Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory results compared with levofloxacin. This has indicated that the presence of the carbonyl of C-3 carboxyl moiety is not essential, as levofloxacin carboxamides showed interesting copper complexes indicating that they retain the activity of levofloxacin, since its activity depends on binding to DNA gyrase via magnesium binding
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The discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Met
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In this paper, a discretization of a three-dimensional fractional-order prey-predator model has been investigated with Holling type III functional response. All its fixed points are determined; also, their local stability is investigated. We extend the discretized system to an optimal control problem to get the optimal harvesting amount. For this, the discrete-time Pontryagin’s maximum principle is used. Finally, numerical simulation results are given to confirm the theoretical outputs as well as to solve the optimality problem.
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ان تصنيع رمال مطلية بأوكسيد الحديد من خلال ترسيب الجزيئات النانوية لذلك الاوكسيد على سطوح الرمال واستخدامها في الحاجز التفاعلي النفاذ لإزالة ايونات الكادميوم والنحاس من المياه الجوفية الملوثة الهدف الرئيسي للدراسة الحالية. تم توصيف بيانات الامتزاز نتيجة تفاعل المادة المازة مع المادة الممتزة قيد الدراسة بشكل جيد من خلال نموذج لانكمير والذي كان أفضل من نموذج فراندلش. لقد وجد ان اعلى قيم لقابلية الامتزاز با
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The exercise of activities and sports are of great importance to public health and to maintain the ideal health weight as well as the psychological and mental comfort of humans. The aim of this study is to determine the contribution and participation of educated females in physical activities at the University of Baghdad hall for the years 2011-2016, and to show the factors that influence women's contribution to physical activities at the university by selecting 100 students of males and 100 females' students randomly. During the questioning questions and statistical analysis of the questioning to find out the reasons for the discouraging contribution of the women to the various physical activities and try to find solutions and r
... Show MoreThe present work involved synthesis of serval new substituted tetrazole via Schiff bases for trimethoprim drug by two steps. The first step involved direct reaction of different ketones and aldehydes with trimethoprim producing the corresponding Schiff bases (1-10), whereas the second step, involved preparation new tetrazoles derivatives (11-20) through reaction of the ready Schiff bases (in the first step) with sodium azidein in dioxin. The prepared compounds were characterized by UV, FT-IR, and some of them by 13C-NMR, 1H-NMR spectroscopy and physical properties.
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
... Show MoreThis work includes two steps of synthesis, the first one is the synthesis of indole which was prepared according to literature of the reaction of phenyl hydrazine with acetaldehyde in glacial acetic acid afforded phenyl hydrazone of acetaldehyde , this product was fused with zinc chloride to give the indole.Reaction of cyclohexanone with phenyl hydrazine using the same procedure for the preparing giving 1,2,3,4-Tetrahydrocarbazole.Second step involved synthesis of a series of (17) of mannich bases derivatives of indole and 1,2,3,4-Tetrahydrocarbazle. Mannich reaction involves the condensation of aldehyde usually formaldehyde with different secondary amine and with compound containing an activated hydrogen.The reaction illustrated by the fo
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New complexes of Al(III) such as [Al (Ura) (Phen) (OH2) Cl ] Cl. 2H2O, [Al(Ura)2(OA)(OH2)Cl].H2O and [Al(Ura)3Cl3]H2O type, where (Ura)=Uracil, (Phen)= 1,10-Phenanthroline monohydrate and (OA)= Oxalic acid dihydrate, were prepared. The elemental microanalysis, FT.IR, electronic spectra, and magnetic susceptibility as well as the conductivity measurements are characterized. For isolated three complexes for six coordinated of Al(III) are proposed with molecular formulas that depend on the nature of (Ura), (Phen) and (OA) present. The suggested molecular structure into all complexes for aluminum ion is octahedral geometries .The antibacterial efficacy was examined from metal salt (AlCl3), ligands and metal complexes into the pathogenic bacteri
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