In this research two series of the new derivatives of Trimethoprim and paracetamol drugs have been prepared which known as a high medicinal effectiveness. Series (A) is including the interaction of diazonium salt of trimethoprim and coupling with some substituted phenol compounds (2-amino phenol, 3-ethyl phenol, 1-naphthol, 2-nitro phenol, Salbutamol). Series (B) is including the interaction coupling alkali solution of paracetamol with diazonium salt of some substituted aniline compounds (Benzedine, 2, 3-di chloro aniline, Trimethoprim, Anilinium chloride, 2-nitro- 4-chloro aniline).Chemical structures of all synthesized compounds were confirmed by UV-visible and FTIR spectroscopy.
Synthesis of 2-mercaptobenzothiazole (A1) is performed from the reaction of o-aminothiophenol and carbon disulfide CS2 in ethanol under basic condition. Compound (A1) is reacted with chloro acetyl chloride to give compound (A2). Hydrazide acid compound (A3) is obtained from the reaction of compound (A2) with hydrazine hydrate in ethanol under reflux in the presence of glacial acetic acid .The reaction of hydrazide acid compound (A3) with ethyl acetoacetate gives pyrazole compound (A4). The new hydrazone compound (A5) was prepared from the reaction of compound (A3) with benzaldehyde. Reaction of compound
... Show MoreThe present study envisaged utilizing 4-aminoantipyrine as key intermediate for the synthesis of some new derivatives bearing anti-bacterial and anti-cancer activities moieties viz., antipyrine diazenyl benzaldehydes 2(ad) which were obtained by coupling of diazotized 4-aminoantipyrine (1) with substituted benzaldehydes at 0◦C (iced) temperature. The other antipyrine derivatives where containing bis heterocycles like bis thiazolidinone-antipyrine (4), bis imidazolidinone -antipyrine (5) and bis azetidinone -antipyrine (6).These compounds were prepared through the reaction between 4- aminoantipyrine and terephthaldicarboxaldehyde to get (3) which were reacted with mercaptoacetic acid , glycine or chloroacetyl chloride separately to get com
... Show MoreThis research include synthesized and characterization the compound [I] by reaction terephthaldehyde , mercaptoacetic acid and thiosemicarbazide with concentrated sulfuric acid then this compound reaction with ethyl chloroacetate and sodium acetate to product ester compound [II],the latter compound reaction with hydrazine hydrate to synthesized acid hydrazide [III] after that reaction with 4-alkoxy benzaldehyde[IV]n to synthesized Schiff bases compounds [V]n, the compound [VI] synthesized via reaction compound [I] with chloroacetic acid and sodium acetate then the compound[VI] reaction with 2-phenylenediamine in 4 N hydrochloric acid to product benzimidazole compound[VII]. The compounds characterized by melting points, FTIR and 1HNMR spectr
... Show MoreMetal complexes of Mn(II), Co(II), Ni(II), Cu(II), Cd(II), Zn(II), Hg(II), Pd(II), and Pt(II) with Schiff base ligand (LH) derived from 2,5-dichloroaniline and 2-hydroxy-5-metheylbenzalaldehyde were synthesized and characterized using a variety of spectrophotometric techniques The findings of the spectroscopic analysis indicated that (LH) behaved as a binary coordinating agent to the metal ion by the N and O atoms, and the geometry shape of the complexes was octahedral, with the exception of the Pd and Pt complexes, which had a square planar geometry. Using the DPPH radical scavenging method, we investigated the antimicrobial activity of the compound against Staphylococcus aureus and Escherichia coli, as well as the antifungal activity of t
... Show MoreThe mixed ligand complexes of Schiff base ligand (Z)-2-(((4-bromo-2-methylphenyl) imino) methyl)-4-methylphenol (L) with some metals ion (II); Mn(1), Co(2), Ni(3), Cu(4), Zn(5) Cd(6) and Hg(7) and 1,10-Phenanthroline (phen) were Synthesis and characterized by the mass and 1HNMR spectrometry (ligand Schiff base), the FTIR, UV-visible and the flame atomic absorption (A.A) spectrum, the C.H.N analysis and the chlorine content, in addition to measuring the magnetic sensitivity of the complexes. All the complexes had octahedral geometry. The bioactivity activity for compounds against; Rhizopodium, Staphylococcus aureus and Escherichia coli, the compounds showed different efficacy towards these microorganisms
The Schiff base (E)-2-(((2-(1H-benzo[d]imidazol-2-yl) phenyl) imino) methyl)-4-methylphenol (Lb) ligand with some metals(II) ion such as; Co, Cu, Cd, and Hg, were synthesis and characterized by the mass and 1 HNMR spectrometry for ligand Schiff base, the fourier-transform infrared spectroscop (FTIR), UV- visible and the flame atomic absorption (AA) spectrum, the CHN analysis, and the chlorine content, in addition to measuring the magnetic sensitivity of the complexes. All the complexes had octahedral geometry. The bioactivity activity for compounds against; Rhizopodium, Staphylococcus aureus, and Escherichia coli showed different efficacy towards these microorganisms
Mefenamic 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 MoreThe snthesis and characterization of cobalt(II), nickel(II), copper(II) and zinc(II) complexes of azo ligand 4-[(5-acetyl-2-aminophenyl)- diazenyl]-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one derived from 4-aminoantipyrine and 4-aminoacetophenone are reported. The nature of the compounds have been studied followed by mole ratio and methods of continuous contrast, Beer′s law followed during a condensation rate (1 × 10-4 – 3 × 10-4 M). The analytical data showed that all the complexes are in 1:2 metal-ligand ratio. An octahedral geometry have been suggested for all the compounds and biological studies of all the complexes were evaluated against different types of antimicrobial strains.
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
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