By Richard V Heinzelman; American Chemical Society. Division of Medicinal Chemistry
Read or Download Annual reports in medicinal chemistry. / Volume 7 PDF
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Additional resources for Annual reports in medicinal chemistry. / Volume 7
The primary ,CH3 ~+$,~~ncs~T 7--@ om3 OH I IS\ OH &*#I.. OH OCH, I1 importance of a lipophilic binding site rather than that previously postulated for the (2-19 hydroxyl was shown by the finding that 11 is as potent (1000 times morphine in the rat tail pressure test) as etorphine (I). la 32 Sect. 1 - Engelhardt, Ed. 7 ( 0 ) - Synthesis and conformation of the 3- (111) and 4-methyl 2. 8 IVa (2 times codeine) was about three times as potent an analgesic as IIIa, but IVb, c and d surprisingly were - inactive, In the I11 series, all were active the cyclopropylmethyl analog (IIIc) about five times as active as the methyl (IIIa) analog ands without antagonist effect or physical dependence capacity in the monkey.
Wheatley, B r i t . J. , 117, 573 (1970). 4, 59 (1971). Goridis and N. H. Neff, Neuropharmacology lo, 557 (1971). B. B. Jones, C. M. B. Pare, W. J. Nicholson, K. R i c e and A. S. Stacey, Brit. Med. , 5791, (1972). W. Fuller, B. J. Warren and B. B. Molloy, Biochem. , 3 3 4 (1970). E. Costa and S. Garatthi, Eds. , 1970. J. M. van Rossum, Lnt. Rev. Neurobiology, l2, 307 (1970). Anonymous, Wall Street Journal, Jan. 29, 1971. D. X. Freedman, Children, l8, 111 (1971). E. H. Ellinwood and S. Cohen, Science, 171, 420 (1971).
59. 60. 29 Kaiser, Zirkle -' 30 2, 206 (1971). 61. G. Gardos and J. 0. Cole, Curr. Ther. , C l h . Exp. l3, 631 (1971). 62. A. H. Tang and J. D. Kirch, Rychophannacologia, 2l, 139 (1971). 63. C. F. Barfknecht, D. E. Nichols, B. Olesen and J. A. Engelbrecht, Pharmacologist 2,233 (1971). 64. B. Hach and F. , 2l, 23 (1971). 65. 0. Nieschulz, h i d . , g,1497 (1970). 66. M. Julia and J. deRosnay, Chh. , 2, 337 (1970). l, 645 (1971). 67. A. A. Siciliano and K. A. Nieforth, J. Med. , 4 68. E. J. Lien, L.