State-of-the-Art of Medicinal and Synthetic Organic Chemistry

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Chemical and Molecular Sciences".

Deadline for manuscript submissions: closed (20 July 2022) | Viewed by 25449

Special Issue Editors


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Guest Editor
Department of DICATECh, Polytechnic University of Bari, 70126 Bari, BA, Italy
Interests: synthetic organic chemistry; medicinal chemistry; carbohydrate chemistry; chemical biology; synthetic chemistry and materials; agrochemicals
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
DICATECh, Polytechnic University of Bari, Bari, Italy
Interests: spectroscopy; process chemistry; food chemistry; environmental chemistry; metabolomics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Organic and Medicinal Chemistry represent key branches of Chemistry, and their impact on our life is an undeniable fact. The prospect to modify and manipulate chemicals with always more emerging and innovative methods expands the possibility to synthesize new compounds and molecules. The research of new methodologies, new reaction classes, and new chemical entities are attractive fields on which thousands of researchers worldwide focus their efforts. The achieved discoveries and goals in these disciplines have strong and positive upshots on our everyday life and on our health, as recently emerged during the COVID-19 pandemic. Research activities in these fields are meant to consolidate and increase, helping the scientific community overcome the continuous challenges that will have to be faced.

Therefore, the Special Issue “State-of-the-Art in Medicinal and Synthetic Organic Chemistry” aims to collect significant research works recently developed and bring out new ideas in the fields of Medicinal and Organic Chemistry, both as original papers and review articles. The Special Issue will consider recent works highlighting contributions on the following topics:

  • Organic synthesis and innovative methodologies;
  • Synthetic processes (including flow chemistry, microwave-assisted chemistry);
  • Homogeneous and heterogeneous catalysis;
  • Green chemistry;
  • Medicinal chemistry;
  • Agrochemicals and agro-drugs;
  • Bio-organic chemistry and chemical biology;
  • Natural products synthesis;
  • Studies of the reaction mechanism;
  • Synthetic materials and polymer chemistry.

Dr. Giuseppe D'Orazio
Dr. Biagia Musio
Guest Editors

Manuscript Submission Information

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Keywords

  • organic synthesis and innovative methodologies
  • synthetic processes (including flow chemistry, microwave-assisted chemistry)
  • homogeneous and heterogeneous catalysis
  • green chemistry
  • medicinal chemistry
  • agrochemicals and agro-drugs
  • bio-organic chemistry and chemical biology
  • natural products synthesis
  • studies of the reaction mechanism
  • synthetic materials and polymer chemistry

Published Papers (5 papers)

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Research

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12 pages, 1897 KiB  
Article
Recent Trends on UV filters
by Ana Jesus, Inês Augusto, Joana Duarte, Emília Sousa, Honorina Cidade, Maria T. Cruz, José M. Sousa Lobo and Isabel F. Almeida
Appl. Sci. 2022, 12(23), 12003; https://doi.org/10.3390/app122312003 - 24 Nov 2022
Cited by 7 | Viewed by 5825
Abstract
UV filters are the shield ingredients of sunscreens against the negative effects of solar radiation. Since the discovery of the first UV filter, nearly 30 filters have become commercially available. Over the years, innovation and regulatory updates have driven their use by the [...] Read more.
UV filters are the shield ingredients of sunscreens against the negative effects of solar radiation. Since the discovery of the first UV filter, nearly 30 filters have become commercially available. Over the years, innovation and regulatory updates have driven their use by the cosmetic industry. This work aimed to characterize commercial sunscreens and unveil the main trends by analyzing the labels of 444 sunscreen formulations that are currently being marketed. Avobenzone, octocrylene, and bis-ethylhexyloxyphenol methoxyphenyl triazine were the three UV filters with the highest usage frequencies (>40%). Emulsified preparations and sprays were the preferred forms, while the most frequent SPF was 50+. Differences were noted between adult and children’s sunscreens, namely the higher usage of inorganic filters for the latter. Over the past few years, the five most used UV filters remained the same, but octocrylene, ethylhexyl salicylate, and nano methylene bis-benzotriazolyl tetramethylbutylphenol had decreased usage. An increasing tendency towards the use of the inorganic UV filter titanium oxide was also observed. Overall, this study characterized the true market impact of approved UV filters and how the market has evolved over recent years. This insight can help pave the way for the design of new UV filters and is helpful for the assessment of environmental risks. Full article
(This article belongs to the Special Issue State-of-the-Art of Medicinal and Synthetic Organic Chemistry)
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13 pages, 3705 KiB  
Article
New Strategies for Potential Contrast Agents’ Synthons Highly Active to MRI Based on Gd3+, Eu3+, and Tb3+
by Carlos Guzmán, Rubén Soria-Martínez and Julián Urresta
Appl. Sci. 2022, 12(19), 9969; https://doi.org/10.3390/app12199969 - 04 Oct 2022
Viewed by 1240
Abstract
The library of new smart contrast agents based on Gd3+, Eu3+, and Tb3+ used as biomarkers is in continuous development due to its applications in diagnostic imaging. The search for safer and more efficient contrast agents has focused [...] Read more.
The library of new smart contrast agents based on Gd3+, Eu3+, and Tb3+ used as biomarkers is in continuous development due to its applications in diagnostic imaging. The search for safer and more efficient contrast agents has focused on the design of compounds that exhibit high relaxivity. Herein, we present alternative synthetic strategies for the development of theoretically high-relaxivity synthons based on lanthanides using the Solomon–Bloembergen–Morgan equations through click chemistry and direct addition. Special attention has been devoted to the analysis of the different aspects interfering with the successful acquisition of these complexes and their troubleshooting during their synthesis. Our preliminary results showed that not only the mathematical background needs to be considered, but also the synthetic strategy and the use of procedures free of metallic ions favor the total synthesis of these challenging complexes. Full article
(This article belongs to the Special Issue State-of-the-Art of Medicinal and Synthetic Organic Chemistry)
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11 pages, 1327 KiB  
Article
Design of an Emulgel for Psoriasis Focused on Patient Preferences
by Rita Sanches Oliveira, Diva Ferraz da Silva, Sandra Mota, Jorge Garrido, Ermelinda Manuela Garrido, José Manuel Sousa Lobo and Isabel Filipa Almeida
Appl. Sci. 2022, 12(7), 3260; https://doi.org/10.3390/app12073260 - 23 Mar 2022
Cited by 3 | Viewed by 3566
Abstract
Adherence to topical treatments is low and is known to be influenced by the vehicle properties. Betamethasone dipropionate (BD) is an anti-inflammatory steroid, used in psoriasis treatment in the form of an ointment, cream, or solution. The aim of this work was to [...] Read more.
Adherence to topical treatments is low and is known to be influenced by the vehicle properties. Betamethasone dipropionate (BD) is an anti-inflammatory steroid, used in psoriasis treatment in the form of an ointment, cream, or solution. The aim of this work was to develop a new vehicle for BD, focusing on the preferences of patients with psoriasis as a strategy to improve treatment adherence. Two vehicles with an aqueous external phase were explored: an emulgel and a hydrogel based on a cyclodextrin inclusion complex used to improve the aqueous solubility of BD. Since BD solubilization was not fully achieved in the hydrogel, only the emulgel was selected for further characterization. This new vehicle (emulgel) is characterized by its white, shiny appearance and good spreading properties. In comparison with petrolatum, a lower residue, higher evaporation rate, lower stickiness, and reduced ability to stain polyester fabric were observed. This vehicle also showed shear thinning behavior. The impact of this new vehicle on adherence to topical treatments should be further confirmed in clinical settings. Full article
(This article belongs to the Special Issue State-of-the-Art of Medicinal and Synthetic Organic Chemistry)
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15 pages, 1788 KiB  
Article
Skin Depigmenting Agents in Anti-Aging Cosmetics: A Medicinal Perspective on Emerging Ingredients
by Diana I. S. P. Resende, Marta S. Ferreira, José M. S. Lobo, Emília Sousa and Isabel F. Almeida
Appl. Sci. 2022, 12(2), 775; https://doi.org/10.3390/app12020775 - 13 Jan 2022
Cited by 10 | Viewed by 10274
Abstract
Human skin aging results from intrinsic and extrinsic factors. Uneven pigmentation is one of the major changes of extrinsic aging. Many compounds have been tested for depigmenting activity but only a few are actually used by the cosmetic industry, which is continually looking [...] Read more.
Human skin aging results from intrinsic and extrinsic factors. Uneven pigmentation is one of the major changes of extrinsic aging. Many compounds have been tested for depigmenting activity but only a few are actually used by the cosmetic industry, which is continually looking for new ingredients. In this study, the trends in the use of skin depigmenting ingredients in a panel of anti-aging formulations commercialized in the Portuguese pharmacy market were analyzed, by comparing the composition of the products marketed in 2011 with products launched or reformulated in 2018 (59% and 74%, respectively). The analysis of the top 12 ingredients put forward three novelties for 2018: tranexamic acid, bakuchiol, and 4-butylresorcinol. Regarding their mechanisms of action, tranexamic acid inhibits melanin synthesis through inhibition of the plasminogen/plasmin system. Bakuchiol depigmenting efficacy was attributed to the ability to block both α-melanocyte-stimulating hormone and tyrosinase activation, while 4-butylresorcinol exerts its action through the inhibition of both tyrosinase and tyrosinase-related protein-1 (TRP-1). Industry-optimized and efficient synthetic methodologies that embrace green chemistry, reducing the environmental impact, are commonly used. This analysis aims to bring insights to both formulators, involved in the development of depigmenting cosmetic products, and chemists performing the synthesis of new and existing compounds intended for this purpose. Full article
(This article belongs to the Special Issue State-of-the-Art of Medicinal and Synthetic Organic Chemistry)
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Review

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18 pages, 1526 KiB  
Review
Quercus suber: A Promising Sustainable Raw Material for Cosmetic Application
by Sandra Mota, Cláudia Pinto, Sara Cravo, Joana Rocha e Silva, Carlos Afonso, José Manuel Sousa Lobo, Maria Elizabeth Tiritan, Honorina Cidade and Isabel Filipa Almeida
Appl. Sci. 2022, 12(9), 4604; https://doi.org/10.3390/app12094604 - 03 May 2022
Cited by 11 | Viewed by 3509
Abstract
There is a drive within the cosmetic industry towards the development of more sustainable products, supported by consumer awareness of the environmental footprint. The cosmetic industry is rising to meet consumer demand by following practices, such as the use of by-products from agro-industrial [...] Read more.
There is a drive within the cosmetic industry towards the development of more sustainable products, supported by consumer awareness of the environmental footprint. The cosmetic industry is rising to meet consumer demand by following practices, such as the use of by-products from agro-industrial waste. Quercus suber is a tree prevalent in the Mediterranean basin. The extraction of cork is considered sustainable, as this process does not harm the tree, and the amount of cork produced increases with the number of extractions. Beyond this, the cork industry produces by-products that are used to sustain the industry itself, such as cork powder, which is reused for generating energy. Additionally, cork and cork by-products contain bioactive compounds mainly with antioxidant activity that can be of use to the cosmetic industry, such as for antiaging, anti-acne, anti-inflammatory, and depigmenting cosmetic products. We provide the reader with an overview of the putative cosmetic applications of cork and its by-products as well as of their bioactive compounds. It is noteworthy that only a few cork-based cosmetic products have reached the market, namely antiaging and exfoliant products. Clearly, the use of cork upcycled cosmetic ingredients will evolve in the future considering the wide array of biological activities already reported. Full article
(This article belongs to the Special Issue State-of-the-Art of Medicinal and Synthetic Organic Chemistry)
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