Dear Colleagues,

Historically, small-molecule screening collections have tended to be heavily populated with achiral, aromatic compounds that can be prepared efficiently and at low cost, but which occupy a narrow region of chemical space. These collections have led to major contributions to our drug pharmacopeia, but have not produced useful leads for numerous targets. This failure has led to the outlook that we may not be able to find pharmaceuticals for such targets.

However, we have recently witnessed the emergence of many innovative strategies for the assembly of chemically diverse libraries that cover a much broader region of chemical space. Diversity-oriented synthesis offers a systematic and efficient strategy to synthesize collections of structurally complex and functionally diverse small molecules that may ultimately exert their biological effects through unique mechanisms. DOS libraries have various common features, such as an increased ratio of sp³-hybridized atoms and a greater number of stereogenic elements relative to conventional compound libraries. These collections combine the structural complexity of natural products with the efficiency of high-throughput synthesis. These new diverse molecular scaffolds are leading to remarkable advances in chemistry and biology.

For this Special Issue, we invite the submission of manuscripts focusing on current investigations in the field of DOS, such as the development and evaluation of new synthetic strategies and approaches, and the application of these diverse molecular scaffolds in probing new biology.

Dr. Eamon Comer
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.

• diversity-oriented synthesis
• asymmetric synthesis
• next generation synthesis
• stereodivergence and stereoselectivity
• chemical library synthesis
• probe molecules
• biologically active molecules
• drug discovery
• molecular scaffolds