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Special Issue "Combinatorial Synthesis"

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A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (20 January 2014)

Special Issue Editors

Guest Editor
Prof. Dr. Fernando Albericio

1. School of Chemistry, University of KwaZulu-Natal, Durban 4001, South Africa
2. Department of Organic Chemistry, University of Barcelona, 08028-Barcelona, Spain
Website | E-Mail
Fax: +34 93 403 71 26
Interests: marine natural products; bioactive natural products; peptides; solid-phase chemistry; combinatorial chemistry; drug delivery systems
Guest Editor
Prof. Dr. Gert Kruger

School of Chemistry, University of KwaZulu-Natal, Durban 4001, South Africa
Website | E-Mail
Interests: chiral catalysis; cage chemistry; pharmaceutical applications of cage compounds

Special Issue Information

Dear Colleagues,

Combinatorial chemistry is a broad field that initially started with peptide synthesis but soon migrated to a much broader range of chemical reactions and applications. The field now involves various synthetic approaches, analytical methods and a magnitude of drug related applications. Synthetic methods involve solid phase and solution phase synthesis, spot synthesis, multicomponent reactions, combinatorial synthesis based on molecular recognition, combinatorial electrochemistry, cosmix-plexing, nucleotides, recombinant DNA synthesis, methods based on Serial Analysis of Gene Expression (SAGE), oligosaccharides, combinatorial catalysis, antibody production, combinatorial biosynthesis, shotgun bacteriophage display cloning and many more. Multiple analytical techniques were developed to facilitate improved methods, and high throughput screening in combination with combinatorial synthesis has also been developed. Finally, the combinatorial philosophy has also been applied to the field of material science.

This special issue of Molecules will consider any submission associated with combinatorial approaches related to the above mentioned topics.

Prof. Dr. Fernando Albericio
Prof. Dr. Gert Kruger
Guest Editors

Submission

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. Papers will be published continuously (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as 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 refereed through a 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 monthly 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 1800 CHF (Swiss Francs).


Keywords

  • combinatorial chemistry
  • combinatorial biology
  • combinatorial material sciences
  • paralell strategies
  • high throughput screening

Published Papers (3 papers)

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Research

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Open AccessArticle Ultrasound-Promoted One-Pot, Four-Component Synthesis of Pyridin-2(1H)-One Derivatives
Molecules 2013, 18(12), 14519-14528; doi:10.3390/molecules181214519
Received: 30 September 2013 / Revised: 19 November 2013 / Accepted: 19 November 2013 / Published: 25 November 2013
Cited by 4 | PDF Full-text (365 KB) | HTML Full-text | XML Full-text
Abstract
An efficient one-pot synthesis of 1,6-diamino-2-oxo-1,2,3,4-tetrahydro- pyridine-3,5-dicarbonitrile derivatives by four-component piperidine-catalyzed reactions of a ketone, malononitrile, ethyl cyanoacetate and hydrazine hydrate under ultrasound irradiation is described. This method provides several advantages such as shorter reaction times, excellent yields, and a simple workup procedure.
[...] Read more.
An efficient one-pot synthesis of 1,6-diamino-2-oxo-1,2,3,4-tetrahydro- pyridine-3,5-dicarbonitrile derivatives by four-component piperidine-catalyzed reactions of a ketone, malononitrile, ethyl cyanoacetate and hydrazine hydrate under ultrasound irradiation is described. This method provides several advantages such as shorter reaction times, excellent yields, and a simple workup procedure. Full article
(This article belongs to the Special Issue Combinatorial Synthesis)
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Open AccessArticle Combinatorial Techniques to Efficiently Investigate and Optimize Organic Thin Film Processing and Properties
Molecules 2013, 18(4), 4120-4139; doi:10.3390/molecules18044120
Received: 9 January 2013 / Revised: 2 April 2013 / Accepted: 3 April 2013 / Published: 8 April 2013
PDF Full-text (1441 KB) | HTML Full-text | XML Full-text
Abstract
In this article we present several developed and improved combinatorial techniques to optimize processing conditions and material properties of organic thin films. The combinatorial approach allows investigations of multi-variable dependencies and is the perfect tool to investigate organic thin films regarding their high
[...] Read more.
In this article we present several developed and improved combinatorial techniques to optimize processing conditions and material properties of organic thin films. The combinatorial approach allows investigations of multi-variable dependencies and is the perfect tool to investigate organic thin films regarding their high performance purposes. In this context we develop and establish the reliable preparation of gradients of material composition, temperature, exposure, and immersion time. Furthermore we demonstrate the smart application of combinations of composition and processing gradients to create combinatorial libraries. First a binary combinatorial library is created by applying two gradients perpendicular to each other. A third gradient is carried out in very small areas and arranged matrix-like over the entire binary combinatorial library resulting in a ternary combinatorial library. Ternary combinatorial libraries allow identifying precise trends for the optimization of multi-variable dependent processes which is demonstrated on the lithographic patterning process. Here we verify conclusively the strong interaction and thus the interdependency of variables in the preparation and properties of complex organic thin film systems. The established gradient preparation techniques are not limited to lithographic patterning. It is possible to utilize and transfer the reported combinatorial techniques to other multi-variable dependent processes and to investigate and optimize thin film layers and devices for optical, electro-optical, and electronic applications. Full article
(This article belongs to the Special Issue Combinatorial Synthesis)

Review

Jump to: Research

Open AccessReview Mixture-Based Combinatorial Libraries from Small Individual Peptide Libraries: A Case Study on α1-Antitrypsin Deficiency
Molecules 2014, 19(5), 6330-6348; doi:10.3390/molecules19056330
Received: 7 February 2014 / Revised: 12 May 2014 / Accepted: 13 May 2014 / Published: 16 May 2014
Cited by 3 | PDF Full-text (1425 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The design, synthesis and screening of diversity-oriented peptide libraries using a “libraries from libraries” strategy for the development of inhibitors of α1-antitrypsin deficiency are described. The major buttress of the biochemical approach presented here is the use of well-established solid-phase split-and-mix
[...] Read more.
The design, synthesis and screening of diversity-oriented peptide libraries using a “libraries from libraries” strategy for the development of inhibitors of α1-antitrypsin deficiency are described. The major buttress of the biochemical approach presented here is the use of well-established solid-phase split-and-mix method for the generation of mixture-based libraries. The combinatorial technique iterative deconvolution was employed for library screening. While molecular diversity is the general consideration of combinatorial libraries, exquisite design through systematic screening of small individual libraries is a prerequisite for effective library screening and can avoid potential problems in some cases. This review will also illustrate how large peptide libraries were designed, as well as how a conformation-sensitive assay was developed based on the mechanism of the conformational disease. Finally, the combinatorially selected peptide inhibitor capable of blocking abnormal protein aggregation will be characterized by biophysical, cellular and computational methods. Full article
(This article belongs to the Special Issue Combinatorial Synthesis)
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