The target of this study was to synthesize several new Ciprofloxacin drug analogs by providing a nucleophilic substitution procedure that provides new functionality at the carboxylic group location. The analogs were synthesized, designed, and characterized by 1HNMR, and FTIR. The synthetic path began from the reaction of ciprofloxacin drug with morpholine to give compound[B], ciprofloxacin derivative was linked with a variety of primary and secondary amines to give compounds[B1-B9]. The above-mentioned prepared compounds [B3 and B5] were applied to liver enzymes, and the increase in the activity of these enzymes was observed. In addition, a theoretical study was conducted to study the energies and properties of the prepared compounds.
Recently, some prostate cancer patients have acquired resistance to the second -generation drugs (anzalutamide and apalutamide) prescribed for the treatment of this disease due to the emergence of the F876L mutation, which represents a challenge to modern medicine. In this study, a new series of 2-thiohydantoin derivatives were prepared through the reaction of different derivatives of maleimide (1c-4c) with isothiocyanate derivatives. The prepared compounds were diagnosed using FT-IR,1H-NMR ,13C-NMR, Mass spectra. The prepared series compounds has been studied against prostate cancer cells. The MTT assay was used to determine the activity of the prepared compounds against prostate cancer cells. The da
... Show MoreThe 4-(?-bromo acetyl)-4?-toluene sulfonanilide (2) was used as key intermediate to synthesize new heterocyclic compounds. This bromo compound was synthesized via sulfonation of amino group of p-amino acetophenone using Hinsburg method with 4-toluene sulfonyl chloride to form 4-acetyl-4?-toluene sulfonanilide (1) which is used as a starting material in this work. This compound was brominated to yield compound (2) which is used as a precursor to synthesize new five and seven membered heterocyclic compounds such as substituted 1,3-oxazoles (3,4), 1,3-thiazole derivatives (5-7), thiourea compounds (8a,b), 1,3-Thiazoline-2-thione compounds (9a-f) and 1,2,5-triazepine compounds (11a-d). The synthesized compounds were identified depending u
... Show MoreThis research includes synthesis of new heterocyclic derivatives of N-benzyl-5-bromoisatin. New 1, 2, 4-triazole, oxazoline and thiazoline derivatives of [N-benzyl-5-bromo-3-(Ethyliminoacetate)-indole-2-one] (2) have been synthesized. The preparation process started by the reaction of 5-bromoisatin with sodium hydride in dimethylformamide (DMF) at 0°C, gave suspension of sodium salt of 5-bromoisatin and subsequent reaction with benzylchloride to give N-benzyl-5-bromoisatin (1). Compound (1) reacted with ethylglycinate (Schiff base) obtained the intermediate compound (2) which reacted with different reagents in two ways. The first way, compound (2) reacted with (hydrazine hydrate, semicarbazide, phenylsemicarbazide and thiosemicarbazide)
... Show MoreIn this work two moles of 2-amino benzothiazole were allowed to react with one mole of pyromellitic dianhydride to produce N,N‾-Bis-(benzathiazol-2-yl) pyromellitamic diacid [I] which was submitted to esterification via the reaction with dimethyl sulphate in sodium carbonate in acetone as a solvent to synthesize N,N‾-bis-(benzothiazol-2-yl) pyromellitam diacetate [II] .This ester was used to produce novel compounds through two paths :- Path one:- Reaction of ester [II] with hydrazine in ethanol as a solvent to form the corresebonding N,N‾-bis (benzothiazole-2-yl) –pyromellitamic acid hydrazide [III] which react with acetyl acetone in ethanol or with phthalic anhydride in dioxa
... Show MoreIn this study, Schiff's bases [S3,S4] were synthezied by condensation of N,N-dimethyl amino benzaldehyde with primary aromatic amine[N-(hydrazinyl methyl)benzamide]. These Sciff's bases were found to react with maleic anhydride and phthalic anhydride to give 1,3Oxazepine[S5,S6,S7,S8] in good yields. The structures confired by m.p ,T.L.C.,FT.IR and 1H-NMR (of some of them).
This work contain many steps starting from esterification of isophthalic acid to yield diester compound [I] which was converted to their acid hydrazide [II], then the later compound reacted with ethylacetoacetate to yield pyrazol-5-one compound [III]. Afterword added acetyl chloride to give the compound [IV], thereaction of this compound with theiosemicarbazide ledto produce a new carbothioamide compound [V], Which was reacted with ethyl chloro acetate to yield thethioxoimidazolidin compound [VI]. The condensation reaction of this compound with different substituted aldehyde give new alkene derivatives[VII]a-d. The synthesized compounds were characterized by melting points , FT-IR ,1H-NMR and Mass spectroscopy .
Endothelin-1 (ET-1) is a potent vasoconstrictor hormone that has been identified as an important factor
responsible for the development of cardiovascular dysfunctions. ET-1 exerts its vasoconstrictor activity
through two pharmacologically distinct receptors, ETA and ETB that are found in vascular smooth muscle
cells (VSMCs) and the vasodilator activity through an ETB receptor located on endothelial cells. This study
aimed to show the impact of 1µM L-arginine (LA), 100µM tetrahydrobiopterin (BH4), and their combined
effect on ET-1 activity in both lead-treated and lead-untreated rat aortic rings. This means, investigating how
endothelial dysfunction reverses the role of nitric oxide precursor and cofa
In this study, the acid-alkaline transesterification of refined coconut seed oil (RCOSO) to fatty acid methyl ester was followed by the production of a trimethylolpropane-based thermosensitive biolubricant using potassium hydroxide, and its physicochemical characteristics were evaluated. The American Standard Test for Materials (ASTM) was employed to ascertain the biolubricant's pour point and index of viscosity, which were found to be -4 oC and 283.75, respectively. The opposite connection between lubricant viscosity and temperature was shown by the measured viscosities at varied transesterification to be transformed into biodiesel. Following this, a biolubricant was created by further transesterifiedtemperature. The ester gr
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