heterocyclic molecules
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2022 ◽  
Vol 0 (0) ◽  
Author(s):  
Naresh Kumar ◽  
Nidhi Goel

Abstract Cancer, one of the key health problems globally, is a group of related diseases that share a number of characteristics primarily the uncontrolled growth and invasive to surrounding tissues. Chemotherapy is one of the ways for the treatment of cancer which uses one or more anticancer agents as per chemotherapy regimen. Limitations of most anticancer drugs due to a variety of reasons such as serious side effects, drug resistance, lack of sensitivity and efficacy etc. generate the necessity towards the designing of novel anticancer lead molecules. In this regard, the synthesis of biologically active heterocyclic molecules is an appealing research area. Among heterocyclic compounds, nitrogen containing heterocyclic molecules has fascinated tremendous consideration due to broad range of pharmaceutical activity. Imidazoles, extensively present in natural products as well as synthetic molecules, have two nitrogen atoms, and are five membered heterocyclic rings. Because of their countless physiological and pharmacological characteristics, medicinal chemists are enthused to design and synthesize new imidazole derivatives with improved pharmacodynamic and pharmacokinetic properties. The aim of this present chapter is to discuss the synthesis, chemistry, pharmacological activity, and scope of imidazole-based molecules in anticancer drug development. Finally, we have discussed the current challenges and future perspectives of imidazole-based derivatives in anticancer drug development.


RSC Advances ◽  
2022 ◽  
Vol 12 (1) ◽  
pp. 355-364
Author(s):  
My V. Nguyen ◽  
Thang B. Phan ◽  
Man V. Tran ◽  
Tuyet A. T. Nguyen ◽  
Hung N. Nguyen

A series of N-heterocyclic⊂VNU-23 materials have been prepared via the impregnation procedure of N-heterocyclic molecules into VNU-23.


Coatings ◽  
2021 ◽  
Vol 12 (1) ◽  
pp. 34
Author(s):  
Sara S. M. Fernandes ◽  
Maria Cidália R. Castro ◽  
Dzmitry Ivanou ◽  
Adélio Mendes ◽  
Maria Manuela M. Raposo

Three heterocyclic dyes were synthesized having in mind the changes in the photovoltaic, optical and redox properties by functionalization of 5-aryl-thieno[3,2-b]thiophene, 5-arylthiophene and bis-methylpyrrolylthiophene π-bridges with different donor, acceptor/anchoring groups. Knoevenagel condensation of the aldehyde precursors with 2-cyanoacetic acid was used to prepare the donor-acceptor functionalized heterocyclic molecules. These organic metal-free dyes are constituted by thieno[3,2-b]thiophene, arylthiophene, bis-methylpyrrolylthiophene, spacers and one or two cyanoacetic acid acceptor groups and different electron donor groups (alkoxyl, and pyrrole electron-rich heterocycle). The evaluation of the redox, optical and photovoltaic properties of these compounds indicate that 5-aryl-thieno[3,2-b]thiophene-based dye functionalized with an ethoxyl electron donor and a cyanoacetic acid electron acceptor group/anchoring moiety displays as sensitizer for DSSCs the best conversion efficiency (2.21%). It is mainly assigned to the higher molar extinction coefficient, long π-conjugation of the heterocyclic system, higher oxidation potential and strong electron donating capacity of the ethoxyl group compared to the pirrolyl moiety.


Cancers ◽  
2021 ◽  
Vol 13 (24) ◽  
pp. 6365
Author(s):  
Christian Bailly ◽  
Xavier Thuru ◽  
Bruno Quesnel

The disaccharide lactose is an excipient commonly used in pharmaceutical products. The two anomers, α- and β-lactose (α-L/β-L), differ by the orientation of the C-1 hydroxyl group on the glucose unit. In aqueous solution, a mutarotation process leads to an equilibrium of about 40% α-L and 60% β-L at room temperature. Beyond a pharmaceutical excipient in solid products, α-L has immuno-modulatory effects and functions as a major regulator of TIM-3/Gal-9 immune checkpoint, through direct binding to the β-galactoside-binding lectin galectin-9. The blockade of the co-inhibitory checkpoint TIM-3 expressed on T cells with anti-TIM-3 antibodies represents a promising approach to combat different onco-hematological diseases, in particular myelodysplastic syndromes and acute myeloid leukemia. In parallel, the discovery and development of anti-TIM-3 small molecule ligands is emerging, including peptides, RNA aptamers and a few specifically designed heterocyclic molecules. An alternative option consists of targeting the different ligands of TIM-3, notably Gal-9 recognized by α-lactose. Modulation of the TIM-3/Gal-9 checkpoint can be achieved with both α- and β-lactose. Moreover, lactose is a quasi-pan-galectin ligand, capable of modulating the functions of most of the 16 galectin molecules. The present review provides a complete analysis of the pharmaceutical and galectin-related biological functions of (α/β)-lactose. A focus is made on the capacity of lactose and Gal-9 to modulate both the TIM-3/Gal-9 and PD-1/PD-L1 immune checkpoints in oncology. Modulation of the TIM-3/Gal-9 checkpoint is a promising approach for the treatment of cancers and the role of lactose in this context is discussed. The review highlights the immuno-regulatory functions of lactose, and the benefit of the molecule well beyond its use as a pharmaceutical excipient.


Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6755
Author(s):  
Maria J. Matos ◽  
Eugenio Uriarte ◽  
Lourdes Santana

3-Phenylcoumarins are a family of heterocyclic molecules that are widely used in both organic and medicinal chemistry. In this overview, research on this scaffold, since 2010, is included and discussed, focusing on aspects related to its natural origin, synthetic procedures and pharmacological applications. This review paper is based on the most relevant literature related to the role of 3-phenylcoumarins in the design of new drug candidates. The references presented in this review have been collected from multiple electronic databases, including SciFinder, Pubmed and Mendeley.


2021 ◽  
Vol 12 ◽  
Author(s):  
Shejuti Rahman Brishty ◽  
Md. Jamal Hossain ◽  
Mayeen Uddin Khandaker ◽  
Mohammad Rashed Iqbal Faruque ◽  
Hamid Osman ◽  
...  

Nowadays, nitrogenous heterocyclic molecules have attracted a great deal of interest among medicinal chemists. Among these potential heterocyclic drugs, benzimidazole scaffolds are considerably prevalent. Due to their isostructural pharmacophore of naturally occurring active biomolecules, benzimidazole derivatives have significant importance as chemotherapeutic agents in diverse clinical conditions. Researchers have synthesized plenty of benzimidazole derivatives in the last decades, amidst a large share of these compounds exerted excellent bioactivity against many ailments with outstanding bioavailability, safety, and stability profiles. In this comprehensive review, we have summarized the bioactivity of the benzimidazole derivatives reported in recent literature (2012–2021) with their available structure-activity relationship. Compounds bearing benzimidazole nucleus possess broad-spectrum pharmacological properties ranging from common antibacterial effects to the world’s most virulent diseases. Several promising therapeutic candidates are undergoing human trials, and some of these are going to be approved for clinical use. However, notable challenges, such as drug resistance, costly and tedious synthetic methods, little structural information of receptors, lack of advanced software, and so on, are still viable to be overcome for further research.


2021 ◽  
Vol 08 ◽  
Author(s):  
Moumita Saha ◽  
Asish R. Das

: C-C or C-heteroatom bond formation from direct C-H bond activation of several heteroarenes containing suitable directing groups has now emerged as an efficient and straightforward strategy for the design of complex heterocyclic molecules as well as their late-stage functionalization. The most common problem of several C-H bond activation reactions is high temperature, long reaction time and unwanted side reactions where recent examples of MW assisted C-H bond activation showed the requirements of low temperature and short completion time and thus proved its efficacy in terms of heating effect and conversion rate of conventional heating methods. The schemes discussed in the present review depict the reaction conditions along with a look into the mechanism involved to render a deep understanding of the catalytic role of palladium-catalysis. In some examples, the optimization procedure of the corresponding strategy has been illustrated through tables, i.e., choice of catalyst, solvent screening, loading of the catalyst and percentage yield with different substrates. Each of the described illustrations has been analyzed considering a wide variety of reactants, reaction conditions, and transition metals employed as the catalyst. This review definitely allows to introduce the synthetic chemists in understanding the challenges associated with the previous methods as well as their drawbacks and future opportunities in choosing substrates, catalyst and reaction conditions. This review would be alluring to a wider range of synthetic chemists in academia and industrial R&D sectors working with heterocyclic chemistry. In this short perspective, an outline of recent eloquent examples of a variety of palladium-catalyzed C-H bond activation involving bio-oriented heterocycles achieved in the past ten years is nicely presented and the pros and cons of each strategy are highlighted so that the researchers could get enough scope for further designing and modification of developed protocols.


Synthesis ◽  
2021 ◽  
Author(s):  
Angelica Peñaranda ◽  
Carlos Eduardo E. Puerto Galvis ◽  
Mario Alberto Macias ◽  
Cristian Ochoa-Puentes ◽  
Vladimir V. Kouznetsov

A tandem approach was developed for the efficient synthesis of substituted chromeno[4,3-b]quinolines from arylamines and O-cinnamyloxy salicylaldehydes under metal-catalyst and photosensitizer-free reaction conditions. Our protocol is based on an inexpensive I2/DMSO system in which molecular iodine first acts as a Lewis acid to promote the formation of the corresponding imine bearing the alkene moiety, then, this species fulfills a second role by catalyzing the intramolecular aza-Diels-Alder cycloaddition to generate the respective tetrahydro-chromenoquinolines as an intermediates. Finally, the dual behaviour of DMSO as an oxidant and as a solvent resulted crucial at this stage, allowing the regeneration of I2 and promoting the aromatization of the tetrahydro-chromenoquinoline intermediates to yield the desired 7-aryl-6H-chromeno[4,3-b]quinolines. This protocol features by being mild, easy to perform, high step-economy (tandem process) and for providing a new access to biologically important nitrogen and oxygen containing heterocyclic molecules.


2021 ◽  
Vol 25 ◽  
Author(s):  
Bharatkumar M. Sapkal ◽  
Shamrao T. Disale ◽  
Raghunath B. Toche ◽  
Dhananjay H. More

: In the last few decades, substituted urea derivatives have got significant importance due to their wide applications in pharmaceutical, polymer, dyes, and agriculture industries. Urea derivatives are the key starting material for the synthesis of novel bioactive heterocyclic molecules. Substituted urea derivatives are known to possess a wide array of biological activities such as herbicidal, antimicrobial, antimalarial, antivirus, anticancer, antioxidants, antiproliferative, antiatherosclerotic, anti-inflammatory, antibiotic, sedatives, anticonvulsants and acting as HIV-1 protease inhibitor. Herein, the synthetic approach and its herbicidal, anticonvulsant, antimicrobial, and antiproliferative activities are reviewed. This review summarizes the current updates regarding the syntheses and biological behavior of substituted urea.


Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2620
Author(s):  
Federico Vittorio Rossi ◽  
Dario Gentili ◽  
Enrico Marcantoni

The outbreak of SARS-CoV-2 has drastically changed our everyday life and the life of scientists from all over the world. In the last year, the scientific community has faced this worldwide threat using any tool available in order to find an effective response. The recent formulation, production, and ongoing administration of vaccines represent a starting point in the battle against SARS-CoV-2, but they cannot be the only aid available. In this regard, the use of drugs capable to mitigate and fight the virus is a crucial aspect of the pharmacological strategy. Among the plethora of approved drugs, a consistent element is a heterocyclic framework inside its skeleton. Heterocycles have played a pivotal role for decades in the pharmaceutical industry due to their high bioactivity derived from anticancer, antiviral, and anti-inflammatory capabilities. In this context, the development of new performing and sustainable synthetic strategies to obtain heterocyclic molecules has become a key focus of scientists. In this review, we present the recent trends in metal-promoted heterocyclization, and we focus our attention on the construction of heterocycles associated with the skeleton of drugs targeting SARS-CoV-2 coronavirus.


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