4-amino-3-(4-(((4-hydroxy-3, 5dimethoxybenzyl) oxy) methyl) phenyl)-1, 2, 4-triazole-5-thione was synthesized by to method the first one from melt reaction of 4-(((4-hydroxy-3, 5-dimethoxybenzyl) oxy) methyl) benzoic acid with Thiocarbonyldihydrazide, the second method from convert the corresponded acid hydrazide to potassium 2-(4-(((4-hydroxy-3, 5-dimethoxybenzyl) oxy) methyl) benzoyl) hydrazinecarbodithioate salt then react with hydrazine hydrate. Newly Schiff base (7a-7f) were synthesized from reaction the 4-amino-1, 2, 4-triazol with substituted hydroxybenzaldehyde. The resulting compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS data. 2, 2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to screened the antioxidant properties of the synthesized compounds. Compounds 7d, 7e and 7f exhibited significant free-radical scavenging ability in both assays.
A small number of researches were done in the design and synthesis of enkephalin analogues that are able to resist degradation effect of proteolytic enzymes with good bioavailability and half-lives.Through studying structure activity relationships we tried to incorporate phthalyl group, tryptophan and lysine amino acids in different positions in the basic backbone structure of the naturally occurring opioid Leu5- and Met5- enkephalin, in the hope that such insertion of these amino acids could induce interesting addition in the biological activity of these analogues with enhancement of their bioavailability, in addition to decrease side effects as addiction liability.
These synthesized peptides are:
This work includes synthesis of sugar tetrazole derivative, D-ribose reacted with acetone in the presence of sulfuric acid H2SO4 to give 2, 3-O-isopropylidene-D-ribose (1). The Aldol condensation of (1) with formaldehyde in methanolic K2CO3 solution gave 2-hydroxymethyl (2, 3-O-isopropylidene-D-ribose)(2). Which was tosylated by Tosyl chloride in pyridine to yield compound (3), SN2 reaction of (3) with sodium cyanide in DMSO afforded compound (4). The [2+ 3] cycloaddition reaction of (4) with sodium azide gave the targeted compound (5). All prepared compounds have been characterized by: TLC, Specific rotation, Microelemental analysis and [FTIR and 1 H NMR spectroscopy]
Two molecular imprinted polymer (MIP) membranes for Levofloxacin (LEV) were prepared based on PVC matrix. The imprinted polymers were prepared by polymerization of styrene (STY) as monomer, N,N methylene di acrylamide as a cross linker ,benzoyl peroxide (BPO) as an initiator and levofloxacin as a template. Di methyl adepate (DMA) and acetophenone (AOPH) were used as plasticizers , the molecular imprinted membranes and the non molecular imprinted membranes were prepared. The slopes and detection limits of the liquid electrodes ranged from -21.96 – -19.38 mV/decade and 2×10-4M- 4×10-4M, and Its response time was around 1 minute, respectively. The liquid electrodes were packed with 0.1 M standar
... Show MoreAmoxicillin 1 was treated with thiosemicarbazide and Phosphoryl chloride to obtain a new derivatives that contains 1,3,4-thiadiazole moiety 2. Schiff bases compounds were synthesized by the reaction of compound 2 with different aldehydes such as benzaldehyde and some substituted Benzaldehyde; p-hydroy, p-Chloro, p-Nitro, p-Dimethylamino, p-Methyl, p-Methoxy, p-Ethoxy to give compounds 3a-h. The obtained compounds have tested towards gram -ve and gram +ve bacteria. The compound shows good to moderate result towards the bacteria.
Till now, isatin derivatives have received a lot of interest in organic and medicinal chemistry due to their significant biological and pharmacological activities. Schiff’s and Mannich bases of isatins are an effective group of heterocyclic derivatives that play a significant role in medicinal chemistry as antimicrobial agents. In light of these facts, new Schiff bases and Mannich bases of isatin were synthesized. The monomer Mannich bases; 3(a-e) have been synthesized by reacting isatin with different secondary amines, piperidine, morpholine, and pyrrolidine, dimethylamine, diphenylamine, separately, and formaldehyde, while the dimer (5) formed by using piperazine and formaldehyde which then react separately with Phenylhydrazine
... Show MoreThe outbreak of a current public health coronavirus 2019 disease is a causative agent of a serious acute respiratory syndrome and even death. COVID-19 has exposed to multi-suggested pharmaceutical agents to control this global disease. Baricitinib, a well-known antirheumatic agent, was one of them. This article reviews the likely pros and cons of baricitinib in attenuation of COVID-19 based on the mechanism of drug action as well as its pharmacokinetics. The inhibitory effect of baricitinib on receptor mediated endocytosis promoter, AKK1, and on JAK-STAT signaling pathway is benefacial in inhibition of both viral assembling and inflammation. Also, its pharmacokinetic has encouraged the physicians toward the drug
... Show MoreBackground Many antidiabetic medications with distinct modes of action are available, The sodium glucose cotransporter-2 (SGLT-2) inhibitors are among the most recent oral antihyperglycemic medications. The American Diabetes Association recommends metformin, a biguanide medication, as the first option for oral control of type 2 diabetes because it has demonstrated promise in this regard. Aim of the study To evaluate and compare the effects of metformin and SGLT-2 inhibitors on general urine parameters in T2DM patients from Iraq. Method a prospective cohort study where 101 adult patients of both sexes aged under 70 years and newly diagnosed with T2DM, patients were divided into two groups, Metformin group (n=52), where metformin was p
... Show MoreSARS-CoV-2 stands for severe acute respiratory syndrome coronavirus 2 which is the causative agent of spreading coronavirus disease 2019 that is known as COVID-19 pandemic, the disease leads to severe acute respiratory illness. Matrix metalloproteinases- 9 (MMP-9) plays several important physiological functions. This enzyme could also be implicated in the "cytokine storm" in some way, which may represent one of the possible scianrios during coronavirus infection, in addition to its role in the mechanism of lung fibrosis on molecular basis.. The tissue inhibitors of metalloproteinase (TIMPs) are well characterized for controlling the activity of MMPs in extracellular matrix remodeling. They also considered as signaling molecules anal
... Show MoreSARS-CoV-2 stands for severe acute respiratory syndrome coronavirus 2 which is the causative agent of spreading coronavirus disease 2019 that is known as COVID-19 pandemic, the disease leads to severe acute respiratory illness. Matrix metalloproteinases- 9 (MMP-9) plays several important physiological functions. This enzyme could also be implicated in the "cytokine storm" in some way, which may represent one of the possible scianrios during coronavirus infection, in addition to its role in the mechanism of lung fibrosis on molecular basis.. The tissue inhibitors of metalloproteinase (TIMPs) are well characterized for controlling the activity of MMPs in extracellular matrix remodeling. They also considered as signaling molecules anal
... Show More