzimidazole derivatives(2-5). Also, the new Schiff-base derivatives (6-10) were synthesized from the reaction of compound (1) with various aromatic aldehydes and the closure-ring was done successfully using mercapto acetic acid to get the new thiazolidine derivatives(11-12).These new compounds were characterized using some physical techniques like:FT-IR Spectra and 1HNMR Spectra.
In this paper a new series of morpholine derivatives was prepared by reacting the morpholine with ethyl chloro acetate in the presence triethylamine as a catalyst in benzene gave morpholin-N-ethyl acetate(1) which reacted with hydrazine hydrate in ethanol, and gave morpholin-N-ethyl acetohydrazide (2) . Morpholin-N-aceto semithiocarbazide (3) were prepared by reacting compound(2) with ammonium thiocyanate , concentrated hydrochloric acid and ethanol as a solvent .Compound (3) reacted with sodium hydroxide and hydrochloric acid to give 5-(morpholin-N-methylene)-1H-1,2,4-triazole-3-thiol (4) .The new series of 1,2,4-triazol derivatives (5-8) was synthesized by reaction of compound(4) with formaldehyde , DMF as a solvent and different
... Show MoreThis study describes the preparation of a new bidentate Schiff base derived from the condensation of Isatin-3-hydrazone with 2-acetylthiophene and the preparation of new series of complexes with a good yield. The prepared ligand was characterized by IR, UV-Vis, C.H.N.S elemental analysis, 1H and 13C NMR, LC-Mass spectroscopy, and physical measurements. Its complexes were analyzed by C.H.N.S elemental analyses, UV-Vis., FTIR, NMR, LC-Mass Spectra, atomic absorption spectroscopy, magnetic susceptibility, and conductivity measurements The results from spectroscopy and measurement studies showed that the ligand coordinated to the metal ion as a bidentate ligand via oxygen and nitrogen, forming an octahedral geometry around it. In vitro antimicr
... Show MoreIn this work, N-hydroxy phthalimide derivatives (NHPID) were synthesized from the nucleuphilic substitution reactions of (NHPI) with different halides (alkyl halides, sulfonyl halides, benzoyl halides and benzyl halides). The products were distinguished using FTIR spectrum and Nuclear magnetic resonsnce (1H-NMR and 13CNMR), in addition to other characteristic methods such as sodium fution for sulfur determination. followed by measuring antibacterial (with different types of gram positive/gram negative bacteria) and antifungal activities of these compounds.
Our goal in this research, some new nucleoside analogues was synthesized. Starting from ?-D glucose which was converted to per acetylated ?-D gluco pyronoside then converted to active from(1-Bromo Sugar (2) as a sugar moiety.The base moiety 2-substituted benzimidazole was prepared from condensation of phenylene diamine with different aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleobase derivatives. Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues then hydrolyzed with sodium methoxide in methanol to obtain our target, the free nucleoside analogues. All prepared compound were identified b
... Show MoreIn this research, 5- membered heterocyclic compounds as oxazolidine-5-one J1-J5 derivatives were prepared using primary aromatic amine, aromatic carbonyl compounds and chloroacetic acid. By combining primary aromatic amines and aromatic carbonyl compounds, Schiff's bases were synthesized. Schiff bases are used with the chloroacetic acid compound to prepare oxazolidine-5-one J1-J5 derivatives. The compounds J1-J5 were described using NMR spectroscopy and FT-IR. .The biological efficacy was evaluated according to maximum inhibitory concentrations (MICs) toward Staphyloccoccus aureus and Esherichia coli. The best MIC was 210 μg ml-1 for J4 against the two pathogenic bacteria, while J1, J4, and J1 did not show any inhibitory effect against all
... Show More