Anticonvulsant Activities of Certain Thiazolidones and Hydantoins as Determined by Electric Shock Procedures in Cats, Rats and Mice

QSAR studies on drugs acting at the central nervous system

“…For a series of enkephalin derivatives of general structure H-Tyr-D-Ala-Gly-X-Y-NH2, where X and Y are variable amino acid residues, the opiate receptor binding affinity was found to be related with hydrophobic, electronic, and steric constants of well-defined X and Y fragments. 149 For potencies to depress the contractions of electrically stimulated guinea pig ileum (gpi) and mouse vas deferens (mvd) preparations, the correlations obtained were149 log (1/Ogpj = 8.103 -0.411(±0.13)UX + tty) -0.694(±0.13)SX + 0.146(±0.05)(ox + vY) (98) n = 12, r = 0.979, s = 0.128, F = 62.8 log (1/C)mvd = 9.685 -0.667(±0.07)(irx + tty) -0.629(±0.04)SX + 0.076(±0.03)(i;x + uY) (99) n = 8, r = 0.998, s = 0.049, F = 845 log (1/Ogpi = 8.186 -0.382(±0.18)(ttx + tty) -0.659(±0.11)SX + 0.129(±0.08)(ux + uY) (100) n = 8, r = 0.992, s = 0.134, F = 90.8 where irx and irY refer to the hydrophobic constants of the side chains (R) of X and Y, respectively, and were obtained by the equation 7t(R) = log P(amino acid) -log P(glycine) (101) and Sx refers to the electronic parameter of the side chain of X, defined as S = pKa(RCOOH) -PKa(HCOOH) (102) The steric parameter v for the side chain was calculated from its van der Waals volume, V, as…”

QSAR studies on drugs acting at the central nervous system

“…For a series of enkephalin derivatives of general structure H-Tyr-D-Ala-Gly-X-Y-NH2, where X and Y are variable amino acid residues, the opiate receptor binding affinity was found to be related with hydrophobic, electronic, and steric constants of well-defined X and Y fragments. 149 For potencies to depress the contractions of electrically stimulated guinea pig ileum (gpi) and mouse vas deferens (mvd) preparations, the correlations obtained were149 log (1/Ogpj = 8.103 -0.411(±0.13)UX + tty) -0.694(±0.13)SX + 0.146(±0.05)(ox + vY) (98) n = 12, r = 0.979, s = 0.128, F = 62.8 log (1/C)mvd = 9.685 -0.667(±0.07)(irx + tty) -0.629(±0.04)SX + 0.076(±0.03)(i;x + uY) (99) n = 8, r = 0.998, s = 0.049, F = 845 log (1/Ogpi = 8.186 -0.382(±0.18)(ttx + tty) -0.659(±0.11)SX + 0.129(±0.08)(ux + uY) (100) n = 8, r = 0.992, s = 0.134, F = 90.8 where irx and irY refer to the hydrophobic constants of the side chains (R) of X and Y, respectively, and were obtained by the equation 7t(R) = log P(amino acid) -log P(glycine) (101) and Sx refers to the electronic parameter of the side chain of X, defined as S = pKa(RCOOH) -PKa(HCOOH) (102) The steric parameter v for the side chain was calculated from its van der Waals volume, V, as…”

QSAR studies on drugs acting at the central nervous system

“…For a series of enkephalin derivatives of general structure H-Tyr-D-Ala-Gly-X-Y-NH2, where X and Y are variable amino acid residues, the opiate receptor binding affinity was found to be related with hydrophobic, electronic, and steric constants of well-defined X and Y fragments. 149 For potencies to depress the contractions of electrically stimulated guinea pig ileum (gpi) and mouse vas deferens (mvd) preparations, the correlations obtained were149 log (1/Ogpj = 8.103 -0.411(±0.13)UX + tty) -0.694(±0.13)SX + 0.146(±0.05)(ox + vY) (98) n = 12, r = 0.979, s = 0.128, F = 62.8 log (1/C)mvd = 9.685 -0.667(±0.07)(irx + tty) -0.629(±0.04)SX + 0.076(±0.03)(i;x + uY) (99) n = 8, r = 0.998, s = 0.049, F = 845 log (1/Ogpi = 8.186 -0.382(±0.18)(ttx + tty) -0.659(±0.11)SX + 0.129(±0.08)(ux + uY) (100) n = 8, r = 0.992, s = 0.134, F = 90.8 where irx and irY refer to the hydrophobic constants of the side chains (R) of X and Y, respectively, and were obtained by the equation 7t(R) = log P(amino acid) -log P(glycine) (101) and Sx refers to the electronic parameter of the side chain of X, defined as S = pKa(RCOOH) -PKa(HCOOH) (102) The steric parameter v for the side chain was calculated from its van der Waals volume, V, as…”

QSAR studies on drugs acting at the central nervous system

“…For a series of enkephalin derivatives of general structure H-Tyr-D-Ala-Gly-X-Y-NH2, where X and Y are variable amino acid residues, the opiate receptor binding affinity was found to be related with hydrophobic, electronic, and steric constants of well-defined X and Y fragments. 149 For potencies to depress the contractions of electrically stimulated guinea pig ileum (gpi) and mouse vas deferens (mvd) preparations, the correlations obtained were149 log (1/Ogpj = 8.103 -0.411(±0.13)UX + tty) -0.694(±0.13)SX + 0.146(±0.05)(ox + vY) (98) n = 12, r = 0.979, s = 0.128, F = 62.8 log (1/C)mvd = 9.685 -0.667(±0.07)(irx + tty) -0.629(±0.04)SX + 0.076(±0.03)(i;x + uY) (99) n = 8, r = 0.998, s = 0.049, F = 845 log (1/Ogpi = 8.186 -0.382(±0.18)(ttx + tty) -0.659(±0.11)SX + 0.129(±0.08)(ux + uY) (100) n = 8, r = 0.992, s = 0.134, F = 90.8 where irx and irY refer to the hydrophobic constants of the side chains (R) of X and Y, respectively, and were obtained by the equation 7t(R) = log P(amino acid) -log P(glycine) (101) and Sx refers to the electronic parameter of the side chain of X, defined as S = pKa(RCOOH) -PKa(HCOOH) (102) The steric parameter v for the side chain was calculated from its van der Waals volume, V, as…”