Heterocycles are diverse compounds that have importance in medicinal chemistry [ 1, 2]. As part of a class of oxygen-containing benzoheterocycles (fused six membered)[3], coumarins (1) are natural lactones in which the benzene ring and α-pyrone are fused together [ 4] the conjugation of coumarin with different pharmacophores gives many hybrids with various pharmacological activities [5]. Sulfonamides (SN)(2), or sulfanilamides belong to a significant class of synthetic antimicrobial medications that are used as broad-spectrum pharmaceuticals to treat bacterial infections in humans and animals
On the basis of known coumarin-based prodrug system, a novel coumarin-based mutual prodrug of 5-fluorouracil and dichloroacetic acid was designed, synthesized and evaluated as a promising oral chemotherapeutic agent basing on in vitro stability study in HCl buffer (pH 1.2) and in phosphate buffer (pH 7.4), as well as in vitro release study in human serum. The chemical structure of prodrug was confirmed by analyzing its FTIR, 1H NMR, 13C NMR and MS-ESI spectra. The results of in vitro kinetic study indicated that the prodrug was significantly stable in HCl and in phosphate buffers, and was hydrolyzed in human serum followed pseudo first order kinetics.
Keywords: Coumarin-bas
... Show MoreBy unusual method for separating two isomers of a substituted nitro-coumarin using a soxhlet extractor and in controlling temperature to get a selective nitration reaction, several new Schiff base coumarins were synthesized from nitro coumarins as starting material, which were reduced by Fe in glacial acetic acid to produce corresponding amino coumarin derivatives. Then the latter was reacted with different aromatic aldehydes to produce the desired Schiff bases derivatives. After characterization by Fourier transform infrared (FT-IR), Proton nuclear magnetic resonance (1HNMR) and Carbon-13 nuclear magnetic resonance (C-NMR), all these compounds were evaluated as potential Antimicrobial and Antioxidant Agents.
Machine learning models have recently provided great promise in diagnosis of several ophthalmic disorders, including keratoconus (KCN). Keratoconus, a noninflammatory ectatic corneal disorder characterized by progressive cornea thinning, is challenging to detect as signs may be subtle. Several machine learning models have been proposed to detect KCN, however most of the models are supervised and thus require large well-annotated data. This paper proposes a new unsupervised model to detect KCN, based on adapted flower pollination algorithm (FPA) and the k-means algorithm. We will evaluate the proposed models using corneal data collected from 5430 eyes at different stages of KCN severity (1520 healthy, 331 KCN1, 1319 KCN2, 1699 KCN3 a
... Show MoreThe purpose of this paper is to develop a hybrid conceptual model for building information modelling (BIM) adoption in facilities management (FM) through the integration of the technology task fit (TTF) and the unified theory of acceptance and use of technology (UTAUT) theories. The study also aims to identify the influence factors of BIM adoption and usage in FM and identify gaps in the existing literature and to provide a holistic picture of recent research in technology acceptance and adoption in the construction industry and FM sector.
In this study, the dynamic modeling and step input tracking control of single flexible link is studied. The Lagrange-assumed modes approach is applied to get the dynamic model of a planner single link manipulator. A Step input tracking controller is suggested by utilizing the hybrid controller approach to overcome the problem of vibration of tip position through motion which is a characteristic of the flexible link system. The first controller is a modified version of the proportional-derivative (PD) rigid controller to track the hub position while sliding mode (SM) control is used for vibration damping. Also, a second controller (a fuzzy logic based proportional-integral plus derivative (PI+D) control scheme) is developed for both vibra
... Show MoreSpeech is the essential way to interact between humans or between human and machine. However, it is always contaminated with different types of environment noise. Therefore, speech enhancement algorithms (SEA) have appeared as a significant approach in speech processing filed to suppress background noise and return back the original speech signal. In this paper, a new efficient two-stage SEA with low distortion is proposed based on minimum mean square error sense. The estimation of clean signal is performed by taking the advantages of Laplacian speech and noise modeling based on orthogonal transform (Discrete Krawtchouk-Tchebichef transform) coefficients distribution. The Discrete Kra
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Many water supplies are now contaminated by anthropogenic sources such as domestic and agricultural waste, as well as manufacturing activities, the public's concern about the environmental effects of wastewater contamination has grown. Several traditional wastewater treatment methods, such as chemical coagulation, adsorption, and activated sludge, have been used to eliminate pollution; however, there are several drawbacks, most notably high operating costs, because of its low operating and repair costs, the usage of aerobic waste water treatment as a reductive medium is gaining popularity. Furthermore, it is simple to produce and has a high efficacy and potential to degrade pollu
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