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Download Analogue-based Drug Discovery II, Volume 2 by János Fischer, C. Robin Ganellin PDF

By János Fischer, C. Robin Ganellin

Born out of a undertaking of the IUPAC's committee on Medicinal Chemistry and Drug improvement, this reference addresses earlier and present concepts for profitable drug analog improvement, extending the formerly released quantity via 9 new analog sessions and 8 case experiences. Like its precursor, this quantity additionally encompasses a basic part discussing universally acceptable innovations for analog discovery and improvement. Spanning quite a lot of healing fields and chemical sessions, the 2 volumes jointly represent the 1st systematic method of drug analog development.Of curiosity to nearly each researcher operating in drug discovery and pharmaceutical chemistry.

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Antimicrob. , 42, 3218–3224. A. (1995) Crystal structure of HIV-1 protease in complex with VX-478, a potent and orally bioavailable inhibitor of the enzyme. J. Am. Chem. , 117, 1181–1182. , and Buthod, J. (1998) Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-[(hydroxyethyl)amino] sulfonamide isostere. Bioorg. Med. Chem. , 8, 687–690. L. (2005) Overriding imatinib resistance with novel Abl kinase inhibitor. Science, 305, 399–401. G. (2006) Nilotinib in imatinib-resistant CML and philadelphia chromosome-positive ALL.

Despite its extensive use, the mechanism of action of paracetamol remained unknown. It can be supposed that it has a primarily CNS activity. In a recent study, Hoegestaett et al. 2) in the CNS [7]. The biological significance of this route was confirmed by Ottani et al. 2 N-Arachidonoyl-phenolamine (AM404). who showed that the effect of paracetamol in pain models is prevented by cannabinoid receptor antagonists [8]. , paracetamol is a selective cyclooxygenase-2 (COX-2) inhibitor in man [9]; however, paracetamol has no significant anti-inflammatory activity.

Parker), McGraw-Hill, New York. B. (2004) The Organic Chemistry of Drug Design and Drug Action, 2nd edn, Elsevier/Academic Press, p. 273. Erika M. , Gyömro˝i út 19/21, 1103 Budapest, Hungary Erika M. Alapi was born in Pasztó, Hungary, in 1974. She received her MSc degree in chemistry at the Faculty of Science of E€otv€os Lorand University in Budapest. She is working as a medicinal chemist in the field of CNS and preparing her PhD thesis “Optimizing Therapy by Analogues” under the supervision of Professor Janos Fischer at Gedeon Richter Pharmaceutical Plc.

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