Etodolac is choice of drug for pain and inflammation but has major side effects of gastric ulcers that are due to free carboxylic group. Etodolac belongs to the chemical class of non-selective COX-inhibitor but preferentially COX-2 inhibitor. Here the ester linked mutual prodrugs of etodolac with phytophenols like vanillin, carvacrol, umbelliferone, guaiacol, sesamol and syringaldehyde were synthesized. All the prodrugs were characterized by IR-spectroscopy, 1H-NMR, 13C-NMR and mass spectrometry. Among the synthesized prodrugs, the Eto-van, Eto-umbe, Eto-sesa and Eto-syr showed improved analgesic and anti-inflammatory activity compared to etodolac. All the synthesized prodrugs showed less ulcerogenic side effects compared to etodolac.
Eruca sativa (jarjeer) is an annual herb (family Brassicaceae), which contains a wide range of chemicals and minerals with nutraceutical and organoleptic characteristics. Jarjeer was generally used as a food and traditionally mainly consumed due to its aphrodisiac properties. This crop known to contain various phytochemicals such as flavonoids, phenolic acids, terpens, carotenoids, tannins, glycosides, saponins, sterols, alkaloids, and other secondary metabolites. In leaves, kaempferol and its derivatives, glucosativin, are the main flavonoids and glucosinolate, respectively, while erucic acid and glucoerucin are the main fatty acid and glucosinolate, respectively. Medicinally, the plant has antibacterial, antidiabetic, antihyperten
... Show MoreIn 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 MorePsidium guajava, belonging to the Myrtaceae family, thrives in tropical and subtropical regions worldwide. This important tropical fruit finds widespread cultivation in countries like India, Indonesia, Syria, Pakistan, Bangladesh, and South America. Throughout its various parts, including fruits, leaves, and barks, guava boasts a rich reservoir of bioactive compounds that have been traditionally utilized as folkloric herbal medicines, offering numerous therapeutic applications. Within guava, an extensive array of Various compounds with antioxidative properties and phytochemical constituents are present, including essential oils, polysaccharides, minerals, vitamins, enzymes, triterpenoids, alkaloids, steroids, glycosides, tannins, fl
... Show MoreMefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-t
... Show MoreMeloxicam is a non-steroidal anti-inflammatory drug. It is practically insoluble in water. It is associated with gastrointestinal side effects at high doses on long term treatment. The aim of this investigation to formulate and evaluate gellified nanoemulsion of meloxicam as a topical dosage form to enhance meloxicam therapeutic activity and reduce systemic side effect.
The pseudo ternary phase diagrams were made, including the oil mixture which is composed of almond oil and peppermint oil at a ratio (1:2), variable surfactant mixture (S mix) which are tween 80 and ethanol at ratios of (1:1, 2:1, 3:1, and 4:1) and double distilled water. Slow dripping of double distilled water to the combination of the oil mixtu
... Show MoreBioavailability is the objective for an optimum formulation. The target of the analysis is to maximize both the fluidity and disintegration profile of class II weakly compounds that are water-soluble. Anti-dyslipidemia drug rosuvastatin calcium (RC) (bioavailability 20%) through formulating as nanofibers (NFs) using electrospinning (ES) technology. Twenty formulas were prepared, and different polymers and polymer combinations with various concentrations were used such as polyethylene oxide (PEO) polyvinyl pyrrolidine (PVPK-30), and hydroxypropyl methylcellulose (HPMC). Three distinct groups of maximum parameters, including polymeric solution, electrospinning method, and ambient parameter, are capable of influencing the creation alon
... Show MoreA new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity ag
... Show MoreThe Fylex extract exert a high inhibition effect against A . flavus growth on PDA medium, as the fungus growth was completely inhibited by 100% at a concentration of 0.2 and 0.3% of studied extract, while the lowest inhibition percentage (71%) was found at a concentration of 0.1%. Whereas magnesium oxide nanoparticles showed the highest inhibition ratio of A. flavus (100%) was detected at 0.2% and the lowest inhibition ratio (81.66%) was at concentration 0.5%. Moreover, the addition of G. lucidum powder to PDA medium with a concentration of 2.5 mg increased the inhibition rate of A. flavus growth which was 54.4%, while the lowest inhibition ration (18.22%) was found at a concentration of 1000 mg. The milky liquid (brocade milk) of Calotropi
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