In this research some new nucleoside analogues were synthesized. Starting from α-D- glucose which was protected to glucose penta acetat α-D- glucose pyronside (1). Which was converted to active form 1-bromo protected sugar (2) as a sugar moiety. The base moiety 2-substituted imidazoline (3,4) was prepared from condensation of ethylene diamine with two kind of aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleaobase derivatives (5-10). Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues (11-16). De blocking of these nucleoside analogues with sodium methoxide in methanol afforded our target the free nucleoside analogues (17-22).All prepared compounds were identified by FT-IR and some of them with 1H-NMR and 13C-NMR spectroscopy. Some of synthesized nucleoside analogues were screened for their antibacterial activity against four types of bacteria, also against four types of fungi.
Solubility problem of many of effective pharmaceutical molecules are still one of the major obstacle in theformulation of such molecules. Candesartan cilexetil (CC) is angiotensin II receptor antagonist with very low water solubility and this result in low and variable bioavailability. Self- emulsifying drug delivery system (SEDDS) showed promising result in overcoming solubility problem of many drug molecules. CC was prepared as SEDDS by using novel combination of two surfactants (tween 80 and cremophore EL) and tetraglycol as cosurfactant, in addition to the use of triacetin as oil. Different tests were performed in order to confirm the stability of the final product which includes thermodynamic study, determination of self-emulsificat
... Show MoreBackground: Rheumatoid arthritis is an autoimmune disease that affects mainly the synovial membranes and articular structures and is characterized by chronic, systemic inflammation involving multiple joints.Being a synovial joint, the Temporomandibular Joint is subject to the same disorders affecting other synovial joints, including RA.Beside it was considered as a specific serological marker for diagnosing RA disease ,antibodies to cyclic citrullinated peptide have proven to be associated with joints destruction, though; it may play a potential role in the prediction of the disease severity. Materials and Methods: Sixty nine individuals (69) were enrolled in this study, forty nine (49) were patients diagnosed with Rheumatoid Arthritis, a
... Show MorePreparation and Identification of some new Pyrazolopyrin derivatives and their Polymerizations study
Abstract
The target derivative are gentamicin linked with L-Val- L-Ala by an ester linkage. These were synthesized by esterification method, which included the reaction of -OH hydroxyl group on (carbon No.5) of gentamicin with the acid chloride of the corresponding dipeptide, The preparation of new derivative of gentamicin involved protected the primary & secondary amine groups of Gentamicin, by Ethylchloroformate (ECF) to give N-carbomethoxy Gentamicin which was used for further chemical synthesis involving the free hydroxyl groups.
Then prepared dipeptide (L-Val- L-Ala) by conventional solution method in present DCC & HoBt then reacted with thionyl
... Show MoreNew derivatives of pyromellitamic diacids and pyromellitdiimides have been prepared by the reaction of one mole of pyromellitic dianhydride with two moles of aromatic amines, these derivatives were characterized by elemental analysis, FT-IR and melting point.
The present work describes guggul as a novel carrier for some anti-inflammatory drugs. Guggulusomes containing different concentration of guggul with aceclofenac were prepared by sonication method and characterized for vesicle shape, size, size-distribution, pH, viscosity, spread ability, homogeneity, and accelerated stability in-vitro drug permeation through mouse skin. The vesicles exhibited an entrapment efficiency of 93.2 ± 12%, vesicle size of 0.769 ± 3μm and a zeta potential of - 6.21mV. In vitro drug release was analyzed using Franz’s diffusion cells. The cumulative release of the guggulusomes gel (G2) was 75.8% in 18 hrs, which is greater than that all the gel formulation. The stability profile of prepare
... Show MoreThis paper deals with novels for group of Iraqi Women novelists published in the time period 2003 – 2013, and the functioning of temporal anomalies in the Iraqi Women's narrative.
In general, the novel contains structural elements such as: the characters, events and the places, these elements must be collected by an artist creating a complete work of fiction. However the time dominates the other elements through progression and regaining called Time paradox, it has a modern critical importance because of its impact in highlighting of political, social and cultural events that make up the fictional environment which cast a shadow over other techniques. And that it is clear in the course of the narrative.
In this paper, we studied the scheduling of jobs on a single machine. Each of n jobs is to be processed without interruption and becomes available for processing at time zero. The objective is to find a processing order of the jobs, minimizing the sum of maximum earliness and maximum tardiness. This problem is to minimize the earliness and tardiness values, so this model is equivalent to the just-in-time production system. Our lower bound depended on the decomposition of the problem into two subprograms. We presented a novel heuristic approach to find a near-optimal solution for the problem. This approach depends on finding efficient solutions for two problems. The first problem is minimizing total completi
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