Pharmaceutical Chemistry
Moath Kahtan Bashir; Mahmood Khudhayer Oglah; Yasser Fakri Mustafa; Ahmed Abdul-jabbar Mahmood
Abstract
Background: The problem of drug side effects necessitates the design, synthesis, and development of novel therapeutic agents that possess high activity with minimal side effects. According to the structure-activity relationship, the dioxolane moiety is found in many natural therapeutic agents and plays ...
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Background: The problem of drug side effects necessitates the design, synthesis, and development of novel therapeutic agents that possess high activity with minimal side effects. According to the structure-activity relationship, the dioxolane moiety is found in many natural therapeutic agents and plays an important role in their medical action. Synthetic dioxolane conjugates have been studied in a variety of biological fields, including cytotoxicity, antibacterial, antifungal, antiviral, antioxidant, and anti-inflammatory activity, and have demonstrated a distinct potency that encourages further research in this mode. Aim: This review highlights the most recent studies on dioxolane ring conjugates in various biological fields as a promising bioactive heterocyclic scaffold. Conclusion: The hydrogen bonding of the oxygen atoms in this heterocyclic ring with the target site may be responsible for the enhanced ligand-target interactions and improved bioactivity.
Pharmaceutical Chemistry
Noor Ahmed Waheed; Noora Thamer Abdulaziz; Sawsan Hasan Hammodi; Yasser Fakri Mustafa
Abstract
Background: Particularly developed ingredients that are easily manufactured and utilized for additional exploitation are used in organic synthetic chemistry. Thionyl chloride serves as a significant illustration of such an ingredient. The usefulness of which has been discussed in a huge number of peer-reviewed ...
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Background: Particularly developed ingredients that are easily manufactured and utilized for additional exploitation are used in organic synthetic chemistry. Thionyl chloride serves as a significant illustration of such an ingredient. The usefulness of which has been discussed in a huge number of peer-reviewed papers. Aim: The literature that has been released since the previous assessment in 1980, which mainly focused on the responses of active methylene compounds, is where this review places its focus. In the present overview, we also discuss O- and N-nucleophiles. For the most part, patents have been disregarded in this analysis in order to keep it feasible. Conclusion: The authors concluded that SOCl2 has a variety of behaviors, including the ability to function as an initiator or a reactant, which makes it essential for the synthesis of many chemically reactive intermediates and final products. Additionally, SOCl2 can speed up and reduce the duration of traditionally long reactions, thereby raising its importance.
Pharmaceutical Chemistry
Rana Naeem Jibroo; Yasser Fakri Mustafa; Wejdan Al-Shakarchi
Abstract
Background: Coumarin-based derivatives (Cou-Ds) are one of the most important types of heterocycles, with a wide range of uses in synthetic and medicinal chemistry. Cou-Ds have interested researchers due to their wide range of biomedical potential and application as valuable synthetic scaffolds, which ...
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Background: Coumarin-based derivatives (Cou-Ds) are one of the most important types of heterocycles, with a wide range of uses in synthetic and medicinal chemistry. Cou-Ds have interested researchers due to their wide range of biomedical potential and application as valuable synthetic scaffolds, which have been instrumental in the creation of coumarin chemistry. Cou-Ds are a unique class of bioactive candidates with novel therapeutic attributes due to their bacteriostatic, antifungal, antioxidant, anticancer, antidepressant, and other pharmacological properties. In addition to their biomedical uses, the literature illustrates the uses of Cou-Ds from a material point of view, such as those in food additives, fragrances, beauty products, optical brighteners, and would disperse fluorescent and laser dyes. Numerous optical purposes using Cou-Ds have been thoroughly investigated. A wide range of natural sources and newly created Cou-Ds are being isolated or produced at a growing rate. The procedures of synthesis and therapeutic uses of Cou-Ds in the treatment of various illnesses were critically found in many published papers. Aim: The aim of this review article is to highlight the most up-to-date information about Cou-Ds and clarify the various natural sources, synthetic strategies, reactions, biological activity, and different pharmaceutical applications of Cou-Ds. Conclusion: From the collected and discussed reviewing information, the authors concluded that the Cou-Ds can open the drug development door for producing more potent, biosafe medicines.
Pharmaceutical Chemistry
Nameer Mazin Zeki; Yasser Fakri Mustafa
Abstract
Background: Esculetin, scientifically referred to as 6,7-dihydroxycoumarin, functions as the primary bioactive constituent found in Cortex Fraxini (commonly known as ash bark), an ancient Asian medicinal substance. Herbal practitioners utilize the outer layer of the branch or stem bark of Cortex Fraxini ...
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Background: Esculetin, scientifically referred to as 6,7-dihydroxycoumarin, functions as the primary bioactive constituent found in Cortex Fraxini (commonly known as ash bark), an ancient Asian medicinal substance. Herbal practitioners utilize the outer layer of the branch or stem bark of Cortex Fraxini for its gentle and safe medicinal properties and its potential as a nutritional component. In contemporary times, the landscape has undergone a notable transformation due to the emergence of a wide range of innovative 6,7-dihydroxycoumarin derivatives. The recent surge of innovation has sparked a heightened interest in understanding the molecular mechanisms that underlie the effects of Cortex Fraxini and 6,7-dihydroxycoumarin in clinical applications. Aim: This succinct review seeks to build up the extensive knowledge accumulated in the past decade concerning the synthesis, pharmacological profiles and principles linked to 6,7-dihydroxycoumarin and its chemical analogues. Furthermore, we aim to provide a concise yet inclusive overview of the unique characteristics of 6,7-dihydroxycoumarin. Conclusion: Satisfying these aims can enhance the comprehension of the diverse possibilities presented by this chemical and its related compounds across different research and application domains.
Pharmaceutical Chemistry
Sawsan Hasan Hammodi
Abstract
Background: Coumarin chemical moiety and its-based molecules attracted a lot of research attention by chemists of natural products and organic synthesis. This attention works in two directions: synthetic approaches and biological activities. Methods: In this work, salicylaldehyde was condensed via a ...
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Background: Coumarin chemical moiety and its-based molecules attracted a lot of research attention by chemists of natural products and organic synthesis. This attention works in two directions: synthetic approaches and biological activities. Methods: In this work, salicylaldehyde was condensed via a thermosonication-catalyzed Knoevenagel reaction with malonic acid, giving coumarin-3-carboxylic acid. The latter was esterified through its carboxylic acid with various 2-functionalized phenols under a thermosonication-promoted SOCl2-catalized esterification reaction. The four 3-esterified coumarins (SY1–SY4) were characterized by different spectrophotometer analyzers, including FTIR, 1H-NMR, and 13C-NMR. Four cell lines of malignant type and one of normal class were used to specify the antitumor activity and biocompatibility of the synthetic SY1-SY4, respectively, by employing the MTT-probing methodology. Results: The outcomes indicated the accuracy of the proposed molecular structures, and the synthetic compounds have poor, with the exception of SY1, antitumor activity. Also, the antiproliferative effect of the three compounds (SY2-SY4) is roughly similar against malignant and normal cells. On the other hand, the compound SY1 demonstrated good antitumor activity against the malignant cells used but a poor inhibitory effect toward normal cells. Conclusion: The author concluded from these findings that the molecular structure of SY1 can offer a promising template to synthesize more potent and biocompatible antitumor agents with a coumarin chemical nucleus.
Pharmaceutical Chemistry
Yasser Fakri Mustafa; Sarah Ahmed Waheed; Sara Firas Jasim; Rahma Mowaffaq Jebir; Reem Nadher Ismael; Omar Qutachi
Abstract
Background: Coumarins and their derivatives excel in chemical diversity, coupled with a wide variety of biological potentials, and tend to be beneficial to the health of the human body. One of these derivatives that has sparked the attention of medicinal chemistry specialists in recent decades is benzo-fused ...
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Background: Coumarins and their derivatives excel in chemical diversity, coupled with a wide variety of biological potentials, and tend to be beneficial to the health of the human body. One of these derivatives that has sparked the attention of medicinal chemistry specialists in recent decades is benzo-fused coumarins, which have demonstrated their potential as antioxidants, antimicrobials, antidiabetics, antithrombotics, and many more. Objective: This paper discusses the medicinal importance of benzo-fused coumarins derived from natural or synthetic sources. Conclusion: The researchers documented that benzo-fused coumarin's basic structure is a promising framework that opens up the chance of discovering innovative applicants with advanced therapeutic potentials.
Pharmaceutical Chemistry
Ahmed A. Saleh; Ahmed A. J. Mahmood
Abstract
Background: Antibiotics with β-Lactam rings (β-Lactams), since they were discovered, have enhanced the typical treatment for bacterial infections. Though their resistance can quickly spread on a universal scale, bacterial resistance is primarily caused by the production of β-lactamases. ...
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Background: Antibiotics with β-Lactam rings (β-Lactams), since they were discovered, have enhanced the typical treatment for bacterial infections. Though their resistance can quickly spread on a universal scale, bacterial resistance is primarily caused by the production of β-lactamases. Hence, there is a serious demand to design and create new anti-β-lactamases or inhibitors. Nowadays, the use of β-lactamase inhibitors with β-lactams reduces this resistance. Aim and Methods: This work aimed to help in silico design and dock two new series of 7-aminocephalosporinic acid derivatives (Schiff’s bases and amides) against both the TEM-1 and the IMP-1 β-lactamases. Results: The results revolve around the possible enhanced activity of eight amides and six Schiff base compounds compared with the standard inhibitors (clavulanic acid, sulbactam, and avabactam). These compounds show promising docking interactions with an active pocket site in both enzymes. Conclosin: We can conclude that both the halogenated and the hydrophobic substituents, alone or when containing oxygen atoms, will potentiate the affinity and the binding ability of any compounds when they are added to their structures to act as β-lactamase inhibitors.