Bioorganic & Medicinal Chemistry 

About: Bioorganic & Medicinal Chemistry is an academic journal. The journal publishes majorly in the area(s): Docking (molecular) & Structure–activity relationship. It has an ISSN identifier of 0968-0896. Over the lifetime, 15758 publication(s) have been published receiving 450851 citation(s).

Natural products in crop protection.

Abstract: The tremendous increase in crop yields associated with the 'green' revolution has been possible in part by the discovery and utilization of chemicals for pest control. However, concerns over the potential impact of pesticides on human health and the environment has led to the introduction of new pesticide registration procedures, such as the Food Quality Protection Act in the United States. These new regulations have reduced the number of synthetic pesticides available in agriculture. Therefore, the current paradigm of relying almost exclusively on chemicals for pest control may need to be reconsidered. New pesticides, including natural product-based pesticides are being discovered and developed to replace the compounds lost due to the new registration requirements. This review covers the historical use of natural products in agricultural practices, the impact of natural products on the development of new pesticides, and the future prospects for natural products-based pest management.

Molecular recognition of DNA by small molecules.

Abstract: Chemists, like artists, are able to construct new three-dimensional objects, molecules and materials that exist only in the mind of a person I became interested in creating novel molecular shapes with properties different from those found in nature shortly after arriving at Caltech in 1973 One cannot design without the brushes and paint of the craft Indeed, modern organic chemists, standing on the shoulders of the pioneering achievements of Woodward, Corey, Merrifield, and others are able to apply the power of synthetic chemistry and the logic of incremental change to the field of structure–function In early 1973, I was inspired by the work of Lehn and Cram in the field of host–guest chemistry where early studies were largely conducted in organic solvents (eg, cation–crown complexation) I decided that a pivotal path forward would be to understand in a predictive mechanistic sense how to create ensembles of weak bonds between synthetic ligands and biological macromolecules in water, the solvent of life

Nanoparticles in cellular drug delivery.

Abstract: This review highlights the properties of nanoparticles used in targeted drug delivery, including delivery to cells as well as organelle targets, some of the known pharmacokinetic properties of nanoparticles, and their typical modifications to allow for therapeutic delivery. Nanoparticles exploit biological pathways to achieve payload delivery to cellular and intracellular targets, including transport past the blood-brain barrier. As illustrative examples of their utility, the evaluation of targeted nanoparticles in the treatment of cancers and diseases of the central nervous system, such as glioblastoma multiforme, neurovascular disorders, and neurodegenerative diseases, is discussed.

Therapeutic peptides: Historical perspectives, current development trends, and future directions.

Abstract: Peptide therapeutics have played a notable role in medical practice since the advent of insulin therapy in the 1920s. Over 60 peptide drugs are approved in the United States and other major markets, and peptides continue to enter clinical development at a steady pace. Peptide drug discovery has diversified beyond its traditional focus on endogenous human peptides to include a broader range of structures identified from other natural sources or through medicinal chemistry efforts. We maintain a comprehensive dataset on peptides that have entered human clinical studies that includes over 150 peptides in active development today. Here we provide an overview of the peptide therapeutic landscape, including historical perspectives, molecular characteristics, regulatory benchmarks, and a therapeutic area breakdown.

5-Substituted-1H-tetrazoles as carboxylic acid isosteres: medicinal chemistry and synthetic methods

Abstract: 5-Substituted-1H-tetrazoles (RCN4H) are often used as metabolism-resistant isosteric replacements for carboxylic acids (RCO2H) in SAR-driven medicinal chemistry analogue syntheses. This review provides a brief summary of the medicinal chemistry of tetrazolic acids and highlights some examples of tetrazole-containing drug substances in the current literature. A survey of representative literature procedures for the preparation of 5-substituted-1H-tetrazoles, focusing on preparations from aryl and alkyl nitriles, is presented in sections by generalized synthetic methods.