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.
The present work involved two steps: the first step include Mannich reaction was carried out on 2- mercaptobenzimidazole using formaldehyde and different secondary amine or amide to gives the compounds(2-16). The secnd step include preparation of (Ethylbenzimidazoly-2-mercaptoacetate)(17) from the reaction of 2- mercaptobenzimidazole with ethylchloroacetate than prepared hydrazide derivative[18]from reaction of compound(17) with hydrazinehydrate. Followed Preparation of shiff bases(19-24) and there reaction with mercaptoacetic acid to give a new compounds containing thiazolidinderivetives(25-30).Structure confirmation of all prepared compound were proved using FTIR and element analysis (C.H.N.S) and mesurmentedmelting poi
... Show MoreNew 2-amino thiazole ,oxodiazole, sulphonilamide and diazin derivatives of N-(α-chloro aceto)-3-(tolyl imino)-5-bromo-2-oxo-indole(2) have been synthesized .The preparation process started by the reaction of 5-bromo isatin with P-toluidine in the presence of glacial acetic acid and dimethylformamide(DMF) as a solvent to give 3-(tolyl imino)5-bromo-1H-indole-2-one.(1), Compound (1) with sodium hydride in dimethylformamide(DMF) at 0C0 gave a suspension of the sodium salt of Schiff base derivative and subsequent reaction with monochloroacetylchloride obtained the intermediate compound(2).Compound(2) was reacted with different reagents in four routes.The first route involved direct reaction with substituted 2-aminobenzothiazole u
... Show More1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.
To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.
The designed compounds were synthesized using convent
Five membered heterocyclics derivatives were synthesized in this work by three routes. The first route includes the synthesis of N-benzoic acid 1,2,3,-triazole derivatives (3),(4) by diazotation of methyl-2-amino benzoate and treating the resulted salt (1) with sodium azide and ethyl acetoacetate or acetyl acetone, respectively. In the second route, derivatives of pyrazole (8) pyrazolin-5-one (9), (10) were prepared by the reaction of the salt (1) with some active methylene compounds to give the corresponding hydrazones derivatives (5-7) which then they were treated with hydrazine hydrate. The third route afforded the synthesis of three derivatives (12), (15a), (15b) of thiazolidinone by two different methods. AII compounds were confirmed b
... Show MoreIn this research, a new 1, 3, 4-Thiadiazole derivatives have been synthesized by many heterocyclic reactions. Starting from (2, 5 – dimercapto -1, 3, 4-Thiadiazole) a variety of derivatives have been synthesis. Compound (1) was synthesized by the reaction of hydrazine hydrate with carbon disulphide in absolute ethanol. The compound (1) was reacted with 1, 2-dibromoethane in presence of alkali ethanol to give the compound (2). The compound (3) was formed from the reaction of compound (2) with hydrazine hydrate. Schiff base (4) was obtained by reacting of compound (3) with the compound (p-hydroxybenzaldehyde) in absolute ethanol. A variety of phenolic Schiff base (Methylolic, Etheric, and Epoxy) derivatives have been synthesized. Methylol
... Show MoreWith the aim of developing potential antimicrobials, a series of new 5-fluoroisatin derivatives incorporated with different secondary amines (piperidine, morpholine, pyrrolidine, dimethylamine, and diphenylamine) for monomer, and (piperazine) in case of dimer Mannich bases, separately in presence of formaldehyde to obtain Mannich bases of 5-fluoroisatin derivatives, which then each Mannich derivatives reacts with phenylhydrazine to form Schiff bases as final products. The resulting compounds were characterized by two spectroscopic analyses; (Fourier- transform infrared) FT-IR and proton nuclear magnetic resonance spectroscopy (¹H-NMR). In addition, the in vitro antibacterial and antifungal activities were tested against some human pathogen
... Show MoreThis study includes synthesis, characterization three series of the new derivatives via schiff bases for ampicillin which known as a high medicinal effectiveness. Series A include preparation schiff bases (A1-A6) by condensation of ampicillin with many substituted aldehyedes, while series B include preparation of six amines (B1-B6) is hydrazine hydrate derivatives by reaction schiff bases compounds which prepared in series A with hydrazine hydrate, then series C included for preparation of new six polymers C1-C6 by reaction of poly methyl methacrylate with amine compounds which prepared in series B. The synthesized polymers were identified by spectroscopic methods (FT-IR and 1 H-NMR) and measurement some of its physical characteristics.
This search reports the synthesis of some new series of Schiff base compounds for trimetheprim derivatives which known high been known as a medicinal effectiveness. Trimetheprim was condensed with several substituted aldehydes compounds.(4-dimethyl amine benzaldehyde , propanal , salicaldehyde, 2.4 dimethoxy benzaldehyde and 4- methyl benzaldehyde) to obtain Schiff base products(1a-5a) and several substituted ketones compound (4-aminoacetophenone,4-chloroacetophenone, isobutyleketone, acetylacetone and acetophenone) to obtain Schiff base products(6b-10b) in ethanol in the presence of concentrated sulphuric acid as a catalyst to yield the Schiff base. The structure of synthesized compounds has been established on the basis of their Chemical
... Show MoreA new series polymers was synthesized from reaction starting material Bisacodyl A or [(2-Pyridinylmethylene) di-4, 1-phenylene di acetate] with hydrogen bromide, then the products were polymerized by addition polymerization from used adipoyl and glutaroyl chloride. The structure of these compounds was characterized by FT-IR, melting points, TLC, X-Ray, DSC and 1H-NMR for starting material. These compounds were also screened for their antibacterial activists?