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. Metronidazole has a half-life of 6.5 ± 2.9 hours. A number of studies have recently been conducted on the selective substitution of hydrogen with deuterium. which increases the bond strength, increasing the biological half-life and, consequently, the drug's metabolic stability also increases. In an attempt to address metronidazole's drawbacks and clinical resistance, deuterated metronidazole was synthesised, characterised, and tested for antibacterial, antifungal, and anti-tubercular activities. The metronidazole and its deuterated compound showed equipotent antifungal activity and aerobic antibacterial activity. Also, when compared with the non-deuterated compound, deuterated metronidazole exhibited better anaerobic antibacterial and anti-tubercular activity.
This paper investigates the performance evaluation of two state feedback controllers, Pole Placement (PP) and Linear Quadratic Regulator (LQR). The two controllers are designed for a Mass-Spring-Damper (MSD) system found in numerous applications to stabilize the MSD system performance and minimize the position tracking error of the system output. The state space model of the MSD system is first developed. Then, two meta-heuristic optimizations, Simulated Annealing (SA) optimization and Ant Colony (AC) optimization are utilized to optimize feedback gains matrix K of the PP and the weighting matrices Q and R of the LQR to make the MSD system reach stabilization and reduce the oscillation of the response. The Matlab softwar
... Show MoreThe aim of the study was to evaluate the efficacy of diode laser (λ=940 nm) in the management of gingival hyperpigmentation compared to the conventional bur method. Materials and methods: Eighteen patients with gingival hyperpigmentation were selected for the study with an age between 12-37 years old. The site of treatment was the upper gingiva using diode laser for the right half and the conventional method for the left half. All patients were re-evaluated after the following intervals: 3 days, 7 days, 1 month and 6 months post-operation. Pain and functions were re-evaluated in each visit for a period of 1 day, 3 days and 1 week post-operation. Laser parameters included 1.5 W in continuous mode with an initiated tip (400 μm) placed in
... Show MoreAbstract: Thorough assessment of the Maxillary,Sinus is very important. Recently 3-dimensional imagewith Cone Beam Computed Tomography (CBCT) is very dependable in Maxillary Sinus diagnosis. The aim of this study is to: shade light on the role of (CBCT) diagnosis of the maxillary sinus anatomical variation and pathological finding among smokers and nonsmokers prior to maxillary sinus lift techniques. Materials and Method: In this study 60 males with age ranged between 20-50 years old, referred for (CBCT) assessment of maxillary sinus in the Specialist Health Center of AL-Sadder city. The scanning were performed using Kodak 9500 (CBCT), the KV was 90, mA10 and scanning time 10 s. Voxel size 0.3mm with( DICOM ) software on a multiplaner re
... Show MoreThe work includes synthesis and characterization of some new heterocyclic compounds, as flow: The compound (3) (5-(4-chlorophenyl) -2-hydrazinyl-1,3,4-oxadiazole was synthesized by using two methods; the first method includes the direct reaction between hydrazine hydrate 80% and 5-(4-chlorophenyl)-2- (ethylthio) 1,3,4-oxadiazole (1), the second method involves converting 5-(4-chlorophenyl)-1,3,4-oxadiazol-2-amine (2) to diazonium salt then reducing this salt to compound (3) by stannous chloride. Compound (3) was used as starting material for synthesizing several fused heterocyclic compounds. The compound 6-(4-chlorophenyl)[1,2.4] triazolo [3,4,b][1,3,4] oxadiazole-3-(2H) thione (compound 4) was synthesized from the reaction of compound (3)
... Show MoreIn this research, CNRs have been synthesized using pyrolysis of plastic waste(pp) at 1000 ° C for one hour in a closed reactor made from stainless steel, using magnesium oxide (MgO) as a catalyst. The resultant carbon nano rods were purified and characterized using energy dispersive X-ray spectroscopy (EDX), X-ray powder diffraction (XRD). The surface characteristics of carbon rods were observed with the Field emission scanning electron microscopy (FESEM). The carbon was evenly spread and had the highest concentration from SEM-EDX characterization. The results of XRD and FESEM have shown that carbon Nano rods (CNRs) were present in Nano figures, synthesized at 1000 ° C and with pyrolysis temperature 400° C. One of t
... Show MoreIn this research, porous silicon (PS) prepared by anodization etching on surface of single crystalline p-type Si wafer, then Gold nanoparticle (AuNPs) prepared by pulsed laser ablation in liquid. NPs deposited on PS layer by drop casting. The morphology of PS, AuNPs and AuNPs/PS samples were examined by AFM. The crystallization of this sample was characterized by X-ray diffraction (XRD). The electrical properties and sensitivity to CO2 gas were investigated to Al/AuNPs/PS/c-Si/Al, we found that AuNPs plays crucial role to enhance this properties.
A new 5‐fluorouracil–naproxen conjugate is synthesized as a mutual prodrug for targeting cancer tissues. The structure of the target compound and their intermediate are characterized by their melting point, IR, 1H NMR, 13C NMR, and elemental microanalysis. The cytotoxic activity is preliminarily evaluated using nonsmall lung cancer CRL‐2049, human breast cancer CAL‐51, and one type of normal cell line; rat embryo fibroblast cell line. The synthesized compound shows a good cytotoxic effect at the cancer cell and no significant effect at rat embryo fibroblast cell line.
The work includes synthesis and characterization of some new heterocyclic compounds, as flow: The compound (3) (5-(4-chlorophenyl) -2-hydrazinyl-1,3,4-oxadiazole was synthesized by using two methods; the first method includes the direct reaction between hydrazine hydrate 80% and 5-(4-chlorophenyl)-2- (ethylthio) 1,3,4-oxadiazole (1), the second method involves converting 5-(4-chlorophenyl)-1,3,4-oxadiazol-2-amine (2) to diazonium salt then reducing this salt to compound (3) by stannous chloride. Compound (3) was used as starting material for synthesizing several fused heterocyclic compounds. The compound 6-(4- chlorophenyl)[1,2.4] triazolo [3,4,b][1,3,4] oxadiazole-3-(2H) thione (compound 4) was synthesized from the reaction of compo
... Show MoreThis work includs synthesis of several Schiff bases by condensation of 6- methoxy – 2- amino benzothiazole with some aldehydes and ketones (2- hydroxyl benzaldehyde, 4- hydroxyl benzaldehyde, 4- N,N –dimethy amino acetophenone, benzophenone) to abtain schiff bases (1-5). These schiff bases were found to react with phthalate anhydride to give oxazepine derivatives (6-10) that were reacted with primary aromatic amines to give Diazepine derivatives (11-15). Besides, we prepared new tetrazole derivatives (16-20) from the reaction of the prepared Schiff bases with sodium azide in the prepared compounds that were characterized by physical properties, FT-IR and some of the 1H-NMR and 13C –NMR spectroscopy.
The purpose of this research work is to synthesize conjugates of NSAIDs (ibuprofen, and naproxen) with sulfadiazine as possible mutual prodrugs to overcome the local gastric irritation of NSAIDs with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo bond that undergo reduction only by colonic bacterial azoreductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)