Previous Issue
Volume 6, March
 
 

Organics, Volume 6, Issue 2 (June 2025) – 6 articles

  • Issues are regarded as officially published after their release is announced to the table of contents alert mailing list.
  • You may sign up for e-mail alerts to receive table of contents of newly released issues.
  • PDF is the official format for papers published in both, html and pdf forms. To view the papers in pdf format, click on the "PDF Full-text" link, and use the free Adobe Reader to open them.
Order results
Result details
Select all
Export citation of selected articles as:
18 pages, 4205 KiB  
Article
Synthesis of Bipyridine Ether-Type Bifunctional Precursors
by Bálint Jávor, Antal Agárdi, Péter Kisfaludi, Barnabás Frigyes, Márton Temesvári, Panna Vezse, Tünde Tóth, Péter Huszthy and Ádám Golcs
Organics 2025, 6(2), 18; https://doi.org/10.3390/org6020018 - 10 Apr 2025
Viewed by 213
Abstract
Bipyridine ethers are commonly occurring structural motifs in supramolecular chemistry. The herein reported efforts aim to extend the synthetic platform of bipyridino-precursors with new bifunctional intermediates and to improve some previously reported synthetic strategies for structural analogues, like bipyridine-diols as common macrocycle precursors. [...] Read more.
Bipyridine ethers are commonly occurring structural motifs in supramolecular chemistry. The herein reported efforts aim to extend the synthetic platform of bipyridino-precursors with new bifunctional intermediates and to improve some previously reported synthetic strategies for structural analogues, like bipyridine-diols as common macrocycle precursors. In addition, their optimized and highly efficient oxidation to the corresponding dialdehydes is reported to obtain further reactive intermediates with wide modifiability. Furthermore, methylations of pyridine-carbaldehydes were carried out alongside different synthetic strategies to introduce chirality centers. Synthetic difficulties and some unsuccessful approaches are also reported to help in focusing future efforts. Full article
(This article belongs to the Special Issue Chemistry of Heterocyclic Compounds)
Show Figures

Graphical abstract

13 pages, 3347 KiB  
Article
Small Deviations in Geometries Affect Detonation Velocities and Pressures of Nitroaromatic Molecules
by Danijela S. Kretić, Marija I. Maslarević and Dušan Ž. Veljković
Organics 2025, 6(2), 17; https://doi.org/10.3390/org6020017 - 9 Apr 2025
Viewed by 229
Abstract
Understanding the factors that affect the detonation performance of high-energy molecules (HEMs) is crucial for the design of novel explosives and fuels with desirable characteristics. While molecular factors, such as the presence of specific functional groups that give organic molecules explosive properties, are [...] Read more.
Understanding the factors that affect the detonation performance of high-energy molecules (HEMs) is crucial for the design of novel explosives and fuels with desirable characteristics. While molecular factors, such as the presence of specific functional groups that give organic molecules explosive properties, are key determinants of detonation characteristics, other factors like the geometry of molecules in crystal structures can also affect the high-energy properties of materials. Although it is known that slight deviations in the crystal structure geometry affect the sensitivity of nitroaromatic explosives, the influence of these variations on detonation performance remains unknown. In this study, we extracted different crystal structures of the same high-energy nitroaromatic molecules from the Cambridge Structural Database and calculated their detonation velocities and pressures using the Kamlet–Jacobs equations. Results indicated that different geometries of the same crystal structure can lead to non-negligible differences in detonation velocities and pressures. In the case of the 2,4,6-triamino-1,3,5-trinitrobenzene molecule, discrepancies in detonation pressures among different crystal structures were calculated to be 7.68%. Analysis of geometrical arrangements showed that these differences are mainly the consequence of diverse non-covalent bonding patterns that affect crystal densities. Full article
Show Figures

Figure 1

49 pages, 14143 KiB  
Review
An Overview of Quinolones as Potential Drugs: Synthesis, Reactivity and Biological Activities
by Ayoub El-mrabet, Amal Haoudi, Youssef Kandri-Rodi and Ahmed Mazzah
Organics 2025, 6(2), 16; https://doi.org/10.3390/org6020016 - 3 Apr 2025
Viewed by 403
Abstract
Quinolones represent one of the largest classes of synthetic antibiotics used in both human and veterinary medicine. Since the discovery of nalidixic acid, a substantial body of research has been carried out on quinolones, resulting in the synthesis of several quinolone derivatives with [...] Read more.
Quinolones represent one of the largest classes of synthetic antibiotics used in both human and veterinary medicine. Since the discovery of nalidixic acid, a substantial body of research has been carried out on quinolones, resulting in the synthesis of several quinolone derivatives with exceptional pharmacology. In addition to their antibacterial action, quinolones have a broad spectrum of diverse biological activities. In this regard, the present review examines the literature of recent years describing synthesis protocols, reactivity and biological properties, with particular emphasis on the antibacterial, antimalarial, antitrypanosomal, antileishmanial, antiviral and anticancer activities of this famous class of molecules. Finally, this review highlights the potential of quinolones as preferred pharmacophores in medicinal chemistry. The aim is to highlight the innovative aspects of the rational design of new therapeutic agents with this structural motif, in the face of emerging antibiotic resistance and the urgent need for new active molecules. Full article
Show Figures

Graphical abstract

11 pages, 1186 KiB  
Article
Synthesis of Indole-Based Derivatives Containing Ammonium Salts, Diamines and Aminoureas for Organocatalysis
by Marcello Casertano, Brian G. Kelly, Malachi W. Gillick-Healy, Paolo Grieco and Mauro F. A. Adamo
Organics 2025, 6(2), 15; https://doi.org/10.3390/org6020015 - 2 Apr 2025
Viewed by 230
Abstract
Indole heterocycles have an established reactivity, and these compounds are H-bond donors via a peculiar non-basic NH. However, the indole core has been scarcely employed in organocatalysis, with only a few examples relevant to electrophilic halogenation reported. To expand the range of potential [...] Read more.
Indole heterocycles have an established reactivity, and these compounds are H-bond donors via a peculiar non-basic NH. However, the indole core has been scarcely employed in organocatalysis, with only a few examples relevant to electrophilic halogenation reported. To expand the range of potential transformations achievable via indole catalysis, we have designed a set of new organic species incorporating an indole core, alongside three privelaged chiral moieties found in many known organocatalysts, namely a quaternary ammonium salt, a diamine and an amino-urea. Herein, we report an optimised synthetic route for the preparation of these potential catalytic species in an enantiomerically pure form. The syntheses are conceived to be modular and therefore will allow each of the three single organic catalysts to be expanded into families without alteration of the synthetic layout, therefore leading to a fast optimisation of new asymmetric procedures. Full article
Show Figures

Graphical abstract

9 pages, 689 KiB  
Article
Optimized Synthesis of Dinitrochalcones via Ultrasonic Bath in a Cyclohexane–Methanol Solvent System
by Alam Yair Hidalgo, Quirino Torres-Sauret, Carlos Ernesto Lobato-García, Erika Madeleyne Ramos-Rivera, Luis Fernando Roa de la Fuente, Abraham Gómez-Rivera, Miguel Ángel Vilchis-Reyes, Erika Alarcón-Matus, Oswaldo Hernández-Abreu and Nancy Romero-Ceronio
Organics 2025, 6(2), 14; https://doi.org/10.3390/org6020014 - 1 Apr 2025
Viewed by 237
Abstract
This study describes the efficient synthesis of five dinitrochalcones (DNCHs) using an ultrasonic bath as an unconventional method to improve reaction yields and reduce reaction times. The Claisen–Schmidt condensation of nitroacetophenones and nitrobenzaldehydes was carried out in a cyclohexane–methanol solvent system under ultrasonic [...] Read more.
This study describes the efficient synthesis of five dinitrochalcones (DNCHs) using an ultrasonic bath as an unconventional method to improve reaction yields and reduce reaction times. The Claisen–Schmidt condensation of nitroacetophenones and nitrobenzaldehydes was carried out in a cyclohexane–methanol solvent system under ultrasonic irradiation, achieving yields between 56% and 92%. The application of ultrasound not only accelerated the reaction but also improved the overall efficiency compared to conventional methods such as magnetic stirring. The synthesized compounds were characterized by NMR spectroscopy, which corroborated their structures. Therefore, it is confirmed that obtaining DNCHs with a nitro group in ortho by ultrasonic irradiation is an energetically efficient and environmentally friendly alternative. Full article
Show Figures

Figure 1

26 pages, 8018 KiB  
Article
Synthesis and In Silico Evaluation of GABA, Pregabalin and Baclofen N-Heterocyclic Analogues as GABAB Receptor Agonists
by Zuleyma Martínez-Campos, Luis Eduardo Hernandez-Dominguez, Fatima Romero-Rivera, Diana López-López, María Vicky Corona-González, Susana T. López-Cortina, Francisco José Palacios-Can, Rodrigo Said Razo-Hernández and Mario Fernández-Zertuche
Organics 2025, 6(2), 13; https://doi.org/10.3390/org6020013 - 24 Mar 2025
Viewed by 251
Abstract
γ-amino butyric acid (GABA) is an inhibitory neurotransmitter whose deficiency has been associated with various neurological disorders. However, its low liposolubility limits its use as a supplement. Thus, multiple investigations have focused on searching for lipophilic GABA analogs that can modulate the [...] Read more.
γ-amino butyric acid (GABA) is an inhibitory neurotransmitter whose deficiency has been associated with various neurological disorders. However, its low liposolubility limits its use as a supplement. Thus, multiple investigations have focused on searching for lipophilic GABA analogs that can modulate the activity of the GABAB receptor, which could be associated with the etiology of some central nervous system disorders. The GABA analogs available on the market are Vigabatrin, Gabapentin as well as Pregabalin and Baclofen. In this work, we report on the synthesis of GABA analogs, taking the scaffold of GABA, Pregabalin, and Baclofen as a starting point. The analogs include structural features that could favor the affinity of the molecules for the GABAB receptor, such as heterocyclic rings in the γ-position and alkyl or p-Cl-phenyl substituents (in analogy to Pregabalin and Baclofen, respectively). These analogs were synthesized by a sequence of reactions involving an N-alkylation, a 1,4-conjugated addition of dialkyl and diarylcuprates and a basic hydrolysis. Furthermore, a computational molecular docking over the GABAB receptor was performed to evaluate the interaction of each compound in the Baclofen binding site. With this information, we evaluated our compounds as GABAB agonists through a QSAR analysis. Finally, by means of molecular similarity analysis, and in silico ADME prediction, we support our three best compounds (8ab, 8d) as potential GABAB receptor agonists. Full article
Show Figures

Graphical abstract

Previous Issue
Back to TopTop