Small molecules drug conjugate mutual prodrug design (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide bond ; represent new interesting approaches for cancer treatment , the component of SMDC intended for targeting folate receptor , along with greater conservation of component until reaching the target tumor tissue . The designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were processed forward successfully by multistep reaction procedures , and by Thin Layer Chromatography (TLC) for preliminary detection of products and their intermediates, along with their purity. The structures of two final compounds and their intermediates were proclaimed by melting point measurement, infrared spectrometry and ¹HNMR analysis given results greatly correspond with theoretical proposed chemical structure of synthesized compounds. Furthermore, cytotoxic activity evaluation on cell line level had been done for two final compounds against human breast tumor cell (MCF-7) and human ovarian tumor cell (SKO-3) types of cancer cell line and the results were confirmed which show greater cytotoxic tumor activity of two final compounds, while compound VI possess optimal activity proportional with increased number of 6-MP molecules.
The present study was designed to synthesize a number of new Ceftriaxone derivatives by its involvement with a series of different amines, through the chemical derivatization of its 2-aminothiazolyl- group into an amide with chloroacetyl chloride, which on further conjugation with these selected amines will produce compounds with pharmacological effects that may extend the antimicrobial activity of the parent compound depending on the nature of these moieties.
Ceftriaxone was first equipped with a spacer arm (linker) by the action of chloroacetyl chloride in aqueous medium and then further reacted with seven different aliphatic and aromatic amines which resulted in the production of the aimed final target products. The syntheses
... Show MoreMyelosuppression is one of the serious adverse effects of cancer chemotherapy that lead to life threatening febrile neutropenia and considered a limiting factor for successful therapy. Cyclophosphamide a widely used anticancer drugs, induces severe bone marrow suppression by damaging hematopoietic stem cells. As cancer incidence expands globally, the demand for an effective myeloprotective therapy during cancer treatment is also increasing.Nigella sativa seed oil, a well-known plant extract that widely used for various health conditions. This study aims to evaluate the myeloprotective activity of Nigella sativa seed oil in cyclophosphamide-induced myelosuppression mice model. Myelosuppression induced by single intraperitoneal injection o
... Show MoreSchiff base (methyl 6-(2- (4-hydroxyphenyl) -2- (1-phenyl ethyl ideneamino) acetamido) -3, 3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0] heptane-2-carboxylate)Co(II), Ni(II), Cu (II), Zn (II), and Hg(II)] ions were employed to make certain complexes. Metal analysis M percent, elemental chemical analysis (C.H.N.S), and other standard physico-chemical methods were used. Magnetic susceptibility, conductometric measurements, FT-IR and UV-visible Spectra were used to identified. Theoretical treatment of the generated complexes in the gas phase was performed using the (hyperchem-8.07) program for molecular mechanics and semi-empirical computations. The (PM3) approach was used to determine the heat of formation (ΔH˚f), binding energy (ΔEb), an
... Show MoreThe objective of the study was to develop microneedle (MN) patch, with suitable properties to ensure the delivery of a therapeutic level of lornoxicam (LXM) in a period suitable to replace parenteral administration in patients, especially those who fear needles. The used polymers were cold water-soluble polyvinyl alcohol (PVA) and polyvinylpyrrolidone (PVP) of low molecular weight with PEG 400 as plasticizer and Tween 80 (to enhance the release) using micro molding technique. Patches were studied for needle morphology, drug content, axial fracture force measurement and drug release while the optimized formulas were further subjected to pH measurement, folding endurance, ex vivo permeation study, histopathology study, stability study and
... Show Moreحضرت معقدات كل من الفنادايل, الخارصين, النحاس والكادميوم بتكافؤهم الثنائي والذهب بتكافؤه الثلاثي بأستخدام صبغة ازوجديدة (6،4،2-ثلاثي هيدروكسي-3-((3-هيدروكسي فنيل) ثنائي زينيل ) فنيل ) ايثان-1-اون المحضرة من ملح الديازونيوم مع ٦,٤,٢- ثلاثي هيدروكسي اسيتوفينون بعد عزل (E)-1-(2,4,6-trihydroxy-3-((3-hydroxyphenyl)diazenyl)phenyl)ethan-1-one تم تشخيصها بواسطة الطرق الطيفية المتاحة والتقنيات التشخيصية لكل من التحليل الدقيق للعناصرواطياف كل من ال
... Show MoreThe research deals with the concept of rationalization of consumption, which is legitimately legitimized, by indicating the permissibility of consumption and its limits in Islam, the legitimate aspects of spending and its controls, and the concept of development in the Islamic economy. The researcher followed the descriptive method by presenting the legal texts and jurisprudential opinions and linking them to contemporary economic problems.The research has reached several conclusions, the most important of which is that the goal of Islam in relation to consumption is to inform the Muslim of the amount of economic maturity, and the truth of alms is good in money and religion. It is necessary for achieving maturity that both means
... Show MoreIn this paper, an attempt was made to measure and interpret the impact of several variables on global maritime transport, including: OECD industrial productions, high growth rates of some developing countries, and growth in world GDP. These variables contribute to higher rates of maritime transport revenues of 800 billion dollars annually; in the form of numerical sequences. The dry canal in Iraq was assumed to transfer 99 million tons of goods annually. This was made sure through the economic feasibility of the difference between maritime and land transport through railways. The effect of geographical and anthropological nature of Iraq on this project was studied too. Our findings indicated that the project will not drive growth
... Show MoreLeishmania is auxotroph to folic acid,antifolates drug inhibit the synthesis and conversion of folate derivatives. In this study, cytotoxic effect of methotrexate was investigated on the procyclic promastigotes proliferation of L. donovani. The results showed a significant (p ≥ 0.05) difference in growth of treated groups at high concentrations (1000, 500, 250, 125.5) μM after 24, 48 hrs., while at 72 hrs. significant difference was observed at all concentration. The IC50 values was measurable after 24, 48 and 72 hrs. and it was 174.238, 52.283 and 109.175 μM, respectively. The present study showed the cytotoxic effect of methotrexate on the proliferation of promastigotes of the visceral type of Leishmania.
The amino thiadiazole [I] on treatment with aromatic aldehydes yielded Schiff bases [IIa-c] , which cyclized to thiazolidinone [IIIa-c] derivatives by reaction with thioglycolic acid .Reaction of carbon disulfide and methyl iodide with [I] gavedithiomethyl[IV] which on treatment with o-phenylenediamine gave the condensed N-Imidazolythiadiazolylamine [V] , However , reaction of [I] with phenylisocyanate and phenylisothiocyanate afforded the carbamideand carbothiamide derivatives[VI.VII]a-c. The structure of these compounds was characterized from their melting point , FTIR spectroscopy and elementalanalysis