Miscellaneous biological activity profile of imidazole-based compounds: An aspirational goal for medicinal chemistry

2022 ◽  
pp. 291-322
Author(s):  
Nusrat Sahiba ◽  
Pankaj Teli ◽  
Dinesh K. Agarwal ◽  
Shikha Agarwal
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Activity Profile

A Revised Modular Approach to D8-THC and Derivatives Through Late-Stage Suzuki-Miyaura Cross-Coupling Reactions

2019 ◽  
Author(s):  
Victor Bloemendal ◽  
Floris P. J. T. Rutjes ◽  
Thomas J. Boltje ◽  
Daan Sondag ◽  
Hidde Elferink ◽  
...  
Keyword(s):  
Biological Activity ◽  
Late Stage ◽  
Medicinal Chemistry ◽  
Cross Coupling ◽  
Modular Approach ◽  
Coupling Reactions ◽  
One Pot ◽  
Biologically Relevant ◽  
Cross Coupling Reactions ◽  
Chemistry Research

<p>In this manuscript we describe a modular pathway to synthesize biologically relevant (–)-<i>trans</i>-Δ<sup>8</sup>-THC derivatives, which can be used to modulate the pharmacologically important CB<sub>1</sub> and CB<sub>2</sub> receptors. This pathway involves a one-pot Friedel-Crafts alkylation/cyclization protocol, followed by Suzuki-Miyaura cross-coupling reactions and gives rise to a series of new Δ<sup>8</sup>-THC derivatives. In addition, we demonstrate using extensive NMR evidence that similar halide-substituted Friedel-Crafts alkylation/cyclization products in previous articles were wrongly assigned as the para-isomers, which also has consequence for the assignment of the subsequent cross-coupled products and interpretation of their biological activity. </p> <p>Considering the importance of the availability of THC derivatives in medicinal chemistry research and the fact that previously synthesized compounds were wrongly assigned, we feel this research is describing a straightforward pathway into new cannabinoids.</p>

Synthesis and Biological Activity of Hydrazones and Derivatives: A Review

2020 ◽  
Vol 20 (5) ◽  
pp. 342-368 ◽  
Author(s):  
Juliana de Oliveira Carneiro Brum ◽  
Tanos Celmar Costa França ◽  
Steven R. LaPlante ◽  
José Daniel Figueroa Villar
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
New Drugs ◽  
New Drug ◽  
Cancer Inflammation

Hydrazones and their derivatives are very important compounds in medicinal chemistry due to their reported biological activity for the treatment of several diseases, like Alzheimer’s, cancer, inflammation, and leishmaniasis. However, most of the investigations on hydrazones available in literature today are directed to the synthesis of these molecules with little discussion available on their biological activities. With the purpose of bringing lights into this issue, we performed a revision of the literature and wrote this review based on some of the most current research reports of hydrazones and derivatives, making it clear that the synthesis of these molecules can lead to new drug prototypes. Our goal is to encourage more studies focused on the synthesis and evaluation of new hydrazones, as a contribution to the development of potential new drugs for the treatment of various diseases.

scholarly journals Enantioselective Catalytic C-H Amidations: An Highlight

Catalysts ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 471
Author(s):  
Eleonora Tosi ◽  
Renata Marcia de Figueiredo ◽  
Jean-Marc Campagne
Keyword(s):  
Biological Activity ◽  
Chemical Synthesis ◽  
Crucial Role ◽  
Medicinal Chemistry ◽  
Life Sciences ◽  
Biological Processes ◽  
Chiral Molecules ◽  
Material Sciences ◽  
Innovative Approaches

The crucial role played by compounds bearing amide functions, not only in biological processes but also in several fields of chemistry, life polymers and material sciences, has brought about many significant discoveries and innovative approaches for their chemical synthesis. Indeed, a plethora of strategies has been developed to reach such moieties. Amides within chiral molecules are often associated with biological activity especially in life sciences and medicinal chemistry. In most of these cases, their synthesis requires extensive rethinking methodologies. In the very last years (2019–2020), enantioselective C-H functionalization has appeared as a straightforward alternative to reach chiral amides. Therein, an overview on these transformations within this timeframe is going to be given.

scholarly journals Recent developments of synthesis and biological activity of sultone scaffolds in medicinal chemistry

2021 ◽  
Vol 14 (4) ◽  
pp. 103037
Author(s):  
Yingying Xu ◽  
Ziwen Zhang ◽  
Jingbo Shi ◽  
Xinhua Liu ◽  
Wenjian Tang
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Recent Developments

scholarly journals Microwave Assisted Reactions of Azaheterocycles Formedicinal Chemistry Applications

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 716 ◽  
Author(s):  
Dorina Amariucai-Mantu ◽  
Violeta Mangalagiu ◽  
Ramona Danac ◽  
Ionel I. Mangalagiu
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Membered Ring ◽  
Reaction Pathways ◽  
Microwave Assisted ◽  
Main Series ◽  
Privileged Scaffolds

Microwave (MW) assisted reactions have became a powerful tool in azaheterocycles chemistry during the last decades. Five and six membered ring azaheterocycles are privileged scaffolds in modern medicinal chemistry possessing a large variety of biological activity. This review is focused on the recent relevant advances in the MW assisted reactions applied to azaheterocyclic derivatives and their medicinal chemistry applications from the last five years. The review is divided according to the main series of azaheterocycles, more precisely 5- and 6-membered ring azaheterocycles (with one, two, and more heteroatoms) and their fused analogues. In each case, the reaction pathways, the advantages of using MW, and considerations concerning biological activity of the obtained products were briefly presented.

Simple Coumarins and Analogues in Medicinal Chemistry: Occurrence, Synthesis and Biological Activity

2005 ◽  
Vol 12 (8) ◽  
pp. 887-916 ◽  
Author(s):  
F. Borges ◽  
F. Roleira ◽  
N. Milhazes ◽  
L. Santana ◽  
E. Uriarte
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry

scholarly journals Benzophenone: a ubiquitous scaffold in medicinal chemistry

MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1803-1817 ◽  
Author(s):  
Khemchand Surana ◽  
Bharatkumar Chaudhary ◽  
Monika Diwaker ◽  
Satyasheel Sharma
Keyword(s):  
Biological Activity ◽  
Drug Discovery ◽  
Bioactive Compounds ◽  
Medicinal Chemistry ◽  
Naturally Occurring

Diaryl ketones are an important scaffold in drug discovery due to their prevalence in naturally occurring bioactive compounds. This review discusses molecules containing the benzophenone moiety that have potent biological activity.

An Overview of Synthesis and Biological Activity of Dihydropyrimidine Derivatives

2021 ◽  
Vol 21 ◽  
Author(s):  
Anshu Chaudhary Dudhe ◽  
Rupesh Dudhe ◽  
Omji Porwal ◽  
Gayatri katole
Keyword(s):  
Natural Products ◽  
Biological Activity ◽  
Biological Effect ◽  
Medicinal Chemistry ◽  
Pharmacological Activities ◽  
Reaction Schemes

: Dihydropyrimidine derivatives are most important scaffolds due to structure similarities with natural products it is a hetrocyclic compound. The chemistry of Dihydropyrimidine is a blossoming field. Various reaction schemes for the preparation of Dihydropyrimidines and produce different biological effect and offer vast scope in the field of medicinal chemistry. This article goal to analysis the work reported the recent chemistry and pharmacological activities of dihydropyrimidine derivatives.

Peptidomimetics and Peptide-Based Blockbuster Drugs

2021 ◽  
Vol 25 ◽  
Author(s):  
Jianlin Han ◽  
Hiroyuki Konno ◽  
Tatsunori Sato ◽  
Kunisuke Izawa ◽  
Vadim A. Soloshonok
Keyword(s):  
Amino Acids ◽  
Biological Activity ◽  
Small Molecule ◽  
Medicinal Chemistry ◽  
Structural Features ◽  
Review Article ◽  
Peptide Drugs

: Amino acids (AAs) play an important role in modern health industry. AAs’ residues are frequently found in the structures of small-molecule modern pharmaceuticals, while peptidomimetics and peptide-based drugs are entirely derived from AAs. The goal of this review article is to highlight that, currently, AAs serve as key structural features in numerous successful pharmaceuticals; they are the so-called blockbuster drugs. In this work, we provide a detailed profile of 5 peptidomimetics and 4 peptide drugs. For each compound, we describe the spectrum of biological activity, medicinal chemistry discovery, and synthetic preparation.

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