In this research four steps of the new derivatives of Naproxen drug have been made which are known as a high medicinal effectiveness; the first step involved converting Naproxen into the corresponding ester (A) by reaction Naproxen with methanol absolute in presence H2SO4. While the second step involved treatment methyl Naproxen ester (A) with hydrazine hydrate 80% in presence of ethanol .The third reaction requires synthesis of Schiff bases (C1-C10) by condensation. of Naproxen hydrazide (B) with many substituted aromatic aldehydes . Finally, the fourth step synthesized new tetrazole derivatives ( D1- D10) by the reaction of the prepared Schiff bases (in the third step) with Sodium azide in THF as a solvent .The prepared compounds were characterized by physical properties ,(FT-IR) ,UV, and somewhat of them by 1H-NMR, 13C-NMR spectroscopy.
Carbazone Derivatives (CD) (semicarbazone, semithiocarbasone) are produced by the condensation reaction between a aldehyde (or ketone) with a carbazide derivatives (semicarbazide, semithiocarbazide). CD and their metal complexes existent a wide range of implementation that stretch from their ply in the medicinal and pharmaceutical area because of their major significant pharmacological characteristic such as anti-fungal,anti-bacterial, anti-cancer, anti-human immunodeficiency virus, anti-inflammation, anti-neoplastic,inhibition corrosion, antioxidation, antiradical. This paper reviews the definition, importance and various applications of carbazone derivatives with transitional meta
This review covers recent progress in the synthesis of curcumin and the bioactivity of semisynthetic and synthetic analogs of curcumin. The review also shows how curcumin is a useful intermediate for the synthesis of more complex organic molecules; historical perspective; the process of preparing the metal complexes and characterization the produced complexes using various spectral and other techniques; shows the importance of curcumin and its derivatives for their potential applications in medical devices and broad-spectrum of medical application such as antibiotic ointment, alternative therapeutics, antifungal, and antibacterial activities
AASAH Enass J Waheed, Shatha MH Obaid, Research Journal of Pharmaceutical, Biological and Chemical Sciences, 2019 - Cited by 5
The ligand [Potassium (E)-(4-(((2-((1-(3-aminophenyl) ethylidene) amino)-4-oxo-1,4- dihydropteridin-6-yl) methyl) amino)benzoyl)-L-glutamate] was prepared from the condensation reaction of folic acid with (3-aminoacetophenone) through Schiff reaction to give a new Schiff base ligand [H2L]. The ligand [H2L] was characterized by elemental analysis CHN, atomic absorption (A.A), (FT-I.R.), (U.V.-Vis), TLC, E.S. mass (for spectroscopes), molar conductance, and melting point. The new Schiff base ligand [H2L], reacts with Mn(II), Co(II), Ni(II), Cu(II), Cr(III) and Cd(II) metal ions and (2-aminophenol), (metal : derivative ligand : 2-aminophenol) to give a series of new mixed complexes in the general formula:- K3[M2(HL)(HA)2], (where M=Mn(II) and
... Show MoreInfertility can be detected when the couples have not completed pregnancy after a year or more of normal coitus. So, in order to treat infertility, there are many supported reproductive techniques are in practice. The success rate of these techniques depends upon the way by which preparation of the paternal semen sample. Over the past 30 years, the manual has been standard as providing global standards and has been used extensively by research and clinical laboratories throughout the world. The spermatozoa of all placental (eutherian) mammals, including humans, are in a protective, no labile formal at ejaculation and are incapable of fertilization even if they are placed in direct contact with an oocyte. Accordingly, they must undergo a sub
... Show MoreAnastrozole (ANZ) is considered constitute of the fourth –generation of Non–steroidal aromatase blockage, ANZ has use for hormone receptor positive breast cancer in postmenopausal women. The serious side effects of ANZ including, vaginal dryness, hot flashes, irritability, breast tenderness and un–stability in circulation.
Nanostructured lipid carriers (NLCs) have recently emerged as a multifunctional platform for drug delivery in cancer therapy.
Five formula were composed of (200 mg of glyceryl monostearate, 40 mg of oleic acid , 1% (w/w) Tween 80, 1% (w/w) Poloxamer 407, 1% (w/w) soy lecithin and Vitamin E Polyethylene Glycol Succinate.
The mean particle size, polydispersity index, zeta potential, entrapme
... Show MoreDNA methylation is one of the main epigenetic mechanisms in cancer development and progression. Aberrant DNA methylation of CpG islands within promoter regions contributes to the dysregulation of various tumor suppressors and oncogenes; this leads to the appearance of malignant features, including rapid proliferation, metastasis, stemness, and drug resistance. The discovery of two important protein families, DNA methyltransferases (DNMTs) and Ten-eleven translocation (TET) dioxygenases, respectively, which are responsible for deregulated transcription of genes that play pivotal roles in tumorigenesis, led to further understanding of DNA methylation-related pathways. But how these enzymes can target specific genes in different malignancies;
... Show MoreThe aim of present study was to develop gel formulation of microsponges of poorly soluble drug meloxicam (MLX) in order to enhance the release and dissolution of MLX which is the limitation for preparation in topical forms. Also skin delivery is an alternative administration for MLX that can minimize gastrointestinal (GI) side effects and improve patient compliance. The microsponges of MLX were prepared by quasi-emulsion solvent diffusion method. The effects of drug:polymer ratio, stirring time and Eudragit polymer type on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selec
... Show MoreBackground: Bilastine (BLA) is a second-generation H1 antihistamine used to treat allergic rhinoconjunctivitis. Because of its limited solubility, it falls under class II of the Biopharmaceutics Classification System (BSC). The solid dispersion (SD) approach significantly improves the solubility and dissolution rate of insoluble medicines. Objective: To improve BLA solubility and dissolution rate by formulating a solid dispersion in the form of effervescent granules. Methods: To create BLA SDs, polyvinylpyrrolidone (PVP K30) and poloxamer 188 (PLX188) were mixed in various ratios (1:5, 1:10, and 1:15) using the kneading technique. All formulations were evaluated based on percent yield, drug content, and saturation solubility. The fo
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