This work includes synthesis of some new derivatives of Schiff bases as intermediate compounds. Through the reaction 1,4- phen ylene diamine with different aromatic aldehydes substituted by many different groups in acidic medium and absolute ethanol as a solvent to obtain the Schiff bases (1a-5a). These compounds are reacted with substituted aromatic carboxylic acids and anhydride to give three types of heterocyclic compounds. The first line includes direct reaction with maleic anhydride under certain conditions to give new derivatives of oxazpine(6b-10b). The second line includes reaction of compounds (1a-5a) with 2-mercapto benzoic acid in the presence of triethyl amine as a catalyst and dry benzene as a solvent to give new derivatives of thiazinone(11c-15c). While the third line involved reaction the Schiff bases (1a-5a) with anthranilic acid in dioxane as solvent to give new derivatives of hydroquinazoline (16d-20d). The structures of these new synthesized compounds were identified by spectral methods their [FTIR, 1HNMR, 13C-NMR] and measurements of some physical properties and some specific reactions. Furthermore the effects of synthesized compounds on some strains of bacteria were studied.
compound [1] was formed from the reaction of benzoin and benzaldehyde in the presence of ammonia, which was reacted with sodium hydride in DMF to obtain imidazole salt. This salt was reacted with adipoyl chloride to give compound [2]. Acid hydrazide derivative [3] was obtained from the reaction of compound [2] with hydrazine hydrate. After that Shiff bases [4-9] have been synthesized from the reaction of compound [3] with different aromatic aldehydes. These new formed compounds were diagnosed by 13C-NMR, 1H-NMR for some of them (in Ahl-Albate University in Jordan) and FT-IR spectroscopy (In Baghdad University). All of the prepared products have been studied their biological activities toward two kinds of bacteria. These products show
... 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 using UV., FT
... Show MoreA series of new 2-quinolone derivatives linked to benzene sulphonyl moieties were performed by many steps: the first step involved preparation of different coumarins (A1,A2) by condensation of different substituted phenols with ethyl acetoacetate. The compound A1 was treated with nitric acid to afford two isomers of nitrocoumarin derivatives (A3) and (A4). The prepared compounds (A2, A3) were treated with hydrazine hydrate to synthesize different 2-quinolone compounds (A5,A6) while the coumarin treated with different amines gave compounds (A7,A8). Then the synthesized 2-quinolone compounds (A5-A8) treated with benzene sulphonyl chloride to afford new sulfonamide derivatives (A9-A12). The synthesized compounds were characterized by FT-IR, 1H
... Show MoreThe antibacterial activity of some extracts of A. eupatoria (aqueous and ethanolic) against some pathogenic bacteria (Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli ) and their activity on wound healing in rats , also the presence of some active compounds in both extracts were detected . The results showed that the ethanolic extract was more effective on inhibiting tested bacteria than the aqueous extract . P.aeruginosa was the most resistant bacteria, while highest inhibition zone appeared on E.coli (20 mm) .There was a moderate activity against S.aureus with inhibition zone 15 mm. by using ethanolic extract (10 mg/ml) . The phytochemical analysis for detection of active compounds revealed the presence of Carbohydrate
... Show MoreSeries of new derivatives of quinoline-2-one were synthesized ,m-cresol was chosen as the starting material which was reacted with ethyl acetoacetate in presence of conc.sulphuric acid to give 4,7-dimethyl coumarin (I) which treated with nitric acid in the presence of sulpharic acid afforded 4,7-dimethyl-6-nitrocumarin (II) and 4,7-dimethyl-8-nitrocumarin (III) and then the compound (II) was treated with hydrazine hydrate80% to give a new compound 1-amino-4,7-dimethyl-6-nitroquinoline-2(1H)-one (IV).The latter compound was used to synthesize different
compounds via the reaction with aldehydic azo compounds (V-VII) by Schiff base reaction to prouduce compounds(VIII-X), these azo compounds were prepared by reaction of different aromatic
Nine new compounds of 2-amino-5-chlorobenzothiazole derivatives were synthesized. These new compounds were formed through the reaction of 2-amino-5-chlorobenzothiazole 1 with ethyl chloroacetate and KOH, which gave an ester derivative 2, followed by refluxing compound 2 with hydrazine hydrate to afford hydrazide derivative 3. The reaction of compound 3 with CS2 and KOH gave 1,3,4-oxadiazole-2-thiol derivative 4, and then the reaction of compound 2 with thiosemicarbazide to produce compound 5 then treated it with 4%NaOH led to ring closure to provide 1,2,4-triazole-3-thiol derivative
... Show MoreThis 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 MoreMefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-t
... Show More