scholarly journals Synthetic approaches to 2-aryl/hetaryl- and 2-(hetaryl)ylidene derivatives of fluorinated 1,3-benzothiazin-4-ones

2020 ◽  
Vol 7 (3) ◽  
pp. 96-103
Author(s):  
Emiliya V. Nosova ◽  
Olga A. Batanova ◽  
Nataliya N. Mochulskaya ◽  
Galina N. Lipunova
Keyword(s):  
New Approach ◽  
Synthetic Approaches ◽  
Further Development ◽  
Derivatives Of ◽  
Tuberculostatic Agents

A series of 2-hetaryl- and 2-(hetaryl)ylidene substituted 5-fluoro-8-nitro-1,3-benzothiazin-4-ones was synthesized by interaction of 2,6-difluoro-3-nitrobenzoylisothiocyanate with C-nucleophiles. Cyclocondensation of polyfluorobenzoylchlorides with aryl and hetaryl thioamides represents new approach to 1,3-benzothiazin-4-ones. Some compounds proved to be promising for further development of tuberculostatic agents.

Synthesis and Biological Potentials of Quinoline Analogues: A Review of Literature

2019 ◽  
Vol 16 (7) ◽  
pp. 653-688 ◽  
Author(s):  
Leena Kumari ◽  
Salahuddin ◽  
Avijit Mazumder ◽  
Daman Pandey ◽  
Mohammad Shahar Yar ◽  
...  
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Building Blocks ◽  
Vital Role ◽  
Review Of Literature ◽  
Drug Discovery Process ◽  
Active Compounds ◽  
Lead Compounds ◽  
Synthetic Approaches ◽  
Derivatives Of

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.

scholarly journals Biguanide-Based Synthesis of 1,3,5-Triazine Derivatives with Anticancer Activity and 1,3,5-Triazine Incorporated Calcium Citrate Nanoparticles

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1028
Author(s):  
Monnaya Chalermnon ◽  
Sarocha Cherdchom ◽  
Amornpun Sereemaspun ◽  
Rojrit Rojanathanes ◽  
Tanatorn Khotavivattana
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Anticancer Agent ◽  
Drug Loading ◽  
Calcium Citrate ◽  
Colorectal Cancer Cell Lines ◽  
Triazine Derivatives ◽  
Further Development ◽  
Derivatives Of ◽  
Potential Use

Twelve derivatives of biguanide-derived 1,3,5-triazines, a promising class of anticancer agent, were synthesised and evaluated for their anticancer activity against two colorectal cancer cell lines—HCT116 and SW620. 2c and 3c which are the derivatives containing o-hydroxyphenyl substituents exhibited the highest activity with IC50 against both cell lines in the range of 20–27 µM, which is comparable to the IC50 of cisplatin reference. Moreover, the potential use of the calcium citrate nanoparticles (CaCit NPs) as a platform for drug delivery system was studied on a selected 1,3,5-triazine derivative 2a. Condition optimisation revealed that the source of citrate ions and reaction time significantly influence the morphology, size and %drug loading of the particles. With the optimised conditions, “CaCit-2a NPs” were successfully synthesised with the size of 148 ± 23 nm and %drug loading of up to 16.3%. Furthermore, it was found that the release of 2a from the synthesised CaCit-2a NPs is pH-responsive, and 2a could be control released under the acidic cancer environment. The knowledge from this study is perceptive for further development of the 1,3,5-triazine-based anticancer drugs and provide the platform for the incorporation of other drugs in the CaCit NPs in the future.

scholarly journals New approach in the application of lignin for the synthesis of hybrid materials

2017 ◽  
Vol 89 (1) ◽  
pp. 161-171 ◽  
Author(s):  
Beata Podkościelna ◽  
Marta Goliszek ◽  
Olena Sevastyanova
Keyword(s):  
Suspension Polymerization ◽  
Nitrogen Adsorption ◽  
Experimental Protocol ◽  
New Approach ◽  
Surface Areas ◽  
Adsorption Data ◽  
Novel Method ◽  
Derivatives Of ◽  
Polymerization Method ◽  
Nitrogen Adsorption Data

AbstractIn this study, a novel method for the synthesis of hybrid, porous microspheres, including divinylbenzene (DVB), triethoxyvinylsilane (TEVS) and methacrylated lignin (L-Met), is presented. The methacrylic derivatives of kraft lignin were obtained by reaction with methacryloyl chloride according to a new experimental protocol. The course of the modification of lignin was confirmed by attenuated total reflectance (ATR-FTIR) and nuclear magnetic resonance (NMR) spectroscopy. The emulsion-suspension polymerization method was employed to obtain copolymers of DVD, TEVS and L-Met in spherical forms. The porous structures and morphologies of the obtained lignin-containing functionalized microspheres were investigated by low-temperature nitrogen adsorption data and scanning electron microscopy (SEM). The microspheres are demonstrated to be mesoporous materials with specific surface areas in the range of 430–520 m2/g. The effects of the lignin component on the porous structure, shape, swelling and thermal properties of the microspheres were evaluated.

Coupling of Steroid O-(Carboxymethyl)oxime Derivatives with Amino Alcohols

1996 ◽  
Vol 61 (2) ◽  
pp. 288-297 ◽  
Author(s):  
Vladimír Pouzar ◽  
Ivan Černý
Keyword(s):  
Amino Acids ◽  
Hydroxy Group ◽  
Building Blocks ◽  
Amino Alcohols ◽  
New Approach ◽  
Alternative Synthesis ◽  
Oxime Derivatives ◽  
A Chain ◽  
Derivatives Of

New approach to the preparation of steroids with connecting bridge, based on an O-carboxymethyloxime (CMO) structure, and with terminal hydroxy group, is presented. 17-CMO derivatives of 3β-acetoxy- and 3β-methoxymethoxyandrost-5-en-17-one were condensed with α,ω-amino alcohols to give derivatives with a chain of seven to nine atoms. After THP-protection, these compounds were converted to 3-keto-4-ene derivatives. An alternative synthesis consisted in transformation of 17-CMO derivatives with bonded amino acids by reduction of the terminal carboxyl. The resulting compounds were designed as building blocks for the preparation of bis-haptens for sandwich immunoassays.

scholarly journals Live experience philosophy. The theory of knowledge of A.A. Bogdanov

Polylogos ◽  
2021 ◽  
Vol 5 (№ 4 (18)) ◽  
pp. 0
Author(s):  
Mikhail Loktionov
Keyword(s):  
Theory Of Knowledge ◽  
Russian Philosophy ◽  
Human Knowledge ◽  
Philosophical Work ◽  
New Approach ◽  
Xxth Century ◽  
The Public ◽  
Scientific Philosophy ◽  
Organizational Science ◽  
Further Development

Considering the philosophical heritage of Alexander Bogdanov, the author focuses on the aspect of the theory of knowledge, which passes through all the work of the famous philosopher and revolutionary. Doubts about the possibility of an exhaustive knowledge of the surrounding reality are also visible in Bogdanov’s earliest works. An attempt to build a new approach to human knowledge, having rinked him with activity experience, was undertaken by him in his main philosophical work, “Empiriomonism”. Standing on the positions of positivism as a “scientific” philosophy, Bogdanov tried to substantiate the dynamics of the public process, while remaining at the Marxist platform. The further development of his ideas led to the creation of a “universal organizational science” – tectology, which, in his opinion, has already passed beyond philosophy and was not only science, but also methodology of knowledge, as well as the style of scientific thinking, to which science, initially not realizing this, always sought. Thus, studying the legacy of Bogdanov, we see the development of views on the ideas of knowledge in the Russian philosophy of the beginning of the XXth century.

A New Approach to the Synthesis of Functional Derivatives of 3-(4-Pyridinyl)-1H-indole and 4-(1H-Indol-3-yl)thieno[2,3-b]pyridine

2018 ◽  
Vol 88 (4) ◽  
pp. 682-688 ◽  
Author(s):  
V. V. Dotsenko ◽  
S. G. Krivokolysko ◽  
B. S. Krivokolysko ◽  
K. A. Frolov
Keyword(s):  
New Approach ◽  
Functional Derivatives ◽  
Derivatives Of

Azaheterocyclic Derivatives of ortho-Carborane: Synthetic Strategies and Application Opportunities

Synthesis ◽  
2019 ◽  
Vol 52 (03) ◽  
pp. 337-352 ◽  
Author(s):  
Lidiia A. Smyshliaeva ◽  
Mikhail V. Varaksin ◽  
Valery N. Charushin ◽  
Oleg N. Chupakhin
Keyword(s):  
Materials Science ◽  
Cross Coupling ◽  
General Character ◽  
Advanced Technologies ◽  
Substituted Acetylenes ◽  
Synthetic Approaches ◽  
Derivatives Of ◽  
Coupling Strategies

Azaheterocyclic derivatives of 1,2-dicarba-closo-dodeca­borane (ortho-carborane) are known to be of particular interest due to numerous plausible applications, particularly, in medicine, materials science, and advanced technologies. Three principal synthetic strategies resulting in azaheterocyclic carboranes, in which boron-enriched and azaheterocyclic fragments are linked to each other, either directly by means of the C–C bonds or through a short spacer (CH2, CH2S, CH2O, etc.), have been outlined. These synthetic approaches are of general character and can be used both individually and in combination to afford promising organoboron clusters of diverse architectures.1 Introduction2 C–C Cross-Coupling Strategies in the Synthesis of Azahetero­cyclic Carboranes3 Carboryne-Based Transformation Strategies4 Condensation Strategies: Reactions of Decaborane B10H14 with Substituted Acetylenes5 Conclusion and Outlook

Rapid computation of rotary derivatives for subsonic and low transonic flows

2019 ◽  
Vol 36 (9) ◽  
pp. 3108-3121
Author(s):  
Jian-Ming Fu ◽  
Hai-Min Tang ◽  
Hong-Quan Chen
Keyword(s):  
Mach Number ◽  
Normal Velocity ◽  
New Approach ◽  
Content Type ◽  
Strip Theory ◽  
Model Aircraft ◽  
Computational Fluid Dynamics Cfd ◽  
Steady Solutions ◽  
State Pressure ◽  
Derivatives Of

Purpose The purpose of this paper is to develop a new approach for rapid computation of subsonic and low-transonic rotary derivatives with the available steady solutions obtained by Euler computational fluid dynamics (CFD) codes. Design/methodology/approach The approach is achieved by the perturbation on the steady-state pressure of Euler CFD codes. The resulting perturbation relation is established at a reference Mach number between rotary derivatives and normal velocity on surface due to angular velocity. The solution of the reference Mach number is generated technically by Prandtl–Glauert compressibility correction based on any Mach number of interest under the assumption of simple strip theory. Rotary derivatives of any Mach number of interest are then inversely predicted by the Prandtl–Glauert rule based on the reference Mach number aforementioned. Findings The resulting method has been verified for three typical different cases of the Basic Finner Reference Projectile, the Standard Dynamics Model Aircraft and the Orion Crew Module. In comparison with the original perturbation method, the performance at subsonic and low-transonic Mach numbers has significantly improved with satisfactory accuracy for most design efforts. Originality/value The approach presented is verified to be an efficient way for computation of subsonic and low-transonic rotary derivatives, which are performed almost at the same time as an accounting solution of steady Euler equations.

scholarly journals Nonclassical Biological Activities of Quinolone Derivatives

2011 ◽  
Vol 15 (1) ◽  
pp. 52 ◽  
Author(s):  
Mohsen Daneshtalab ◽  
Abeer Ahmed
Keyword(s):  
Mammalian Cells ◽  
Antibacterial Agents ◽  
Biological Activities ◽  
Antiviral Agent ◽  
Bioactive Molecules ◽  
Structural Modifications ◽  
Further Development ◽  
Derivatives Of ◽  
Ns5b Polymerase

Quinolones are considered as a big family of multi-faceted drugs; their chemical synthesis is flexible and can be easily adapted to prepare new congeners with rationally devised structures. This is shown by the description of many thousands of derivatives in the literature. Scientists could accurately describe their QSAR, which is essential for effective drug design. This also gave them the chance to discover new and unprecedented activities, which makes quinolones an endless source of hope and enables further development of new clinically useful drugs. Quinolones are among the most common frameworks present in the bioactive molecules that have dominated the market for more than four decades. Since 1962, 4(1H)-quinolone-3-carboxylic acid derivatives are widely used as antibacterial agents. Quinolones have a broad and potent spectrum of activity and are also used as second-line drugs to treat tuberculosis (TB). Recently, quinolones have been reported to display “nonclassical” biological activities, such as antitumor, anti-HIV-1 integrase, anti- HCV-NS3 helicase and -NS5B-polymerase activities. The present review focuses on the structural modifications responsible for the transformation of an antibacterial into an anticancer agent and/or an antiviral agent. Indeed, quinolones’ antimicrobial action is distinguishable among antibacterial agents, because they target different type II topoisomerase enzymes. Many derivatives of this family show high activity against bacterial topoisomerases and eukaryotic topoisomerases, and are also toxic to cultured mammalian cells and in vivo tumor models. Moreover, quinolones have shown antiviral activity against HIV and HCV viruses. In this context the quinolones family of drugs seem to link three different biological activities (antibacterial, anticancer, and the antiviral profiles) and the review will also provide an insight into the different mechanisms responsible for these activities among different species. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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