A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of diclofenac sodium in the 60–240 minute time interval time, and compound 13 showed a comparable effect to that of diclofenac sodium at all experimental times. The result of this study indicates that the incorporation of the 4-(methylsulfonyl)aniline pharamacophore into naproxen, indomethacine, diclofenac and mefanamic acid maintained their anti-inflammatory activity and may increase selectivity towards the COX-2 enzyme which will be confirmed in the future by assessing COX-2: COX-1 inhibitory ratios using a whole blood assay.
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-vivo perm
... Show MoreBackground: Contact between implant material and bones must be strong and fast creation, to fulfill these properties appropriate surface modifications must apply on used implants. In this contribution; double surface modifications are applied on Ti-6Al-4V alloy to accelerate osseointegration. Materials and methods: Anodic process is utilized to create titania nanotubes (TNTs) on the screws made from Ti-6Al-4V alloy. These implants were coated with nano ZrO2 particles. Second modification was annealing anodized screws at 8000C, and implanted in tibiae of nine adult New Zealand white rabbits. Results: Physical and histological consequences of two surface modifications on Ti-6Al-4V alloy screws were studied. Scanning electron microscope (SEM)
... Show MoreThe evacuated tube solar collector ETC is studied intensively and extensively by experimental and
theoretical works, in order to investigate its performance and enhancement of heat transfer, for Baghdad climate
from April 2011 till the end of March 2012. Experimental work is carried out on a well instrumented collector
consists of 16 evacuated tubes of aspect ratio 38.6 and thermally insulated tank of volume 112L. The relation
between convective heat transfer and natural circulation inside the tube is estimated, collector efficiency, effect of
tube tilt angles, incidence angle modifier, The solar heating system is investigated under different loads pattern (i.e
closed and open flow) to evaluate the heat loss coefficient
Generally, direct measurement of soil compression index (Cc) is expensive and time-consuming. To save time and effort, indirect methods to obtain Cc may be an inexpensive option. Usually, the indirect methods are based on a correlation between some easier measuring descriptive variables such as liquid limit, soil density, and natural water content. This study used the ANFIS and regression methods to obtain Cc indirectly. To achieve the aim of this investigation, 177 undisturbed samples were collected from the cohesive soil in Sulaymaniyah Governorate in Iraq. Results of this study indicated that ANFIS models over-performed the Regression method in estimating Cc with R2 of 0.66 and 0.48 for both ANFIS and Regre
... Show MoreIn the present study a series of some four-,five-and seven-membered heterocyclic compounds have been synthesized by the reaetion of Schiff bases (1a,b) with chloroacetyl chloride, sodium azide, thioglycolic acid or various anhydrides to give azetidinone (2a,b), tetrazole (3a,b), thiazolidinone (4a,b) and 1,3-oxazepine derivatives (5-8a,b) respectively. Schiff bases (1a,b)were prepared from the reaction of p-toluidine with aromatic aldehydes. All synthesized compounds were characterized by physical properties and spectral data.
The present work involved synthesis of several new N-Sulfamethoxazol derivatives imide on Polymeric chain by two steps. The first stip involved preparation of N- (sub.orunsub benzoyl and sub unsub acetyl) amidyl sub sulfamethoxazole (1-5) by condensation of sulfamethoxazole drug with many substituted acid chloride, then the second step include, preparation new five N-(acrly-N–sub or unsub benzoyl) imidyl substituted sulfamethoxazol(6-10) by reaction of poly acryloyl chloride with the prepared compound (1-5) in first stepin asuitable solvent in the presenceamount triethylamine (Et3N) with heating. The structure confirmations of all polymers wereconfirmed using FT-IR,1H-NMR,13C-NMR and UV spectroscopy. Other physical properties including so
... Show MoreThe sol-gel route using an agar gel with calcium nitrate and phosphate solution as starting materials for producing hydroxyapatite (HAP). The product formed were needle like, zigzag and straight fibres. The fibrous products on sintering transformed into stoichiometric HAP with a biological Ca/P ratio of 1.67. The influences of pH, temperature, nature of base and phosphate solution on the growth of fibrous HAP were studied. The pH of the solution was found to greatly influence the growth rate and morphology of the resultant product. The optimum gel temperature was found to be 60oC and sintering temperature of 900oC for 1 hour. The crystalline, thermal, functional and morphological characteristics of the fibrous HAP were investigated.
In this research, two drugs were bonded through amide and ester attachment, using lactic acid as aspacer binder, produced di pro drug such as Procain and Ciprofloxacin. Since Procain has ailocail anesthetic action and Ciprofloxacin as antibacterial drug was reacted with lactic acid produced ester compound (1), then the carboxylic acid of lactic acid could reacted with free Procain oil produced amide attachment, the controlled drug release in different pH values at 37C˚was studied to improve their characteristic and to minimize the side effect of the drug could be used in broad spectrum activity as atherapeutic material.This mutual prodrug was used with another biological active drug instead of single action. The prepared prodrug was charac
... Show MoreThe present work involved synthesis of serval new substituted tetrazole via Schiff bases for trimethoprim drug by two steps. The first step involved direct reaction of different ketones and aldehydes with trimethoprim producing the corresponding Schiff bases (1-10), whereas the second step, involved preparation new tetrazoles derivatives (11-20) through reaction of the ready Schiff bases (in the first step) with sodium azidein in dioxin. The prepared compounds were characterized by UV, FT-IR, and some of them by 13C-NMR, 1H-NMR spectroscopy and physical properties.
The interest in calcium phosphates arises from the fact that bones contain a high percentage of mineralized calcium phosphate . In this study, pure and biocompatible hydroxyapatite (HAP) powder was successfully synthesized using hen’s egg shell as calcium source and phosphoric acid by precipitation method.The precipitate obtained was subjected to ripenning process for 24 hours, filtered, air dried, and calcined at temperatures of 400,800,900,and 1000 ºC.
X-Ray diffraction(XRD) technique was used to investigate the formation of HAP powder, XRD results revealed the HAP formation and also indicate no occurrence of secondary phases. Fourier Transform Infrared(FT-IR) spectrum shows the characterstic peaks for phosphate and hydroxyl grou