Krogsgaard-Larsen

P. Krogsgaard-Larsen and H. Bungaard, eds.,M Textbook of Drug Design and Development, Harwood Academic Pubhshers, Swit2edand, 1991. 

N. Ikekawa, in H. Danielsson and. Sjovah, eds.. Steroids andBile Acids, Elsevier Science Pubhshers BV, Amsterdam, the Nethedands, 1985, pp. 199—230 C. Djerassi, in P. Krogsgaard-Larsen, S. Brogger Christensen, and H. Kofod, eds., Alfred Benpon Symposium 20 Natural Products and Drug Development, Munksgaard, Copenhagen, Denmark, 1984, pp. 164—176 N. W. Withers, in P. J. Scheuer, ed.. Marine Natural Products, Vol. V, Academic Press, Inc., New York, 1983, pp. 87—130 C. Djerassi, Pure Appl Chem. 53, 873 (1981). 

Krogsgaard-Larsen and co-workers have protected the P-keto functionality as a ketal as a modification to the traditional conditions so attack of hydroxylamine is directed towards the ester. They prepared hydroxamic acid 10 from ester 9 then cyclized with sulfuric acid to isoxazole 11, in route to 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP), a selective GABAa receptor agonist studied clinically for insomnia. 

Krogsgaard-Larsen and co-workers continued to utilize Claisen isoxazole chemistry in the preparation of GABAa receptor antagonists reported in 2000. In the synthesis of protected 3-isoxazolols 17a-f, P-oxoesters 16a-f were cyclized at -30°C followed by heating with concentrated hydrochloric acid at 80°C. 

Kubinyi H. QSAR Hanch analysis and related approaches. In Mannhold R, Krogsgaard-Larsen P, Timmerman H, editors, Methods and principles in medicinal chemistry, Vol. 1. Weinheim VCH, 1993. 

Albuquerque, E. X. Spivak, C. E. In Natural Products and Drug Development, Krogsgaard-Larsen, P. Br6gger Christensen, S. Kofod, H., Eds. Alfred Benson Symposium 20 Munksgaard, Copenhagen, 1984 pp 301-321. 

In the early 1990s, I founded the book series Methods and Principles in Medicinal Chemistry with Verlag Chemie Henk Timmerman and Povl Krogsgaard Larsen joined me on the initial board of series editors. Hugo Kubinyi followed Povl Krogsgaard Larsen after the first three volumes were released. Henk contributed... 

Copeland, R. A., and Anderson, P. S. (2001) in Textbook of Drug Design and Discovery, 3rd ed., P. Krogsgaard-Larsen, T. Liljefors, and U. Madsen, eds., Taylor and Francis, New York, pp. 328—363. Cornish-Bowden, A. (1995), Fundamentals of Enzyme Kinetics, Portland Press, London. 

Egebjerg, Schousboe, and Krogsgaard-Larsen, Eds., Glutamate and GABA Receptors and Transporters Structure, Function and Pharmacology, Taylor Francis, London, 2001. 

Krogsgaard-Larsen, P. Liljefors, T. Madsen, U. (Eds.) Textbook of Drug Design and Discovery -, Taylor Francis London, 2002. 

Stcnsbpl, T. B Madsen, U., and Krogsgaard-Larsen, P. (2002) The AMPA receptor binding site focus on agonists and competitive antagonists. Curr. Pharm. Design 8, 857-872. 

Brauner-Osbome, H., Jensen, A. A., Sheppard, P. O., O Hara, P., and Krogsgaard-Larsen, P. (1999) The agonist-binding domain of the calcium-sensing receptor is located at the amino-terminal domain. J. Biol. Chem. 274,18382-18386. 

Thomsen, C. and Ebert, B. (2002) Modulators of the GABAA receptor complex novel therapeutic aspects, in Glutamate and GABA Receptors and Transporters (Egebjerg, J., Schous-boe, A., and Krogsgaard-Larsen, P., eds.), Taylor Francis, London, pp. 407 127. 

Mortensen, M., Frplund, B., Jprgensen, A., Liljefors, T., Krogsgaard-Larsen, R, and Ebert, B. (2002) Activity of novel 4-PIOL analogues at human alpha(l)beta(2)gamma(2S) GABA(A) receptors-correlation with hydrophobicity. Eur. J. Pharmacol. 451,125-132. 

Ebert, B., Mortensen, M., Thompson, S. A., Kehler, J., Wafford, K. A., and Krogsgaard-Larsen, P. (2001) Bioisosteric determinants for subtype selectivity of ligands for het-eromeric GABA(A) receptors. Bioorg. Med. Chem. Lett. 11, 1573-1577. 

Kristiansen, U., Lambert, J. D., Falch, E and Krogsgaard-Larsen, P. (1991) Electrophysio-logical studies of the GABAA receptor ligand, 4-PIOL, on cultured hippocampal neurones. Br. J. Pharmacol. 104, 85-90. 

Bente Fralund, Anne T. Jorgensen, Tommy Liljefors, Martin Mortensen, and Povl Krogsgaard-Larsen... 

Krogsgaard-Larsen, P Brehm, L and Schaumburg, K. (1981) Muscimol, a psychoactive constituent of amanita muscaria, as a medicinal chemical model structure. Acta Chem. Scand. B 311, 0-24. 

Krogsgaard-Larsen, P Hjeds, H Curtis, D. R Lodge, D., and Johnston, G. A. R. (1979) Dihydromuscimol, thiomuscimol and related heterocyclic compounds as GABA analogues. J. Neurochem. 32,1717-1724. 

Brehm, L Frydenvang, K., Hansen, L. M., Norrby, P.-O., Krogsgaard-Larsen, P, and Lilje-fors, T. (1997) Structural features of muscimol, a potent GABAa receptor agonist. Crystal structure and quantum chemical ab initio calculations. Struct. Chem. 8,443 451. 

Frplund, B Kristiansen, U., Brehm, L., Hansen, A. B., Krogsgaard-Larsen, R, and Falch, E. (1995) Partial GABAa receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridin-3-ol (THIP).. /. Med. Chem. 38, 3287-3296. 

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