Journal ArticleDOI
Cardiovascular activity of aromatic guanidine compounds.
Hughes Jl,R. C. Liu,Enkoji T +2 more
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TLDR
Preliminary mechanism studies indicated that the 3,4-dihydroxyphenylguanidines act at least partially by a direct alpha-adrenergic mechanism.Abstract:
A series of aromatic guanidines and several 1-phenylbiguanides was prepared and tested for cardiovascular (CV) effects in anesthetized dogs measuring heart rate, blood pressure, carotid artery blood flow, and myocardial force changes. The predominant CV effect at minimally effective dose was vasoconstriction unassociated with cardiac stimulation. The structure-activity relationships of the compounds were discussed comparing their structural similarities to the beta-phenylethylamines. The most potent members of the series were phenylguanidines substituted in the 3 and 4 positions on the aromatic nucleus with hydroxy or chloro groups. Preliminary mechanism studies indicated that the 3,4-dihydroxyphenylguanidines act at least partially by a direct alpha-adrenergic mechanismread more
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Synthesis and Identification of [1,3,5]Triazine-pyridine Biheteroaryl as a Novel Series of Potent Cyclin-Dependent Kinase Inhibitors
Gee-Hong Kuo,Alan Deangelis,Stuart Emanuel,Aihua Wang,Yan Zhang,Peter J. Connolly,Xin Chen,Robert H. Gruninger,Catherine A. Rugg,Angel R. Fuentes-Pesquera,Steven A. Middleton,Linda Jolliffe,William V. Murray +12 more
TL;DR: Molecular docking studies were conducted in an attempt to enhance the understanding of the observed structure-activity relationship and led to the discovery of [1,3,5]triazine-pyridine as a new series of potent CDK inhibitors.
Journal ArticleDOI
Mitochondria targeting by guanidine- and biguanidine-porphyrin photosensitizers.
TL;DR: The syntheses of three new amphiphilic porphyrin derivatives, containing a guanidine, a biguanidine, or an MLS peptide, that were designed to target the cell mitochondria showed low dark toxicity toward human carcinoma HEp2 cells.
Journal ArticleDOI
Structure−Activity Relationships for the Binding of Arylpiperazines and Arylbiguanides at 5-HT3 Serotonin Receptors
Malgorzata Dukat,Ashraf A. Abdel-Rahman,Abd M. Ismaiel,Stacy P. Ingher,Milt Teitler,Laszlo Gyermek,Richard A. Glennon +6 more
TL;DR: Although curious similarities exist between the structure-activity relationships of the arylpiperazines, arylbiguanides, and aRYlguanidines, it cannot be concluded that all three series of compounds are binding in the same manner.
Journal ArticleDOI
Arylguanidine and arylbiguanide binding at 5-HT3 serotonin receptors: A QSAR study
Richard A. Glennon,Maha Khalifa Daoud,Malgorzata Dukat,Milt Teitler,Katharine Herrick-Davis,Anil Purohit,Hasan Syed +6 more
TL;DR: For a series of monosubstituted arylguanidines, 5-HT3 receptor affinity was found generally related to the electron withdrawing nature of the substituent at the aryL 3-position and the lipophilicity of the 4-position substituents.
Journal ArticleDOI
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha(2)-adrenoceptor antagonists, 1: toward new antidepressants with heteroatomic linkers.
TL;DR: Both 2-aminoimidazoline derivatives and 18b and 26b showed antagonistic properties over alpha(2)-ARs not only in vitro [(35)S]GTPgammaS binding but also in vivo microdialysis experiments and can be considered as potential antidepressants.