Research Medicinal Chemistry

This work was carried out in Medicinal Chemistry Research, Pharmacia, Kalamazoo MI 49001. Author s present address Eli Lilly Corporation, Lilly Corporate Center, Drop Code 1523, Indianapolis, IN 46285... 

ArifJM, Kunhi M, Siddiqui YM, El Sayed KA, Orabi KY, Al-HazzaniA, Al-Ahdal MN, Al-Khodairy FM, Role of intermediary biomarkers in determining the anticancer efficacy of marine compounds, Medicinal Chemistry Research 13 553-562, 2004. 

The potential utility of peptides as therapeutic agents with clinical applications is limited as a consequence of intrinsic peptide properties such as metabolic instability or poor transmembrane mobility. Hence, the design and synthesis of meta-bolically stable peptide analogs that can either mimic or block the bioactivity of natural peptides or enzymes is an important area of medicinal chemistry research. Numerous structural modifications to peptides have been examined in pursuit of molecules with more desirable properties [1-3]. These modified structures, peptidomimetics, are nonpeptide molecules that imitate the desired properties of the natural substances. 

Small-molecule inhibitors of caspases would have obvious use as therapeutics. The current medicinal chemistry research literature is rich in studies attempting to achieve this important design goal. In early work, both reversible and irreversible peptide-based inhibitors of various caspases have been developed. Peptidomimetic ketones were also devised for example, acyloxymethyl ketones were designed and developed as potent, time-dependent irreversible caspase inhibitors. 

Masanori Kawasaki, Medicinal Chemistry Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, 17-85, Jusohon-machi 2-chome, Yodogawa-ku, Osaka 532-8686, Japan... 

In several papers the Kunos group has reported observations that may represent a starting point for novel medicinal chemistry research in this area [167, 168], Anandamide (i.v. bolus 4 mg/kg) caused a triphasic blood pressure response, brief hypotension, followed by a transient pressor and then a prolonged depressor phase. The hypotensive effect was not initiated in the CNS, but was due to a presynaptic action that inhibited norepinephrine release from sympathetic nerve terminals in the periphery (heart and vasculature). The inhibitory effect (but not the pressor effect) was antagonized by SR141716A, indicating that this peripheral action was mediated by CB receptors. 

Quinacrine (162) is an obvious embodiment of the principle outlined above as a derivative of both quinine and 9-aminoacridine it combined a known antimalarial with a known antimicrobial. The result was a useful, relatively nontoxic antimalarial, although it stained the skin and eyeballs yellow (216).De-spite this side effect and a high incidence of gastrointestinal disturbance, quinacrine was widely used during World War II by European troops in East Asia. The availability of the results of medicinal chemistry research to both sides in wartime is a curious feature of antimalarial development, highlighted below. 

Medicinal Chemistry Research. Cambridge, MA Birkhauser Boston. ISSN 1054-2523. 

H.-J. Bohm and M. Stahl. Rapid empirical scoring functions in virtual screening applications. Medicinal Chemistry Research, 9 445-462, 1999. 

Medicinal Chemistry Research, H. Lundbeck A/S2500 Valby, Denmark F.S. Menniti (M)... 

Cristin Hagaman Department of Pharmacology, Alanex Corporation, 3550 General Atomics Court, San Diego, CA 92121, USA Dennis Heyer Glaxo Wellcome, Department of Medicinal Chemistry, Research Triangle Park, NC 27709, USA... 

Due to its psychotropic properties, Cannabis sativa was one of the first plants to be used by man, both in social-religious rites and in medicine [1-3]. In ancient times, the distinction between use in religious ceremonies and medical use was blurred. Later, in most countries, the ceremonial rites associated with Cannabis were forgotten or discarded, but the medical use continued for many centuries. In various parts of the world, Cannabis was used in a very wide range of medical conditions. This is not surprising, as the placebo effects of drugs with psychotropic action are particularly strong. However, many of the actions produced by Cannabis are undoubtedly distinct from the placebo effect and in recent years some have been confirmed in animals and in man. In the present survey, we shall try to compare past use with modem data, to present an overview of modem use and developments and to predict future pathways in medicinal chemistry research in this area. 

Medicinal chemistry research also takes place in three of the National Institutes of Health (NIH). It s a great place to work at the interface between chemistry and biology, said Dr. Kenneth Kirk, Acting Chief of the Laboratory of Bioorganic Chemistry. His institute, which is the National Institute of Diabetes and Digestive Kidney Diseases, and two others employ 20 to 30 organic chemists in tenured research jobs. The other two are the National Cancer Institute (NCI), which operates the Laboratory of Medicinal Chemistry, and the National Heart, Lung, and Blood Institute. 

Expanding the envelope of structure-based drug design using chemical libraries application to small-molecule inhibitors of thrombin. Medicinal Chemistry Research, 8, 244-260. 

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