scholarly journals Synthesis of 3-alkenylindoles through regioselective C–H alkenylation of indoles by a ruthenium nanocatalyst

2020 ◽  
Vol 16 ◽  
pp. 140-148 ◽  
Author(s):  
Abhijit Paul ◽  
Debnath Chatterjee ◽  
Srirupa Banerjee ◽  
Somnath Yadav
Keyword(s):  
Functional Groups ◽  
Medicinal Chemistry ◽  
Catalytic Efficiency ◽  
Three Phase ◽  
Electron Donating Groups

3-Alkenylindoles are biologically and medicinally very important compounds, and their syntheses have received considerable attention. Herein, we report the synthesis of 3-alkenylindoles via a regioselective alkenylation of indoles, catalysed by a ruthenium nanocatalyst (RuNC). The reaction tolerates several electron-withdrawing and electron-donating groups on the indole moiety. Additionally, a “robustness screen” has also been employed to demonstrate the tolerance of several functional groups relevant to medicinal chemistry. With respect to the Ru nanocatalyst, it has been demonstrated that it is recoverable and recyclable up to four cycles. Also, the catalyst acts through a heterogeneous mechanism, which has been proven by various techniques, such as ICPMS and three-phase tests. The nature of the Ru nanocatalyst surface has also been thoroughly examined by various techniques, and it has been found that the oxides on the surface are responsible for the high catalytic efficiency of the Ru nanocatalyst.

scholarly journals Late stage C–H functionalization via chalcogen and pnictogen salts

2020 ◽  
Vol 11 (37) ◽  
pp. 10047-10060
Author(s):  
Christopher B. Kelly ◽  
Rosaura Padilla-Salinas
Keyword(s):  
Functional Groups ◽  
Late Stage ◽  
Potential Application ◽  
Medicinal Chemistry

Three unrelated cationic groups, which can replace C–H bonds late stage, have been identified as progenitors to various functional groups. This review discusses the chemistry of these salts and their potential application in medicinal chemistry.

Double graphitic-N doping for enhanced catalytic oxidation activity of carbocatalysts

2019 ◽  
Vol 21 (10) ◽  
pp. 5481-5488 ◽  
Author(s):  
Meiling Hou ◽  
Xin Zhang ◽  
Shandong Yuan ◽  
Wanglai Cen
Keyword(s):  
Work Function ◽  
Catalytic Oxidation ◽  
Functional Groups ◽  
Reactive Oxygen ◽  
Catalytic Efficiency ◽  
Oxidation Activity ◽  
Promotion Effect ◽  
Oxygen Functional Groups ◽  
N Doping

Double-GrN remarkably enhanced the catalytic efficiency for O2 dissociation reactions and accelerates the generation of highly chemically reactive oxygen functional groups. The promotion effect is ascribed to the reduction of the work function of carbocatalysts due to N doping, which facilitates the transfer of electrons from carbocatalysts to the adsorbed O2 molecules for their activation.

scholarly journals Recent Advances in Indazole-Containing Derivatives: Synthesis and Biological Perspectives

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2783 ◽  
Author(s):  
Shu-Guang Zhang ◽  
Chao-Gen Liang ◽  
Wei-Hua Zhang
Keyword(s):  
Functional Groups ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Drug Molecules ◽  
Recent Advances

Indazole-containing derivatives represent one of the most important heterocycles in drug molecules. Diversely substituted indazole derivatives bear a variety of functional groups and display versatile biological activities; hence, they have gained considerable attention in the field of medicinal chemistry. This review aims to summarize the recent advances in various methods for the synthesis of indazole derivatives. The current developments in the biological activities of indazole-based compounds are also presented.

scholarly journals Pharmacological and Medicinal Chemistry Aspects of Cannabis Compounds

2011 ◽  
Vol 6 (2) ◽  
pp. 16-18
Author(s):  
T. Cotelea
Keyword(s):  
Chemical Analysis ◽  
Functional Groups ◽  
Medicinal Chemistry ◽  
Spatial Arrangement ◽  
Pharmacological Action ◽  
Scientific Interest ◽  
General Overview

The current communication includes a general overview of the scientific interest and medicianl chemistry aspects of Cannabis compounds. It relates to metabolism, pharmacological action and phisico-chemical analysis of these compounds, as well as of some isomers differing in spatial arrangement of functional groups.

Visible-light-driven photocatalytic CO2 reduction over ketoenamine-based covalent organic frameworks: role of the host functional groups

2021 ◽  
Author(s):  
Lianlian Peng ◽  
Shuqing Chang ◽  
Ziling Liu ◽  
Yanghe Fu ◽  
Rui Ma ◽  
...  
Keyword(s):  
Visible Light ◽  
Functional Groups ◽  
Charge Separation ◽  
Photocatalytic Performance ◽  
Co2 Reduction ◽  
Covalent Organic Frameworks ◽  
Visible Light Driven ◽  
Photogenerated Charge Separation ◽  
Electron Donating Groups

Compared to the electron-withdrawing groups, the electron-donating groups in TpBD can accelerate the photogenerated charge separation and transfer, thereby improving the photocatalytic performance for photocatalytic CO2 reduction.

Anticancer Activity-Structure Relationship of Quinolinone-Based Compounds: An Overview

2021 ◽  
Vol 21 ◽  
Author(s):  
Hüseyin K. Beker ◽  
Işıl Yıldırım
Keyword(s):  
Functional Groups ◽  
Anticancer Agents ◽  
Drug Candidates ◽  
Activity Structure ◽  
Gene And Protein Expression ◽  
Structure Relationship ◽  
New Vision ◽  
Relationship Of ◽  
Novel Drug ◽  
Electron Donating Groups

Background: Heterocyclic compounds play an important role in the pharmaceutical and biological processes. Among all heterocycles, quinolinone/quinoline has one of the most unique structures in the discovery of these compounds. These derivatives have been prepared by various on the structures, positions, and they have attracted a great deal of attention in the field of medicinal chemistry. The great interest to medicinal chemists is the basic scaffold of the fused quinolines derivative. The large road maps of gene and protein expression produced by these methods often can be used to classify cancers or predict responses to certain types of treatments targeting regulated at both the level of transcription and translation and at the level of enzyme activity. These specific regulations may open the door for the discovery of novel drug candidates including an anti-cancer target. Objective: This review will attempt to provide a comprehensive description of different quinolinone derivatives especially by concentrating on compounds containing benzimidazole ring. Quinolones moieties are experimentally proven anticancer pharmacophores. We think these pharmacophore and additional substitutions on these scaffolds would further enhance their activity as anticancer agents. This activity associate with the positioning of these different functional groups, such as fluoro, methoxy, methyl, amino, hydroxy, nitro, bromo, chloro, methylamino, ethoxy, carbonyl, iodo, and trifluoromethyl groups. Among the functional groups, most of the electronwithdrawing groups such as fluoro, chloro, nitro, amino, and carbonyl groups showed stronger activity than those with electron-donating groups such as methyl and methoxy groups. Presence of electron-withdrawing or electron-donating group by varying the quinolinone redox properties affect its capacity of DNA synthesis. Conclusion: The structural motifs attributed to noteworthy inhibitory results have been identified and highlighted in order to encourage further research and develop more efficient. This work to aim to present knowledge and it hoped that this review can be help researchers to explore an interesting quinoline class, and researchers will be able to develop a new vision in the search for rational designs of more powerful, active and less toxic quinoline-based anticancer drugs.

scholarly journals The Effects on Lipophilicity of Replacing Oxygenated Functionality with Their Fluorinated Bioisosteres

2021 ◽  
Author(s):  
Richard J. Glyn ◽  
Graham Pattison
Keyword(s):  
Physicochemical Properties ◽  
Aromatic Ring ◽  
Fluorine Atom ◽  
Medicinal Chemistry ◽  
Matched Pair ◽  
Matched Pair Analysis ◽  
Bioisosteric Replacement ◽  
The Difference ◽  
Electron Donating Groups ◽  
Pair Analysis

The replacement of oxygenated functionality (hydroxy, alkoxy) with a fluorine atom is a very commonly used bioisosteric replacement in medicinal chemistry. In this paper we use a Molecular Matched Pair Analysis approach to better understand the effects of this bioisosteric replacement on the physicochemical properties of compounds, particularly in terms of lipophilicity. We observe that the presence of electron-donating groups on an aromatic ring generally increase the difference in lipophilicity between an oxygenated compound and its fluorinated analogue.

scholarly journals Transformation of 2H-1,2,3-benzothiadiazine 1,1-dioxides variously substituted at the aromatic ring, via nucleophilic substitution and demethylation reactions

2020 ◽  
Author(s):  
Imre Gyűjtő ◽  
Márta Porcs-Makkay ◽  
Ernák Ferenc Várda ◽  
Gyöngyvér Pusztai ◽  
Gábor Tóth ◽  
...  
Keyword(s):  
Nucleophilic Substitution ◽  
Functional Groups ◽  
Aromatic Ring ◽  
Methoxy Group ◽  
Medicinal Chemistry ◽  
Building Blocks ◽  
Chlorine Atoms ◽  
New Methods ◽  
Pharmacological Interest

2H‑1,2,3‑Benzothiadiazine 1,1-dioxides are a class of compounds of pharmacological interest. After earlier studies carried out at our laboratory on various transformations (alkylation, acylation, reduction) at the hetero ring, the present manuscript focuses on the transformation of substituents at the aromatic carbocycle, including nucleophilic substitution of chlorine atoms and demethylation of the methoxy group with amines. The new methods described here allow the introduction of versatile functional groups on the aromatic ring, making these compounds useful building blocks for organic and medicinal chemistry applications.

REVIEW ON THE SYNTHESIS AND POTENTIAL THERAPEUTIC APPLICATIONS OF HETEROCYCLIC PRODUCTS OF 5-AMINO-3-METHYLISOXAZOLE

2021 ◽  
Vol 12 (08) ◽  
pp. 154-172
Author(s):  
Tahira Saleem ◽  
Muhammad Humble Khalid Tareen ◽  
Muhammad Rashid ◽  
Mehwish Nawaz ◽  
Hina Aftab ◽  
...  
Keyword(s):  
Functional Groups ◽  
Building Block ◽  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Drug Molecule ◽  
Therapeutic Applications ◽  
Biological Actions

In general, heterocyclic compounds have evoked interest and concern because of their fundamental role in biological profiles and biological actions in nature. Now, most of the lead molecules in medicinal chemistry are based on hetero-atoms. In medicinal chemistry- to bring two hetero-atoms to the drug molecule, isoxazoles are interesting functional groups. Isoxazole as a key building block has been widely used and is an important heterocyclic unit.

Structures and energetic properties of 4-halobenzamides

2018 ◽  
Vol 74 (11) ◽  
pp. 1395-1402
Author(s):  
Aleksandra Piontek ◽  
Elwira Bisz ◽  
Błażej Dziuk ◽  
Roman Szostak ◽  
Michal Szostak
Keyword(s):  
Crystal Structures ◽  
Functional Groups ◽  
Organic Synthesis ◽  
Molecular Interactions ◽  
Medicinal Chemistry ◽  
Twist Angle ◽  
Amide Bond ◽  
Energetic Properties ◽  
Resonance Energies ◽  
Substituted Benzamides

The amide bond represents one of the most fundamental functional groups in chemistry. The properties of amides are defined by amidic resonance (nN→π*C=O conjugation), which enforces planarity of the six atoms comprising the amide bond. Despite the importance of 4-halo-substituted benzamides in organic synthesis, molecular interactions and medicinal chemistry, the effect of 4-halo-substitution on the properties of the amide bond in N,N-disubstituted benzamides has not been studied. Herein, we report the crystal structures and energetic properties of a full series of 4-halobenzamides. The structures of four 4-halobenzamides (halo = iodo, bromo, chloro and fluoro) in the N-morpholinyl series have been determined, namely 4-[(4-halophenyl)carbonyl]morpholine, C11H12 XNO2, for halo = iodo (X = I), bromo (X = Br), chloro (X = Cl) and fluoro (X = F). Computations have been used to determine the effect of halogen substitution on the structures and resonance energies. 4-Iodo-N-morpholinylbenzamide crystallized with a significant distortion of the amide bond (τ + χN = 33°). The present study supports the correlation between the Ar—C(O) axis twist angle and the twist angle of the amide N—C(O) bond. Comparison of resonance energies in synthetically valuable N-morpholinyl and N-piperidinyl amides demonstrates that the O atom of the morpholinyl ring has a negligible effect on amidic resonance in the series.

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