Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Abd M. Ismaiel"'
Autor:
Abd M. Ismaiel, Joseph De. Los Angeles, Jeffery Herndon, Richard A. Glennon, Nantaka Khorana, Malgorzata Dukat, Kamel Metwally, Milt Teitler
Publikováno v:
Current Topics in Medicinal Chemistry. 2:539-558
The structures of ketanserin (1) and spiperone (2) were examined in detail to determine the role of various substituent groups on 5-HT(2A) receptor affinity and selectivity. It was found that the presence of the quinazoline ring of ketanserin detract
Publikováno v:
Journal of Medicinal Chemistry. 38:1196-1202
Ketanserin (1) is a fairly selective 5-HT2 antagonist that binds both at 5-HT2A and 5-HT2C receptors. A previous structure-affinity relationship study revealed that the structure of the piperidine-containing ketanserin molecule could be rather severe
Autor:
Kathleen J. Burke Howie, Seth Y. Ablordeppey, Abd M. Ismaiel, Mahmoud B. El-Ashmawy, James B. Fischer, Richard A. Glennon
Publikováno v:
Journal of Medicinal Chemistry. 37:1214-1219
Two problems that have hampered sigma receptor research are (i) a lack of high-affinity agents and (ii) the recent identification of multiple populations of sigma receptors (i.e., sigma 1 and sigma 2 sites). Recently, several high-affinity sigma liga
Ketanserin analogs: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding
Publikováno v:
Journal of Medicinal Chemistry. 35:4903-4910
Ketanserin is the prototypic 5-HT2 serotonin antagonist; although it has been an important tool for the study of serotonin pharmacology, it has had relatively little impact on drug design because remarkably little is known about its structure-affinit
Publikováno v:
Drug Development Research. 22:25-36
As a prelude to the design of 5-HT1D agents, we systematically investigated the structure-affinity relationships for the binding of indolealkylamines and related derivatives at 5-HT1D serotonin receptors. The results of the investigation reveal that
Publikováno v:
Journal of Heterocyclic Chemistry. 27:723-726
Because of the close structural similarity between triazoloquinazolines and certain 5-membered ring mesoionic heterocycles, all of which possess antiinflammatory activity, we prepared several examples of the novel mesoionic 1,2,4-triazolo[4,3-c]quina
Publikováno v:
Journal of Heterocyclic Chemistry. 27:497-501
The synthesis and characterization of several 3-aryl-1,2,4-triazolo[4,3-c]quinazolines is described. The first step comprises the condensation of aromatic aldehydes with 2-(H or Cl)-4-hydrazinoquinazolines 2 to afford the corresponding hydrazones 3.
Publikováno v:
Journal of Medicinal Chemistry. 33:755-758
alpha-Methyl-5-hydroxytryptamine (alpha-Me-5-HT; 2) and 2-methyl-5-hydroxytryptamine (2-Me-5-HT; 3) are considered to be 5-HT2-selective and 5-HT3-selective agents, respectively. These agents were synthesized and examined at serotonin (5-HT) binding
Autor:
Seth Y. Ablordeppey, Mahmoud B. El-Ashmawy, Fisher James B, Abd M. Ismaiel, Richard A. Glennon
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(9)
An investigation of the structure-affinity relationships for the binding of thioxanthene-related structures indicates that an intact thioxanthene ring is not required for binding at sigma(1) receptors, and that with the appropriate structural modific
Autor:
Lucia Mazzocco, Ermi Fan, Milt Teitler, David K. H. Lee, Ho Law, Malgorzata Dukat, Rajender Kamboj, Myles E. Pierson, Abd M. Ismaiel, Donna Buekschkens, Richard A. Glennon
Publikováno v:
Journal of medicinal chemistry. 40(26)
Although the beta-adrenergic antagonist propranolol (1) binds at rodent 5-HT1B serotonin receptors, it displays low affinity (Ki > 10,000 nM) for its species homologue 5-HT1D beta (i.e., h5-HT1B) receptors. The structure of propranolol was systematic