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Total Synthesis of Biologically Active Product
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Total Synthesis of Biologically Active Product

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Organic Chemistry".

Deadline for manuscript submissions: closed (30 May 2020) | Viewed by 15583

Special Issue Editor

Dr. Marc C. Kimber

E-Mail Website
Guest Editor
Department of Chemistry, Loughborough University, Loughborough, UK
Interests: target synthesis; alkynes; allenes; allenamides; homogenous transition metal catalysis

Special Issue Information

Dear Colleagues,

Biologically active products, whether derived from nature or synthetic in origin, have been vital in the elucidation of numerous biological processes and in the treatment of human diseases. While the identification of a biological active product is central to the development of new drug, crucially it is their total synthesis that can provide key mechanistic understandings, as well as delivering a ‘practical’ synthetic route for the supply of valuable materials. The synthetic chemist has been pivotal to this success, by developing novel and innovative total syntheses. This development has been motivated by several factors including (a) curiosity—where a total synthesis is inspired by the unique chemical structure of a natural product; (b) methodology—where the total synthesis of biological product is used to display a novel synthetic methodology; and (c) efficiency—where an existing total synthesis of biologically active products requires streamlining.

In this forthcoming Special Issue of Molecules entitled “Total Synthesis of Biologically Active Products” we invite contributions on the total synthesis of biologically-active products, including recent key findings, latest developments and innovative synthetic approaches.

Dr. Marc C. Kimber
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Total synthesis
  • Natural products
  • Asymmetric synthesis
  • Chiral pool
  • Catalysis

Published Papers (4 papers)

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Research

22 pages, 2139 KiB  
Article
Total Syntheses of Marrubiin and Related Labdane Diterpene Lactones
by Yukari Sakagami, Naoki Kondo, Yuki Sawayama, Hiroyuki Yamakoshi and Seiichi Nakamura
Molecules 2020, 25(7), 1610; https://doi.org/10.3390/molecules25071610 - 01 Apr 2020
Cited by 5 | Viewed by 3173
Abstract
Total syntheses of the labdane diterpene lactones marrubiin, marrulibacetal, desertine, marrulibacetal A, marrubasch F, cyllenine C, marrulanic acid, and marrulactone are described. The trans-decalin moiety of these molecules was constructed in a stereoselective manner by a Pauson-Khand reaction, and the resultant cyclopentenone [...] Read more.
Total syntheses of the labdane diterpene lactones marrubiin, marrulibacetal, desertine, marrulibacetal A, marrubasch F, cyllenine C, marrulanic acid, and marrulactone are described. The trans-decalin moiety of these molecules was constructed in a stereoselective manner by a Pauson-Khand reaction, and the resultant cyclopentenone was oxidatively cleaved for formation of the lactone ring. Elongation of the side chain at C9 was achieved by an epoxide-opening reaction with a variety of nucleophiles, and the functional group manipulations completed the syntheses of these natural products. Stereochemistries of desertine could be established by the transformations. Full article
(This article belongs to the Special Issue Total Synthesis of Biologically Active Product)
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11 pages, 1758 KiB  
Article
Palladium(II)-Catalyzed Efficient Synthesis of Wedelolactone and Evaluation as Potential Tyrosinase Inhibitor
by Huidan Huang, Jianqiu Chen, Jie Ren, Chaofeng Zhang and Fei Ji
Molecules 2019, 24(22), 4130; https://doi.org/10.3390/molecules24224130 - 15 Nov 2019
Cited by 3 | Viewed by 2926
Abstract
Tyrosinase is an enzyme widely distributed in nature, which has multiple functions, especially in the melanin biosynthesis pathway. Despite the few clinically available tyrosinase inhibitors for whitening, a great demand remains for novel compounds with low side effects in terms of potential carcinogenicity [...] Read more.
Tyrosinase is an enzyme widely distributed in nature, which has multiple functions, especially in the melanin biosynthesis pathway. Despite the few clinically available tyrosinase inhibitors for whitening, a great demand remains for novel compounds with low side effects in terms of potential carcinogenicity and improved clinical efficacy. A natural product, wedelolactone (WEL), with a polyhydroxyl moiety, attracted our attention as a potential tyrosinase inhibitor. Before we studied the biological activity of the natural product, a synthetic methodological research was firstly carried to obtain enough raw material. WEL could be obtained efficiently through palladium-catalyzed boronation/coupling reactions and 2,3-dicyano-5,6-dichlorobenzoquinone (DDQ)-involved oxidative deprotection/annulation reactions. Immediately after, the natural product was proven to be an efficient tyrosinase inhibitor. In conclusion, we developed a mild and efficient approach for the preparation of WEL, and the natural product was disclosed to have anti-tyrosinase activity, which could be widely used in multiple fields. Full article
(This article belongs to the Special Issue Total Synthesis of Biologically Active Product)
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9 pages, 1157 KiB  
Communication
Concise and Gram-Scale Total Synthesis of Lansiumamides A and B and Alatamide
by Ran Lin, Xi Lin, Qian Su, Binbin Guo, Yanqin Huang, Ming-An Ouyang, Liyan Song and Huiyou Xu
Molecules 2019, 24(20), 3764; https://doi.org/10.3390/molecules24203764 - 19 Oct 2019
Cited by 4 | Viewed by 3157
Abstract
The total synthesis of potent anti-obesity lansiumamide B was accomplished in four steps using commercially available materials. The synthetic strategy, featured with copper-catalyzed Buchwald coupling, is concise, convergent, practical and can be carried out on a one-gram scale. This approach could give either [...] Read more.
The total synthesis of potent anti-obesity lansiumamide B was accomplished in four steps using commercially available materials. The synthetic strategy, featured with copper-catalyzed Buchwald coupling, is concise, convergent, practical and can be carried out on a one-gram scale. This approach could give either Z- or E-configured enamide moiety in natural products with absolute stereocontrol and was applied in the total synthesis of natural products. Full article
(This article belongs to the Special Issue Total Synthesis of Biologically Active Product)
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12 pages, 1952 KiB  
Article
Total Synthesis and Antimicrobial Evaluation of 23-Demethyleushearilide and Extensive Antimicrobial Evaluation of All Synthetic Stereoisomers of (16Z,20E)-Eushearilide and (16E,20E)-Eushearilide
by Takayuki Tonoi, Takehiko Inohana, Teruyuki Sato, Yuuki Noda, Miyuki Ikeda, Miku Akutsu, Takatsugu Murata, Yutaro Maekawa, Anna Tanaka, Rio Seki, Misako Ohkusu, Katsuhiko Kamei, Naruhiko Ishiwada and Isamu Shiina
Molecules 2019, 24(19), 3437; https://doi.org/10.3390/molecules24193437 - 22 Sep 2019
Cited by 5 | Viewed by 5899
Abstract
A novel stereoisomer of eushearilide, 23-demethyleushearilide, was synthesized, and the structure–activity relationships of this compound along with known eushearilide stereoisomers were investigated in order to design novel lead compounds for the treatment of fungal infections. It was discovered that all of these congeners, [...] Read more.
A novel stereoisomer of eushearilide, 23-demethyleushearilide, was synthesized, and the structure–activity relationships of this compound along with known eushearilide stereoisomers were investigated in order to design novel lead compounds for the treatment of fungal infections. It was discovered that all of these congeners, together with the natural product, exhibited a wide range of antimicrobial activity against not only fungi but also against bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Full article
(This article belongs to the Special Issue Total Synthesis of Biologically Active Product)
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