Research Topic

Phosphonate Chemistry in Drug Design and Development

About this Research Topic

The current state of the chemical and biological sciences dictate that 5,000–10,000 chemical compounds must undergo laboratory screening for each new drug approved for use in humans. Of these, approximately 250 will enter preclinical testing, and only 5 will enter clinical testing. The overall process from discovery to marketing of a drug can take 10 to 15 years. Drug discovery includes drug design and development, and is a multifarious and expensive endeavor. Drug design is the inventive process of finding new medications based on the knowledge of a biological target. It defines the search for molecules that are complementary in shape and charge to the target, typically a key biomolecule (mostly enzyme or other protein receptor) involved in a particular step of the metabolism. Drug development is the process of bringing a new pharmaceutical to the market once a lead compound has been identified through the process of drug discovery.

Phosphonates are compounds containing a direct C-P bond and possess one or more phosphonate moieties (-PO3H2). They are mimics of naturally-occurring phosphates, and their isometric and isoelectronic analogs. This group is also generally used as a bio-isostere of carboxylate in analogues of acids, amino acids and peptides. Phosphon(in)ate groups are also active mimics of transition state of hydrolysis of amides and esters being effective transition-state inhibitors. Thus, these compounds were used for their bioactive properties (drug, pro-drug), for the design of enzyme inhibitors, for bone targeting, for the design of novel antibacterial and anticancer agents, for medical imaging, for diagnostic purposes or as phosphoantigens. On the other hand, bisphosphonates are well-known active drugs against osteoporosis, with rich chemistry and biology. These applications cover a plethora of research fields including chemistry, biology and physics.

This Research Topic focuses on all aspects of design, identification, synthesis and introduction of new potential phosphonate medicines, including novel synthetic and natural compounds. Original Research articles, Reviews and Perspectives are welcome.

We encourage contributions on the following topics (but not restricted to):
• Novel and improved synthetic methods to prepare phosphonate-based drugs and prodrugs
• Phosphonates as structural analogues
• Phosphonates as transition state analogs
• Natural phosphates as novel drug scaffolds
• Phosphonates as enzyme inhibitors and pathological stones inhibitors (e.g. kidney stones)
• Computer-aided drug design of new potential phosphonate medicines


Keywords: organophosphorus, phosphonate, drug targeting, nucleotides, prodrug


Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.

The current state of the chemical and biological sciences dictate that 5,000–10,000 chemical compounds must undergo laboratory screening for each new drug approved for use in humans. Of these, approximately 250 will enter preclinical testing, and only 5 will enter clinical testing. The overall process from discovery to marketing of a drug can take 10 to 15 years. Drug discovery includes drug design and development, and is a multifarious and expensive endeavor. Drug design is the inventive process of finding new medications based on the knowledge of a biological target. It defines the search for molecules that are complementary in shape and charge to the target, typically a key biomolecule (mostly enzyme or other protein receptor) involved in a particular step of the metabolism. Drug development is the process of bringing a new pharmaceutical to the market once a lead compound has been identified through the process of drug discovery.

Phosphonates are compounds containing a direct C-P bond and possess one or more phosphonate moieties (-PO3H2). They are mimics of naturally-occurring phosphates, and their isometric and isoelectronic analogs. This group is also generally used as a bio-isostere of carboxylate in analogues of acids, amino acids and peptides. Phosphon(in)ate groups are also active mimics of transition state of hydrolysis of amides and esters being effective transition-state inhibitors. Thus, these compounds were used for their bioactive properties (drug, pro-drug), for the design of enzyme inhibitors, for bone targeting, for the design of novel antibacterial and anticancer agents, for medical imaging, for diagnostic purposes or as phosphoantigens. On the other hand, bisphosphonates are well-known active drugs against osteoporosis, with rich chemistry and biology. These applications cover a plethora of research fields including chemistry, biology and physics.

This Research Topic focuses on all aspects of design, identification, synthesis and introduction of new potential phosphonate medicines, including novel synthetic and natural compounds. Original Research articles, Reviews and Perspectives are welcome.

We encourage contributions on the following topics (but not restricted to):
• Novel and improved synthetic methods to prepare phosphonate-based drugs and prodrugs
• Phosphonates as structural analogues
• Phosphonates as transition state analogs
• Natural phosphates as novel drug scaffolds
• Phosphonates as enzyme inhibitors and pathological stones inhibitors (e.g. kidney stones)
• Computer-aided drug design of new potential phosphonate medicines


Keywords: organophosphorus, phosphonate, drug targeting, nucleotides, prodrug


Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.

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Submission Deadlines

18 August 2020 Manuscript

Participating Journals

Manuscripts can be submitted to this Research Topic via the following journals:

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Topic Editors

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Submission Deadlines

18 August 2020 Manuscript

Participating Journals

Manuscripts can be submitted to this Research Topic via the following journals:

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