Medicinal chemistry, and

Kubinyi H 1995. The Quantitative Analysis of Structure-Activity Relationships. In Wolff M E (Editor) Burger s Medicinal Chemistry and Drug Discovery. 5th Edition, Volume 1. New York, John Wiley Sons, pp. 497-571. 

A meaningful dialogue between chemists and pharmacologists is the single most important element of the drug discovery process. The necessary link between medicinal chemistry and pharmacology has been elucidated by Paton [2] ... 

Department of Medicinal Chemistry and Pharmacology, Northeastern University, Boston, Massachusetts 02115. 

Benzothiophenes have always been of interest for medicinal chemistry and can be found in a number of marketed drugs such as Sertaconazole (Gineder-mofix), Zileuton (Leutrol) and Raloxifene (Evista). The classical synthesis of benzo thiophenes starts from thiophenols, reacting with bromoacetaldehyde dimethyl acetal, followed by cycUzation using strong acid. An alternative and more convenient route was also described starting from benzaldehydes which... 

Acknowledgements. We are grateful to the US-Israel Binational Science Foundation, to the Marcus Center for Pharmaceutical and Medicinal Chemistry and to the Research Authority at Bar-Ilan University for support of this work. 

Muegge I, Enyedy I. Docking and scoring. In Tollenaere J, de Winter H, Langenaeker W, Bultinck P, editors. Computational medicinal chemistry and drug discovery. New York Marcel Dekker. 2004. p. 405-36. 

Chebib, M and Johnston, GA (2000) GABA-Activated ligand gated ion channels medicinal chemistry and molecular biology. J. Med. Chem. 43 1427-1447. 

The solubility of chemicals, drugs or pollutants in water (S ), in octanol (S ), their saturation concentration in air Qii), as well as their partitioning in the corresponding two-phase systems [octanol-water (P /w = Q/Cw), air-water (Pair/w = C IC ) and air-octanol (Paij/ = C /Co)] are important physicochemical parameters in medicinal chemistry and in environmental research. The following correlahons of those properties with HYBOT descriptors have been published recently [54—58] ... 

Nasal, A., Siluk, D., Kaliszan, A. Chromatographic retention parameters in medicinal chemistry and molecular pharmacology. Curr. Med. Chem. 2003, 10, 381 26. 

Lipophilicity is the measure of the partitioning of a compound between a lipidic and an aqueous phase [1]. The terms lipophilicity and hydrophobicity are often used inconsistently in the literature. Lipophilicity encodes most of the intramolecular forces that can take place between a solute and a solvent. Hydrophobicity is a consequence of attractive forces between nonpolar groups and thereby is a component of lipophilicity [2]. Lipophilicity is one of the most informative physicochemical properties in medicinal chemistry and since long successfully used in quantitative structure-activity relationship (QSAR) studies. Its... 

A quite comprehensive section concerns Lipophilicity, one of the most informative physicochemical properties in medicinal chemistry and since long successfully used in QSAR studies. 

A large number of DNA-alkylating agents are known and we will not attempt a comprehensive survey here. A number of excellent reviews provide an overview of this area. " Here we will review DNA alkylation by three types of reactive intermediates that are important in medicinal chemistry and toxicology— episulfonium ions, aziridinium ions, and carbocations. 

Judy L. Bolton, Department of Medicinal Chemistry and Pharmacognosy (M/C 781), College of Pharmacy, University of Illinois at Chicago, 833 S. Wood Street, Chicago, IL 60612-7231, USA... 

Multhauf, Robert P. Medicinal chemistry and "the Paracelsians". Bull Hist Med 24 (1954). 

Today, multi-parallel synthesis lies at the forefront of organic and medicinal chemistry, and plays a major role in lead discovery and lead optimization programs in the pharmaceutical industry. The first solid-phase domino reactions were developed by Tietze and coworkers [6] using a domino Knoevenagel/hetero-Diels-Alder and a domino Knoevenagel/ene protocol. Reaction of solid-phase bound 1,3-dicarbonyl compounds such as 10-22 with aldehydes and enol ethers in the presence of piperidinium acetate led to the 1-oxa-1,3-butadiene 10-23, which underwent an intermolecular hetero-Diels-Alder reaction with the enol ethers to give the resin-bound products 10-24. Solvolysis with NaOMe afforded the desired dihydro-pyranes, 10-25 with over 90 % purity. Ene reactions have also been performed in a similar manner [7]. 

Filler, R., Kobayashi, Y., and Yagupolskii, L. M., Editors (1993). Organofluorine compounds in medicinal chemistry and biomedical applications. Stud. Org. Chem. (Amst.) 48. 

This review chapter focuses on the syntheses and reactions of these 5-membered heterocyclic ring systems containing nitrogen and sulfur (or selenium) (reported during 2006). The importance of these 71-rich heterocycles in medicinal chemistry and natural products is also covered. 

Wadhwani P, Strandherg E (2009) Structure analysis of membrane-active peptides using 19F-labeled amino acids and solid-state NMR. In Ojima I (ed) Fluorine in medicinal chemistry and chemical biology. Wiley, Chichester, pp 463-493... 

Solid-supported technologies are already well established methods in medicinal chemistry and automated synthesis. Over the last couple of years new trends have evolved in this field which are of utmost importance as they have the potential to revolutionize the way chemical synthesis especially for library production is performed. Microchip-based synthesis technologies and multistep sequences with solid-supported catalysts or reagents in flow-through systems are only two spectacular examples. A new approach is the use of solid-supported systems for the scale-up of chemical reactions thereby enabling the rapid and smooth transition from discovery to development units. 

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