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.
In this work, nanostructure zinc sulfide (ZnS) thin films at temperature of substrate 450 oC and thickness (120) nm have been produced by chemical spray pyrolysis method. The X-Ray Diffraction (XRD) measurements of the film showed that they have a polycrystalline structure and possessed a hexagonal phase with strong crystalline orientation of (103). The grain size was measured using scanning electron microscope (SEM) which was approximately equal to 80 nm. The linear optical measurements showed that ZnS nanostructure has direct energy gap. Nonlinear optical properties experiments were performed using Q-switched 532 nm Nd:YAG laser Z-scan system. The nonlinear refractive index (n2) and nonlinear absorption coefficient (β) estimated for Z
... Show MoreBeryllium Zinc Oxide (BexZn1-xO) ternary nano thin films were deposited using the pulsed laser deposition (PLD) technique under a vacuum condition of 10-3 torr at room temperature on glass substrates with different films thicknesses, (300, 600 and 900 nm). UV-Vis spectra study found the optical band gap for Be0.2Zn0.8O to be (3.42, 3.51 and 3.65 eV) for the (300, 600 and 900nm) film thicknesses, respectively which is larger than the value of zinc oxide ZnO (3.36eV) and smaller than that of beryllium oxide BeO (10.6eV). While the X-ray diffraction (XRD) pattern analysis of ZnO, BeO and Be 0.2 Zn 0.8 O powder and nano-thin films indicated a hexa
... Show MoreThis study includes synthesis of some nitrogenous heterocyclic compounds linked to amino acid esters or heterocyclic amines that may have a potential activity as antimicrobial and/or cytotoxic. Quinolines are an important group of organic compounds that possess useful biological activity as antibacterial, antifungal and antitumor .8-Hydroxyquinoline (8-HQ) and numerous of its derivatives exhibit potent activities against fungi and bacteria which make them good candidates for the treatment of many parasitic and microbial infection diseases.
These pharmacological properties of quinolones aroused our interest in synthesizing several new compounds featuring heterocyclic rings of the quinoline derivatives linke
... Show MoreIn this work, corrosion parameters were evaluated using potentiodynamic polarization curves. In order to determine corrosion parameters of potential and current density of the interesting metal, carbon steel, environmental conditions of external corrosion of buried carbon steel pipeline in Iraqi soil were prepared in the laboratory using simulated prepared conditions. Solutions of sodium chloride at different concentrations (300, 1100, 1900, 2700, and 3500 ppm) were used. pH of solution were acidic at pH =5, and alkaline at pH = 9. Laboratory conditions were similar to those of Iraqi soil where the pipelines were buried. Temperature was constant at 20 °C. Potentiodynamic polarization curves, of potential vs. log current density, were ob
... Show MoreBackground: This study evaluated the influence of different fiber formulations incorporation in resin composite on cuspal deflection (CD) of endodontically-treated teeth with mesio-occluso-distal (MOD) cavities. Materials and Methods: Thirty-two freshly extracted maxillary premolar teeth received MOD cavity preparation followed by endodontic treatment using single cone obturation technique, and divided into: Group I: direct composite resin only using a centripetal technique, Group II: direct composite resin with short fiber-reinforced composite (everX Flow), Group III: direct composite resin with leno wave ultra-high molecular weight polyethylene (LWUHMWPE) fibers placed on the cavity floor, and Group IV: direct composite resin with LWUHMWP
... Show MoreMyelosuppression is a serious disease that is related to the malfunction of blood cells production that leads to cytopenia which is the most serious hematologic toxicity of cancer chemotherapies including cyclophosphamide, which is a strong oxazaphosphorine [a nitrogen mustard alkylating agent] that can be used alone or combined with other chemotherapeutic agents for the treatment of different malignant diseases. It induces severe bone marrow suppression by damaging hematopoietic stem cells through the generation of oxidative stress. Fisetin is a hydrophobic polyphenolic compound with a wide range of pharmacological properties such as antioxidant, anti-inflammatory, antimicrobial, osteoprotective, antidiabetic, and anti-carcinogenic activit
... Show MoreMyelosuppression is a serious disease that is related to the malfunction of blood cells production that leads to cytopenia which is the most serious hematologic toxicity of cancer chemotherapies including cyclophosphamide, which is a strong oxazaphosphorine [a nitrogen mustard alkylating agent] that can be used alone or combined with other chemotherapeutic agents for the treatment of different malignant diseases. It induces severe bone marrow suppression by damaging hematopoietic stem cells through the generation of oxidative stress. Fisetin is a hydrophobic polyphenolic compound with a wide range of pharmacological properties such as antioxidant, anti-inflammatory, antimicrobial, osteoprotective, antidiabetic, and anti-carcinogenic
... Show MoreThis study aims to develop a thermosensitive mucoadhesive periodontal in situ gel of secnidazole for local release of drug for treatment of periodontitis, in order to increase the drug residence time and to increase patient compliance while lowering the side effects of the drug.
Cold method was used to prepare 30 formulas of secnidazole periodontal in situ gel, using different concentrations of thermosensitive polymers (poloxamer407 alone or in combination with poloxamer 188) and methyl cellulose (MC ) or hydroxypropyl methylcellulose (HPMC K4M )in different concentrations used as mucoadhesive polymer and the resultant formulations were subjected to several tests such as gelation temperature GT, appearance and pH value. The fo
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