Synthesis, pharmacology, and molecular modeling studies of semirigid, nicotinic agonists

JA Waters, CE Spivak, M Hermsmeier…

Index: Waters; Spivak; Hermsmeier; Yadav; Liang; Gund Journal of Medicinal Chemistry, 1988 , vol. 31, # 3 p. 545 - 554

Full Text: HTML

Citation Number: 36

Abstract

Eight nicotinic agonists were synthesized, and their potencies were estimated by contracture of the frog rectus abdominis muscle. The most potent, l-methyl-4-acetyl-l, 2, 3, 6- tetrahydropyridine methiodide (3b), 50 times as potent as carbamylcholine, served as a template for the rest. Although all of the agonists could easily conform to the putative nicotinic pharmacophore, their potencies spanned a nearly 10 000-fold range. This ...

Related Articles:

Acetylenic aminoalcohols VIII. 3, 3-Diphenyl-3-hydroxypropynylpiperidines

[Kuznetsov, S. G.; Libman, N. M.; Gorchakov, V. S.; Golikov, S. N.; Zatsepin, E. P. Pharmaceutical Chemistry Journal, 1984 , vol. 18, # 4 p. 253 - 258 Khimiko-Farmatsevticheskii Zhurnal, 1984 , vol. 18, # 4 p. 435 - 440]

Acetylenic aminoalcohols VIII. 3, 3-Diphenyl-3-hydroxypropynylpiperidines

[Kuznetsov, S. G.; Libman, N. M.; Gorchakov, V. S.; Golikov, S. N.; Zatsepin, E. P. Pharmaceutical Chemistry Journal, 1984 , vol. 18, # 4 p. 253 - 258 Khimiko-Farmatsevticheskii Zhurnal, 1984 , vol. 18, # 4 p. 435 - 440]

Acetylenic aminoalcohols VIII. 3, 3-Diphenyl-3-hydroxypropynylpiperidines

[Kuznetsov, S. G.; Libman, N. M.; Gorchakov, V. S.; Golikov, S. N.; Zatsepin, E. P. Pharmaceutical Chemistry Journal, 1984 , vol. 18, # 4 p. 253 - 258 Khimiko-Farmatsevticheskii Zhurnal, 1984 , vol. 18, # 4 p. 435 - 440]

More Articles...