Propranolol is a nonselective-adrenergic blocker used in the treatment of hypertension, cardiac arrhythmias, and angina pectoris. A significant problem in propranolol therapy is that it undergoes extensive presystemic metabolism after oral administration leading to reduced bioavailability. In this study, two new propranolol derivatives have been designed, synthesized and characterized. These compounds were formed by acylation of propranolol followed by nucleophilic substitution reaction of acylated propranolol, these derivatives were analyzed for IR, CHN, melting points, and evaluated for their lipophilic properties compared with propranolol. The lower partition coefficient of these two derivatives revealed that the prodrug approach may be an effective means of avoiding first- pass metabolism.
Asthma is a chronic respiratory disorder in which immunological and structural cells play a role. The limits of conventional medicines necessitate the development of innovative therapeutic techniques for asthma. In the present study, we investigated the possible protective effect of cinnamic acid (CA) on ovalbumin-induced asthma in a mouse model. Sixty albino male mice BALB/c type weighing (20-30) grams were chosen at random and divided into five groups each one contains 12 animal: Group I: PBS/liquid paraffin control. Group II: asthma model group. Group III: cinnamic acid control group; mice received cinnamic acid (50 mg/kg) in liquid paraffin orally by gavage. Group IV: asthma model / group of (25 mg / kg) cinnamic acid; mice received
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The organic compound imidazole has the chemical formula C3N2H4. Numerous significant biological compounds contain imidazole. The amino acid histidine is the most prevalent. The substituted imidazole derivatives have great potential for treating a variety of systemic fungi infections. Thiourea is an organosulfur compound with the formula SC(NH2)2. It is a reagent in organic synthesis. In this paper, some new imidazole and thiourea derivatives are synthesized, characterized, and studied for their biological activity. These new compounds were synthesized from the starting material terephthalic acid, which was transformed to corresponding ester [I] by the refluxing of diacid with methanol in the presence of H2SO4 as a catalyst, compound [I] con
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4,4'-(pyridine-2,6-diylbis(1,3,4-oxadiazole-5,2-diyl))bisphenol monomer (3)was synthesized from cyclization of N'2,N'6-bis(4-hydroxybenzylidene)pyridine-2,6-dicarbohydrazide (2)in the presence of bromine in glacialacetic acid. Newly five polymers (P1-P5) were synthesized from reaction bis-1,3,4-oxadiazole bisphenolmonomer with five different di acid chloride. The antibacterial activity of the synthesized polymers was screened against gram positive and gram negative bacteria. Polymers P4 and P5 exhibited significant antibacterial against all microorganisms, as well these polymers showed highest antifungal activity.
This research includes the synthesis of some new different heterocyclic derivatives of 5-Bromoisatin. New sulfonylamide, diazine, oxazole, thiazole and 1,2,3-triazole derivatives of 5-Bromoisatin have been synthesized. The synthesis process started by the reaction of 5-Bromoisatin with different reagents to obtain schiff bases of 5-Bromoisatin intermediate compounds(1, 8, 19) by using glacial acetic acid as a catalyst in three routes. The first route, 5-Bromoisatin reacted with p-aminosulfonylchloride to product compound(1), then converted to sulfonyl amide derivatives(2-7) by the reaction of compound(1) with different substituted primary aromatic amine in absolute ethanol. The second route includes the reaction of 5-Bromoisatin rea
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Coupling reaction of 4-aminoantipyrene with 8-hydroxyqunoline gave the new bidentate azo ligand 5-(4-antipyrene azo)-8-hydroxyqunoline. Treatment of this ligand with the following metals ions (MnII, CoII, NiII, CuII and ZnII) in aqueous ethanol with a 1:2 M:L ratio yielded a series of neutral complexes of the general formula [M(L)2Cl2]. The prepared complexes were characterized using flame atomic absorption, FT.IR, UV-Vis spectroscopic as well as magnetic susceptibility and conductivity measurements. Chloride ion content were also evaluated by (Mohr Method). From above data, the proposed molecular structure for these complexes as octahedral geometry.
This 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 MoreNew bidentate dithiocarbamate ligand (NaL) namely [Sodium-2-(((3-methyl -4- “(2,2,2-tri fluoro ethoxy) pyridin-2”-yl) methyl) sulfinyl)-1H-benzoimidazole -1-carbodithioate] was prepared. This free ligand was synthesized from the reaction of a (RS)-2-([3-methyl -4-(2,2,2-tri fluoroethoxy) pyridin-2-yl] methyl sulfinyl)-1H benzoimidazole, CS2 and NaOH in methanol as solvent. From reaction of dithiocarbamate salt (NaL) with metal ions (M); Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Pd(II)”, have obtained the DTC complexes at general molecular formula [M(L)2(H2O)2] and [Pd(L)2]. To characterize the ligand and its complexes, used different analyses methods such FTIR, UV-Vis, elemental microanalysis, atomic absoreption, magnetic susceptibil
... 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
This work has been done to prepare a series of new alkene compounds derived from 4-thiozolidinones by substituting different aldehydes, P-acetamido-phenol, and 2-mercapto-benzoimidazole, which were used as starting materials to form ester [I]a,b and then make hydrazides [II]a,b, which were used to prepare 1, 3, and 4-oxadiazoles [III]a,b, which were then used for prepared Schiff bases [IV]a-f, The next step was the synthesis of 4-thiazoldinone derivatives [V]a-f from Schiff bases. The final step was the synthesis of alkenes [VII]a-f, the prepared derivatives were identified with spectral methods (FT-IR, 1H-NMR, mass, and CHNS). The antibacterial activity of the prepared derivatives was evaluated against four types of bacteria, pos
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