scholarly journals Synthesis, Characterization and Anti-Diabetic Activity of 1,3,5-Triaryl-2-Pyrazolines in Acetic Acid Solution under Ultrasound Irradiation

2013 ◽  
Vol 14 ◽  
pp. 172-185 ◽  
Author(s):  
M. Emayavaramban ◽  
N. Santhi ◽  
C. Gopi ◽  
C. Manivannan ◽  
A. Raguraman
Keyword(s):  
Sodium Hydroxide Solution ◽  
Acetic Acid Solution ◽  
Ultrasound Irradiation ◽  
Temperature Treatment ◽  
Reference Drug ◽  
H Nmr ◽  
Phenylhydrazine Hydrochloride ◽  
Semicarbazide Hydrochloride ◽  
New Compounds

A chalcone was prepared by the reaction of 4-methylbenzaldehyde with 4-methylacetophenone in dilute methanolic sodium hydroxide solution under ultrasonic irradiationin the water bath of an ultrasonic cleaner at room temperature. Treatment of this chalcone with thiosemicarbazide/semicarbazide hydrochloride/benzhydrazide/benzenesulphonyl hydrazide/phenylhydrazine hydrochloride afforded the corresponding 2-pyrazoline in good yields. All the new compounds have been characterized by IR, 1H-NMR, 13CNMR spectral data. All the target compounds were evaluated for their In Vivo anti-diabetic activity in rates in comparison with as reference drug.

scholarly journals Design, Synthesis, and Acute Anti-inflammatory Assessment of New 2-methyl Benzoimidazole Derivatives Having 4-Thiazolidinone Nucleus

2019 ◽  
pp. 151-160
Keyword(s):  
Molecular Docking ◽  
Control Group ◽  
Design Synthesis ◽  
Reference Drug ◽  
Reference Ligand ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Cox 2 Inhibitors

New two derivatives of 2- methyl benzoimidazole were designed, synthesized and evaluated as a potential cyclooxygenase-2 [COX-2] inhibitors. The synthesized compounds have been recognized according to their spectral FT-IR, 1H-NMR data and physical pro- perties. The newly synthesized compounds were investigated in vivo for their anti-inflammatory activities using egg-white stimulated paw edema method with respect to the effect of propylene glycol 50%v/v [control group] and the ibuprofen [10mg/kg i.p.] was selected as a reference ligand. New compounds showed a significantly higher in vivo anti-inflammatory activity compared with ibuprofen as a reference drug. COX-2 selectivity evaluation through molecular docking via GOLD suite [v. 5.6.2.]. The new compounds via molecular docking showed significant higher activities when compared with ibuprofen as referenced drugs because of having hydrogen bonding interaction toward the key amino acids within COX-2 structure and all these results were compatible with the study of in vivo acute anti-inflammatory activities for tested compounds. ADME studies were performed to predict absorption, bioavailability, topological polar surface area, and drug-likeness. The results of ADME studies showed that all synthesized compounds absorbed from the gastrointestinal tract.

Nyctanthes Arbor-Tristis and its Role in the Alleviation of Arthritic Pain: A Review

2020 ◽  
Vol 16 (8) ◽  
pp. 1147-1156
Author(s):  
Ruchi Singh ◽  
Syed M. Hasan ◽  
Amit Verma ◽  
Sanjay K. Panda
Keyword(s):  
Research Work ◽  
Plant Distribution ◽  
Pharmacological Activities ◽  
Whole Plant ◽  
Modern Drug ◽  
Active Chemical ◽  
Drug Synthesis ◽  
New Compounds

Background: A plant is a reservoir of potentially useful active chemical entities which act as drugs as well as intermediates for the discovery of newer molecules and provide newer leads for modern drug synthesis. The demand for new compounds in the field of medicine and biotechnology is centuries old and with a rise in chronic diseases and resistance to existing drugs in the field of anti-infective agents, the chemicals obtained from plant sources have been an area of attraction. The whole plant has possessed multiple pharmacological activities. This is scientifically established by in-vivo and in-vitro studies. Methods: Various electronic databases such as PubMed, Science Direct, Scopus and Google were searched to collect the data of the present review. All the collected information is categorized into different sections as per the aim of the paper. Results: Fifty-six research and review papers have been studied and were included in this review article. After a detailed study, we provide a significant description of various phytochemicals present in Nyctanthes arbor-tristis Linn., which is responsible for various pharmacological activities. Twenty of studied articles gives a general introduction and ethnobotanical information about the plant, two papers contained microscopic detail of leaf and fruit. Twenty papers contained information about the phytoconstituents present in different parts of Nyctanthes arbor-tristis plant and fourteen articles reported pharmacological activities like antioxidant, anti-inflammatory, antiarthritic, antimicrobial and immunobiotic activity. Conclusion: This review explores the published research work comprising the ethnobotanical description of the subjected plant, distribution, phytochemical profile, and arthritis-related pharmacological activities.

scholarly journals G2-S16 Polyanionic Carbosilane Dendrimer Can Reduce HIV-1 Reservoir Formation by Inhibiting Macrophage Cell to Cell Transmission

2021 ◽  
Vol 22 (16) ◽  
pp. 8366
Author(s):  
Ignacio Relaño-Rodríguez ◽  
María de la Sierra Espinar-Buitrago ◽  
Vanessa Martín-Cañadilla ◽  
Rafael Gómez-Ramírez ◽  
María Ángeles Muñoz-Fernández
Keyword(s):  
T Cells ◽  
Developed Countries ◽  
Main Role ◽  
Viral Particles ◽  
Carbosilane Dendrimer ◽  
Science Community ◽  
New Compounds ◽  
Hiv 1

Human immunodeficiency virus (HIV-1) is still a major problem, not only in developing countries but is also re-emerging in several developed countries, thus the development of new compounds able to inhibit the virus, either for prophylaxis or treatment, is still needed. Nanotechnology has provided the science community with several new tools for biomedical applications. G2-S16 is a polyanionic carbosilane dendrimer capable of inhibiting HIV-1 in vitro and in vivo by interacting directly with viral particles. One of the main barriers for HIV-1 eradication is the reservoirs created in primoinfection. These reservoirs, mainly in T cells, are untargetable by actual drugs or immune system. Thus, one approach is inhibiting HIV-1 from reaching these reservoir cells. In this context, macrophages play a main role as they can deliver viral particles to T cells establishing reservoirs. We showed that G2-S16 dendrimer is capable of inhibiting the infection from infected macrophages to healthy T CD4/CD8 lymphocytes by eliminating HIV-1 infectivity inside macrophages, so they are not able to carry infectious particles to other body locations, thus preventing the reservoirs from forming.

Synthesis, investigation of biological effects and in silico studies of new benzimidazole derivatives as aromatase inhibitors

2020 ◽  
Vol 75 (9-10) ◽  
pp. 353-362
Author(s):  
Begüm Nurpelin Sağlık ◽  
Ahmet Mücahit Şen ◽  
Asaf Evrim Evren ◽  
Ulviye Acar Çevik ◽  
Derya Osmaniye ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
In Silico ◽  
Biological Effects ◽  
Docking Studies ◽  
Benzimidazole Derivatives ◽  
Binding Modes ◽  
Reference Drug ◽  
In Silico Studies ◽  
New Compounds ◽  
Mcf 7

AbstractInhibition of aromatase enzymes is very important in the prevention of estrogen-related diseases and the regulation of estrogen levels. Aromatase enzyme is involved in the final stage of the biosynthesis of estrogen, in the conversion of androgens to estrogen. The development of new compounds for the inhibition of aromatase enzymes is an important area for medicinal chemists in this respect. In the present study, new benzimidazole derivatives have been designed and synthesized which have reported anticancer activity in the literature. Their anticancer activity was evaluated against human A549 and MCF-7 cell lines by MTT assay. In the series, concerning MCF-7 cell line, the most potent compounds were the 4-benzylpiperidine derivatives 2c, 2g, and 2k with IC50 values of 0.032 ± 0.001, 0.024 ± 0.001, and 0.035 ± 0.001 µM, respectively, compared to the reference drug cisplatin (IC50 = 0.021 ± 0.001 µM). Then, these compounds were subject to further in silico aromatase enzyme inhibition assays to determine the possible binding modes and interactions underlying their activity. Thanks to molecular docking studies, the effectiveness of these compounds against aromatase enzyme could be simulated. Consequently, it has been found that these compounds can be settled very properly to the active site of the aromatase enzyme.

scholarly journals Antibacterial and In Vivo Studies of a Green, One-Pot Preparation of Copper/Zinc Oxide Nanoparticle-Coated Bandages

Membranes ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 462
Author(s):  
Archana R. Deokar ◽  
Ilana Perelshtein ◽  
Melissa Saibene ◽  
Nina Perkas ◽  
Paride Mantecca ◽  
...  
Keyword(s):  
Zinc Oxide ◽  
Metal Oxide ◽  
Ultrasound Irradiation ◽  
Face Mask ◽  
In Vivo Studies ◽  
One Pot ◽  
The Face ◽  
Bulk Scale ◽  
Particle Size And Shape

Simultaneous water and ethanol-based synthesis and coating of copper and zinc oxide (CuO/ZnO) nanoparticles (NPs) on bandages was carried out by ultrasound irradiation. High resolution-transmission electron microscopy demonstrated the effects of the solvent on the particle size and shape of metal oxide NPs. An antibacterial activity study of metal-oxide-coated bandages was carried out against Staphylococcus aureus (Gram-positive) and Escherichia coli (Gram-negative). CuO NP-coated bandages made from both water and ethanol demonstrated complete killing of S. aureus and E. coli bacteria within 30 min., whereas ZnO NP-coated bandages demonstrated five-log reductions in viability for both kinds of bacteria after 60 min of interaction. Further, the antibacterial mechanism of CuO/ZnO NP-coated bandages is proposed here based on electron spin resonance studies. Nanotoxicology investigations were conducted via in vivo examinations of the effect of the metal-oxide bandages on frog embryos (teratogenesis assay—Xenopus). The results show that water-based coatings resulted in lesser impacts on embryo development than the ethanol-based ones. These bandages should therefore be considered safer than the ethanol-based ones. The comparison between the toxicity of the metal oxide NPs prepared in water and ethanol is of great importance, because water will replace ethanol for bulk scale synthesis of metal oxide NPs in commercial companies to avoid further ignition problems. The novelty and importance of this manuscript is avoiding the ethanol in the typical water:ethanol mixture as the solvent for the preparation of metal oxide NPs. Ethanol is ignitable, and commercial companies are trying the evade its use. This is especially important these days, as the face mask produced by sonochemistry (SONOMASK) is being sold all over the world by SONOVIA, and it is coated with ZnO.

scholarly journals Organic-Inorganic Hybrid Hollow Mesoporous Organosilica Nanoparticles for Efficient Ultrasound-Based Imaging and Controlled Drug Release

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Xiaoqin Qian ◽  
Wenping Wang ◽  
Wentao Kong ◽  
Yu Chen
Keyword(s):  
Drug Release ◽  
Ultrasound Irradiation ◽  
Controlled Drug Release ◽  
Inorganic Hybrid ◽  
Templating Method ◽  
Anticancer Drug Delivery ◽  
Cavitation Effect ◽  
Contrast Enhanced

A novel anticancer drug delivery system with contrast-enhanced ultrasound-imaging performance was synthesized by a typical hard-templating method using monodispersed silica nanoparticles as the templates, which was based on unique molecularly organic/inorganic hybrid hollow periodic mesoporous organosilicas (HPMOs). The highly dispersed HPMOs show the uniform spherical morphology, large hollow interior, and well-defined mesoporous structures, which are very beneficial for ultrasound-based theranostics. The obtained HPMOs exhibit excellent performances in contrast-enhanced ultrasonography bothin vitroandin vivoand can be used for the real-time determination of the progress of lesion tissues during the chemotherapeutic process. Importantly, hydrophobic paclitaxel- (PTX-) loaded HPMOs combined with ultrasound irradiation show fast ultrasound responsiveness for controlled drug release and higherin vitroandin vivotumor inhibition rates compared with free PTX and PTX-loaded HPMOs, which is due to the enhanced ultrasound-triggered drug release and ultrasound-induced cavitation effect. Therefore, the achieved novel HPMOs-based nanoparticle systems will find broad application potentials in clinically ultrasound-based imaging and auxiliary tumor chemotherapy.

Chemie polyfunktioneller Liganden, 64 [1]. Über Hydridoiridium(III)-Komplexe des N.N-Bis(diphenylphosphino)-p-tolylamiii Chemistry of Polyfunctional Ligands, 64 [1]. On Hydridoiridium(III) Complexes of N,N-Bis(diphenylphosphino)-p-tolylamine

1981 ◽  
Vol 36 (5) ◽  
pp. 571-577 ◽  
Author(s):  
Jochen Ellermann ◽  
Leo Mader ◽  
Kurt Geibel
Keyword(s):  
Nmr Spectra ◽  
Oxidative Addition ◽  
H Nmr ◽  
New Compounds

H2 reacts with [Ir{(Ph2P)2N-p-C6H4CH3}2]Cl · 3 C6H6 (1) to give cis-[Ir(H)2{(Ph2P)2N-p-C6H4CH3}2]Cl · CH2Cl2 (2a). By reaction of 2a with NaBPh4 cis-[Ir(H)2{(Ph2P)2N-p-C6H4CH3}2]BPh4 (2 b) is obtained. Refluxing of 2a in CH2Cl2 yields trans-[lr(H)2{(Ph2P)2N-p-C6H4CH3}2]Cl · 1/2 CH2Cl2 (3a), which undegoes metatheses with NaBPh4 to trans-[Ir(H)2{(Ph2P)2N-p-C6H4CH3}2]BPh4 (3b). 3a is also formed by refluxing of 1 in methanol in the presence of oxygen. Oxidative addition of HCl to 1 and reaction with NaBPh4 yields trans-[Ir(H)(Cl){(Ph2P)2N-p-C6H4CH3}2]BPh4 (4b). The new compounds are characterised by their IR, Raman, 31P{1H} PFT and 1H NMR Spectra

Magnetic resonance imaging (1H) and spectroscopy (1H, 31P) of growing chicken embryos

1993 ◽  
Vol 73 (4) ◽  
pp. 953-965 ◽  
Author(s):  
A. Lirette ◽  
Z. Liu ◽  
D. C. Crober ◽  
R. A. Towner ◽  
U. M. Oehler ◽  
...  
Keyword(s):  
Nmr Spectroscopy ◽  
Magnetic Resonance ◽  
Nmr Spectra ◽  
Surface Coil ◽  
Nmr Imaging ◽  
Chicken Embryos ◽  
H Nmr ◽  
Imaging And Spectroscopy ◽  
Two Peaks

Nuclear magnetic resonance (NMR) imaging and spectroscopy techniques were used to observe in vivo anatomical and metabolite changes, respectively, in developing chicken embryos. Proton (1H) NMR images of the eggs revealed major changes in yolk shape from day 2 to day 6. Embryos were visible from day 6 to hatching, and good embryonic anatomical images were obtained. Two peaks were observed from 1H-NMR spectroscopy of fertilized eggs: one for lipid methylene protons, and one for water protons. Water peak to lipid peak ratios did not vary significantly (P > 0.05) from day 2 to day 21 of incubation. Localized 31P-NMR spectra of developing embryos were obtained with either a 31P surface coil or a double-tuned 31P/1H volume coil. The surface-coil method gave a greater signal to noise ratio by a factor of four. The 31P-NMR spectra indicated two peaks at day 2; these were attributed to phosphomonoesters and phosphodiesters. The three peaks characteristic of ATP appeared on day 11 and increased in size until hatching. From day 19, phosphocreatine was detectable. There appeared to be a good correlation between 31P-metabolite changes detected by in vivo 31P-NMR spectroscopy and literature values for biochemical analyses of developing chicken embryos. The advantage in using NMR imaging and spectroscopy techniques is that anatomical and metabolic changes can be obtained in vivo, non-invasively and repeatedly as an embryo develops. Key words: NMR, MRI, embryo, poultry

scholarly journals Yb3+-containing chitosan hydrogels induce B-16 melanoma cell anoikis via a Fak-dependent pathway

2019 ◽  
Vol 8 (1) ◽  
pp. 645-660 ◽  
Author(s):  
Yu Miao ◽  
Jiawei Lu ◽  
Junhui Yin ◽  
Changchun Zhou ◽  
Yaping Guo ◽  
...  
Keyword(s):  
Acetic Acid Solution ◽  
Tumor Model ◽  
In Vivo Studies ◽  
High Recurrence Rate ◽  
Mixed Solution ◽  
Chitosan Hydrogel ◽  
Chitosan Hydrogels ◽  
Dermal Cells

AbstractMelanoma is the most lethal dermal tumor, and a high recurrence rate and skin defects are two main serious problems. An antimelanoma material,which effectively inhibits tumor recurrence and possesses excellent biocompatibility, is urgently needed to treat melanoma. In this study, we developed a novel antitumor Yb3+ [Yb(NO3)3]containing chitosan hydrogel (Yb-CS hydrogel) by dissolving Yb(NO3)3 and chitosan in acetic acid solution and forming composite hydrogels by a freeze-drying process after adding NaOH to the mixed solution. In vitro studies demonstrated that the Yb3+ produces effect of inducing cell death in Yb-CS hydrogel. Moreover, we found that the Yb-CS hydrogel inhibited a focal adhesion kinase (FAK)-dependent signaling pathway and induced B-16 cell anoikis. However, the Yb-CS hydrogel was less effective on L929 normal mouse dermal cells. In vivo studies showed that the Yb-CS hydrogel inhibited the recurrence of melanoma in a mouse bare xenograft tumor model. We concluded that the Yb-CS hydrogel could potentially be used in the antimelanoma field, especially in the inhibition of melanoma recurrence.

scholarly journals Molecular Docking, Computational, and Antithrombotic Studies of Novel 1,3,4-Oxadiazole Derivatives

2018 ◽  
Vol 19 (11) ◽  
pp. 3606 ◽  
Author(s):  
Majda Batool ◽  
Affifa Tajammal ◽  
Firdous Farhat ◽  
Francis Verpoort ◽  
Zafar Khattak ◽  
...  
Keyword(s):  
Factor Xa ◽  
Clot Lysis ◽  
Clotting Time ◽  
Reference Drug ◽  
Docking Score ◽  
High Affinity ◽  
Oxadiazole Derivatives ◽  
Inhibitory Potential

A new series of 1,3,4-oxadiazoles derivatives was synthesized, characterized, and evaluated for their in vitro and in vivo anti-thrombotic activity. Compounds (3a–3i) exhibited significant clot lysis with respect to reference drug streptokinase (30,000 IU), and enhanced clotting time (CT) values (130–342 s) than heparin (110 s). High affinity towards 1NFY with greater docking score was observed for the compounds (3a, 3i, 3e, 3d, and 3h) than the control ligand RPR200095. In addition, impressive inhibitory potential against factor Xa (F-Xa) was observed with higher docking scores (5612–6270) with Atomic Contact Energy (ACE) values (−189.68 to −352.28 kcal/mol) than the control ligand RPR200095 (Docking score 5192; ACE −197.81 kcal/mol). In vitro, in vivo, and in silico results proposed that these newly synthesized compounds might be used as anticoagulant agents.

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