A series of new pyrazole and thiadiazole compounds including the Nabumetone moiety were conceptualized, produced, and subjected to assessment for their anti-inflammatory potential against cyclooxygenase enzyme 2. Following an Insilico test involving molecular docking analysis, the most promising compound set was synthesized and further described. After prediction of their activity by molecular docking study using Cambridge Crystallographic Data Base software tool (GOLD), We tested them in real in vivo as anti-inflammatory agents using egg white procedure. Hydrogen bonding interaction with key amino acids in COX-2 isozymes, including Arginine120, Tyrosine355, and Serine530, gave the compounds investigated in molecular docking muc

A series of novel tetrazole derivatives were designed and synthesized through ring closure.  The structures of compounds (T1-T9) were characterized by FT-IR, ¹H, and ¹³C-NMR spectroscopy. All tetrazole derivatives were screened for their antimicrobial activities against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria. All compounds showed a high activitiy against E. coli at a concentration of 0.01 mg/mL, while the tested compound T2 did not exhibit remarkable activity against Gram-positive Staphylococcus aureus. The potential DNA gyrase inhibitory activity of these compounds ( T1-T9 ) was investigated by Insilico using the molecular docking

Abstract

Objective: the idea of this study to improve transdermal permeability of Methotrexate using eucalyptus oil, olive oil and peppermint oil as enhancers.
Method: eucalyptus oil (2% and 4%), peppermint oil (2% and 4%) and olive oil (2% and 4%) all used as natural enhancers to develop transdermal permeability of Methotrexate via gel formulation. The gel was subjected to many physiochemical properties tests. In-vitro release and permeability studies for the drug were done by Franz cell diffusion across synthetic membrane, kinetic model was studied via korsmeyer- peppas equation.
Result: the results demonstrate that safe, nonirritant or cause necrosis to rats' skin and stable till 60 days gel was successfully formulated.<

                 Lercanidipine HCl, a third-generation calcium channel blocker, blocks calcium entry into smooth muscle L-type calcium channels. This action leads to a decrease in blood pressure and induces peripheral vasodilation. Lercanidipine HCl belongs to the Biopharmaceutical classification system class II category of drugs. It is practically insoluble in water and has high solubility in methanol. The oral bioavailability of lercanidipine HCl is 10%, and irregular absorption due to its poor solubility and significant first-pass metabolism. This study aimed to produce and evaluate the nanosuspension of lercanidipine HCl with improved solubility and dissolution rates. The research used the solvent/antisolvent precipit

Kidney damage in workers within environments of highly expected exposure to toxin, including heavy metals, could be a primary marker to expect hazards in population exposed to low levels of many environmental pollutants. The present study was designed to evaluate the possible effect of environmental exposure to cadmium and zinc on renal function among painters in Sulaimani city. Cross sectional study was performed on 37 male painting workers in Sulaimani city. Each worker was interviewed using structured questionnaire. Twenty five non-exposed healthy subjects were included as control group. Venous blood samples (10 ml) were obtained by vein puncture from both subjects and utilized for estimation of serum urea, creatinine levels, serum le

The purpose of this study was to investigate the effect of omega-3 poly unsaturated fatty-acids co-administered with the therapeutic dose of lornoxicam on liver of healthy rats. Twenty-eight adults male rats weighing 180-200g were used in this study and the animals were randomly divided into four groups of seven rats each. Group I: negative control/rats intraperitoneally injected with normal saline in a dose 5ml/kg/day; Group II: rats intraperitoneally injected with lornoxicam at dose 0.7 mg/kg/day; Group III: rats orally-administered omega-3 only at a dose 185mg/kg/day; Group IV: rats co-administered omega-3 (185mg/kg/day) orally and in

Drug nanocrystals are nanoscopic crystals of the parent compound with dimensions less than 1 µm. A decrease in particle size will lead to an increase in effective surface area in the diffusion layer, which, in turn, increases the drug dissolution rate. Drug nanocrystals are one of the most important strategies to enhance the oral bioavailability of hydrophobic drugs.

Cefixime is the first member of what is generally termed the third generation orally active cephalosporins. These third generation cephalosporins are distinct from the older β-lactam antibiotics in their intensive antibacterial activity against a wide range of gram-negative bacteria.

The aim of this study is to prepare nanocrystals of cefixime as a caps

Hyperglycemia and hyperinsulinemia, two common metabolic disorders associated with type 2 diabetes mellitus, are the main causes of metabolic abnormalities that result in a wide range of complications, such as cardiac dysfunction, nephropathy, neuropathy, and retinopathy. Substance-P is an 11-amino acid neuropeptide that is highly conserved and secreted by sensory nerve endings as well as different types of non-neural cells. It was believed that substance P would reduce inflammation triggered on by diabetes, interrupting the development of complications associated with this disease. The current study aims to investigate whether serum levels of substance P are associated with glycemic measures &/or lipids profile in patients with type

The isatin molecule is present in many natural substances, like plants and animals, and it is utilized to prepare compounds with various biological activities. A series of Schiff and Mannich bases derived from isatin were synthesized in this research. First, acetylenic Mannich bases (IIa-e) were prepared by a reaction of isatin with propargyl bromide and different secondary amines (morpholine, piperidine, pyrrolidine, dimethylamine, and diphenylamine) separately, and cuprous chloride (CuCl) was used as a catalyst. Second, these Mannich bases were treated with 2-aminothiazole to obtain the desired final compounds (AM1-AM5). The synthesized compounds were characterized on the basis of their spectral (FT-IR

Targeting histone deacetylase enzymes (HDACs) is an effective way to treat a variety of diseases, including cancer. A number of HDAC inhibitors (HDACi) have been clinically used. Most of the clinically used HDACi are pan-inhibitors and have poor pharmacokinetic properties. Therefore, several attempts are ongoing to develop new HDACis with optimum structural features to overcome the structural limitations. In this work, six new triazole-based compounds (k1-k6) were proposed via special modification of common pharmacophores of HDACi using 1,2,4-triazole as a zinc-binding group (ZBG), diverse group in CAP group, and hydrophobic linker. These compounds were analyzed by docking study

Histone deacetylases (HDACs) are a class of proteins that responsible of the hydrolysis of N-acetyl lysine residues in histones as well as non-histone protein substrates. This phenomenon may provide an explanation for the involvement of these enzymes in a wide range of clinical situations, encompassing cancer, metabolic, cardiovascular problems, and neurological diseases. Most of HDAC inhibitors are often used in clinical settings consist of a hydroxamate group (ZBG) that binds to zinc ion inside the active site. The poor selectivity and pharmacokinetic characteristics of numerous medicines belonging to the hydroxamates group have prompted the exploration of non-hydroximic ZBG HDAC inhibitors with a potential selectivity and potency prof

         Fibromyalgia (FM) is a common, debilitating, and chronic pain syndrome. The women are more likely to have more tender points on examination than are their male counterparts. Iraqi study showed that FM occur in 1.5% among adolescents of Iraqi population. In compare to normal healthy women, present study was revealed that Iraqi women with FM have significant elevation of calcium (p = 0.003) with significant reduction of magnesium (p = 0.001), whereas the inorganic phosphorous was not differs (p = 0.31). In conclusion, magnesium and calcium would play a crucial role in etiopathogenesis of fibromyalgia.

Key words: calcium, magnesium, phosphorous, Fibromyalgia.

Invasomes are newly developed types of nanovesicles. A vesicular drug delivery system is considered one of the approaches for transdermal delivery to enhance permeation and improve drug bioavailability. Ondansetron is a serotonin receptor antagonist used for treating vomiting associated with different clinical cases. The study aimed to prepare invasomal dispersions for improving permeation of ondansetron across the skin with a controlled release pattern. Twenty-seven formulas of ondansetron-loaded invasomes were prepared by a modified mechanical dispersion method. These formulas were optimized by studying the effect of variables on entrapment efficiency. Vesicle size, polydispersity, zeta potential, in-vitro release and ex-v

In folk medicine there are various medicinal amalgamation possessing hepatoprotective activity. This activity is of significance because several toxins cause liver injury. Hence, many pharmaceutical companies are targeting herbal medicines for the treatment of liver abnormalities and towards evolving a safe and effective formulation with desired route of administration. In current review we have focused on the studies showing hepatoprotective effect using marine compounds and plant derived compounds. Liver disorder, a global health problem, usually include acute or chronic hepatitis, heptoses, and cirrhosis. It may be due to toxic chemicals and certain antibiotics. Uncontrolled consumption of alcohol also affects liver in an unhealthy wa

Abstract:

       The aim of the current study was to investigate the possible protective effect of graded doses (5, 10, and 15mg/kg) of pyridoxine hydrochloride intraperitoneally injected against (15mg/kg) doxorubicin-induced cardiotoxicity in female rats. Fifty-six (56) Wistar albino female rats were utilized weighing 180-200 gm allocated into eight groups, seven rats each; Group I: negative control distilled water; Group II: Pyridoxine (5mg/kg); Group III: Pyridoxine (10mg/kg); Group IV: Pyridoxine (15mg/kg); Group V: doxorubicin (15 mg/kg); Group VI: Pyridoxine (5 mg/kg) prior to

A group of amino derivatives [4-aminobenzenesulfonamide,4-amino-N¹ methylbenzenesulfonamide, or N¹-(4-aminophenylsulfonyl)acetamide] bound to carboxyl group of mefenamic acid a well known nonsteroidal anti-inflammatory drugs (NSAIDs) were designed and synthesized for evaluation as a potential anti-inflammatory agent.  In vivo acute anti-inflammatory activity of the final compounds (9, 10 and 11) was evaluated in rat using egg-white induced edema model of inflammation in a dose equivalent to (7.5mg/Kg) of mefenamic acid. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-amino-N-methylbenzenesulfonamide derivative (c

Background: Cystinosis is a rare autosomal recessive lysosomal storage disease with high morbidity and mortality. It is caused by mutations in the CTNS gene that encodes the cystine transporter, cystinosin, which leads to lysosomal cystine accumulation. It is the major cause of inherited Fanconi syndrome, and should be suspected in young children with failure to thrive and signs of renal proximal tubular damage. The diagnosis can be missed in infants, because not all signs of renal Fanconi syndrome are present during the first months of life. Elevated white blood cell cystine content is the cornerstone of the diagnosis. Since chitotriosidase (CHIT1 or chitinase-1) is mainly produced by activated macrophages both in normal and inflammator

Naproxen is non-steroidal anti-inflammatory drug, which has antipyretic and anti-inflammatory effect. It is extensively bound to plasma albumin, and exhibits gastric toxicity, so it may be more efficient to deliver the drug in its sustained release dosage form and adequate blood level is achieved. Three liquid formulations with in situ gelling properties have been assessed for their potential for the oral sustained delivery of naproxen . The formulations were dilute solutions of: (a) pectin; (b) gellan gum and; (c) sodium alginate, all containing complexed calcium ion that form gels when these ions are released in the acidic environment of the stomach . The viscosity of the sols and drug release were measured, and was found to be depende

Celiac disease (CD) is an inflammatory small intestinal disorder that can lead to severe villous atrophy, and malabsorption . Since the measurement of α-amylase activity is the most widely used biochemical test for the diagnosis of pancreatic and non pancreatic disease , therefore serum α-amylase were studied in the present study in an attempt to evaluate the usefulness of this enzyme in the diagnosis of celiac disease and its relationship with anti gliadin IgA and IgG and serum glucose . Thirty one patients with celiac disease were studied and compared with twenty four healthy individuals . Significant elevation of α-amylase activity , glucose and anti gliadin IgA and IgG were observed in the sera of patients with celiac diseas

Antacids have been widely used in the treatment of various gastric and duodenal disorders such as heartburn, reflux esophagitis, gastritis, irritable stomach, gastric and duodenal ulcers. A pH-responsive of bi-polymer of sodium alginate and pectin have been studied as raft-forming polymers using sodium bicarbonate and calcium carbonate as gas-generating and calcium ion sources. The aim of study was to formulate and evaluate mono and bilayer tablets of floating and sustained release antacid delivery systems using sodium carboxy methyl cellulose as a gel forming substance, calcium and magnesium carbonate as sources of acid neutralizing and carbon dioxide gas generators agents upon contact with acidic solution. The effect of the formulation

Social factors may affect the available sources of toxic substances and causes of poisoning, and these factors may change over time. Additionally, understanding the characteristics of poisoning cases is important for treating such patients. Therefore, the present study investigated the characteristics of poisoning cases in Baghdad Poisoning Consultation Center (PCC) and Forensic Medicine Institute (FMI). Data on all poisoning cases reported in PCC and FMI during 2013 were retrospectively obtained from medical records. Total of 1131 reports of poisoning cases (1082 from PCC and 49 from FMI) were analyzed according to age, sex, geographical distribution and causes of poisoning according to the type and class of poisoning agent. The results

A total of 41 patients with gastro duodenal symptoms (show signs of inflammation with or without duodenal ulcer) . 21 males (51.2%) and 20 female (48.8%) with an average age 0f  (20 – 80) years old under  going gastrointestinal endoscopy at Baghdad teaching hospital in internal disease clinical laboratory , between (February – June)  2009 . Biopsies specimen of antrum , gastric fundus ,& duodenal bulb were examined by the following methods (rapid urease test , Giemsa stain section to detect bacteria , & Haematoxilin and Eosin stained section for pathological study which are considered the gold standard methods , sera or plasma from these patients were tested by immunochromotography (ICM),serological m

The objective of this study was to investigate and compare among five different methods of contraception including combined oral contraceptive pills (COC), Depot medroxyprogesterone acetate (DMPA), copper Intrauterine contraceptive device (IUCD), vaginal spermicides and male condom used in Hawler City through estimate of their effect, relative failure rate, percentage of use, adherence and compliance and adverse effects of each contraceptive method. In order to reach to these aims, a retrospective study was conducted in Hawler City in Azadi Health Care Center over a period of 6 months from 22^th November, 2010 to 15^th May, 2011 during which data collection and subjects follow up for 3 months had been achieved. A conv

Abstract

There are many risk factors significantly associated with readmission of diabetic patients after discharge  like surgical site reinfection with methicillin-resistant Staphylococcus aureus which has been demonstrated to be associated with more amputations, longer hospitalization , increase healthcare costs and increased mortality .This study was to describe the impact of clinical pharmacist tele-follow-up on diabetic patient’s readmission due to reinfection of methicillin-resistant Staphylococcus aureus, rate of referral to inpatients team and, return visits to the emergency department, 203 patients who were randomized into two groups. Group A (interventional group) 103 patients and group B (co

Breast cancer (BC) is the most commonly diagnosed cancer in women. The metabolism of iron is closely regulated by hepcidin which exerts its action by interacting with a ferroportin.

 The aim of the present study was to assess the alterations in the levels of some serum biomarkers that have a role in iron homeostasis (hepcidin and ferroportin) in addition to hematological parameters (hemoglobin, leukocyte and platelets count) in different stages of BC.

This study included 66 women with BC. The patients were categorized as follows : group 1 includes :22 patients with stage I disease ,group 2 includes: 22 patients with stage II disease ,and group 3 include: 22 patients with stage III disease .Group 4 includes :22 appare

Hedera helix L. plant belongs to the family Araliaceae that provide a host of bioactive compounds (mainly saponins) of important biological activities, like spasmolytic, secretolytic, anti-inflammatory, and antibacterial activities. Literature survey revealed that there was no previously study concerning H. helix L. which is cultivated in Iraq, so we decided to carry out this study which include extraction, isolation, purification and identification of biologically important triterpenoid saponin hederacoside C from leaves of H. helix L. Extraction of hederacoside C was carried out using two methods; in the first method maceration  was done with methanol 99.8% and in the second method soxhlet extraction wit

Abstract

The  common types of movement disorders are ; dystonia which is a syndrome  of  repetitive muscle contractions. While , Huntington disease is autosomal dominant progressive neurodegenerative disorder, which is characterized by involuntary movements (“chorea”).

Tetrabenazine therapy has been shown to effectively control this movements compared with placebo.

Design the proper dosing approach for patients treated with tetrabenazine with genotype polymorphisms and their hepatic effect on patients.

A prospective case controlled study was carried on 50 patients whom    divided into 2 groups :first group involved 25 patients who had cho

         Certain cyclic amine derivatives of metronidazole via acetate spacer were prepared. Cyclic amines used are piperidine and piperazine to improve the physicochemical properties and reduce some of metronidazole side effects. This is believed to be done by modification of its structural features to get prodrugs with improved properties over that of metronidazole. The present work includes esterification of metronidazole with choroacetic acid, N-alkylation of the cyclic amines by the halogenated ester and characterization of their structures by spectral(UV and IR) and elemental(CHN)analysis.The melting points, degree of solubilities and partition coefficients were also determined. Both metronid

One of the most common metabolic illnesses in the world is diabetes mellitus. This metabolic disease is responsible for a large percentage of the burden of kidney damage and dysfunction. The goal of this study was to look into the renal function of diabetic patients using metformin monotherapy who came to Mosul's Al-Wafaa diabetes care and research facility. During the period 1 January 2021 to 30 April 2021, 47 patients with T2DM (age 50.48 7.74 years) were enrolled in this case-control study. These patients' results were compared to a control group of 47 seemingly healthy people (age 45.89 9.06 years). All participants' demographic and medical histories were acquired through the delivery of a questionnaire. Blood samples were collected

The present study aim at preparing frusemide in liquid form suitable for oral use. This is achieved through preparing different liquid forms of frusemide. The frusemide liquid is prepared in the following forms: oral solution, syrup and elixir with intensity of 1, 0.4 and 0.8% weight /volume respectively and in combination with potassium carbonate, polysorbate 80, alcohol and phosphate buffer solution of pH8 to dissolve the frusemide in the above mentioned forms. The different forms of the prepared medicine have been stored in glass bottles that can provide protection against light and at 40, 50, 60⁰C for four months. Besides the pH has been checked to decide the period of validity. The results show that the expiration date of