Qiao-Hong Chen
University of Alberta
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Publication
Featured researches published by Qiao-Hong Chen.
Journal of Medicinal Chemistry | 2008
Carlos A. Velázquez; Qiao-Hong Chen; Michael L. Citro; Larry K. Keefer; Edward E. Knaus
The carboxylic acid group of the anti-inflammatory (AI) drugs aspirin and indomethacin was covalently linked to the 1-(2-carboxypyrrolidin-1-yl)diazen-1-ium-1,2-diolate ion via a one-carbon methylene spacer to obtain two new hybrid prodrugs. The aspirin prodrug ( 23) was a 2.2-fold more potent AI agent than aspirin, whereas the indomethacin prodrug ( 26) was about 1.6-fold less potent than indomethacin. Prodrugs 23 and 26 slowly released nitric oxide (NO) upon dissolution in phosphate buffer at pH 7.4 (1.1 mol of NO/mol of compound after 43 h), but the rate and the extent of NO release were higher (1.9 mol of NO/mol of compound in 3 min or less) when the compounds were incubated in the presence of porcine liver esterase. In vivo ulcer index (UI) studies showed that the aspirin prodrug 23 (UI = 0.7) and indomethacin prodrug 26 (UI = 0) were substantially less ulcerogenic than the parent drugs aspirin (UI = 51) and indomethacin (UI = 64).
Bioorganic & Medicinal Chemistry | 2008
Erin M. MacKenzie; Afshin Fassihi; Asghar Davood; Qiao-Hong Chen; Gillian Rauw; Gail Rauw; Edward E. Knaus; Glen B. Baker
A group of beta-phenylethylidenehydrazines possessing a variety of substituents (Me, OMe, Cl, F, and CF(3)) at the ortho-, meta-, or para-positions of the phenyl ring, in conjunction with either a N-bis-(2-propynyl) or a N-mono-(2-propynyl) moiety, were synthesized and compared to the novel neuroprotective drug beta-phenylethylidenehydrazine (PEH) with regard to their ability to inhibit the enzymes GABA-transaminase (GABA-T) and monoamine oxidase (MAO)-A and -B in vitro in brain tissue. Two of the analogs synthesized (mono- and bis-N-propynylPEH) were also studied exvivo in rats to compare their effects to those of PEH with regard to ability to inhibit GABA-T and MAO and to change brain levels of several important amino acids. Unlike PEH, none of the new drugs inhibited GABA-T in vitro at 10 or 100 microM, and all of the drugs (including PEH) were poor inhibitors (at 10 microM) of MAO-A and -B invitro. The two analogs studied exvivo inhibited GABA-T to a lesser extent than PEH, unlike PEH that did not elevate brain levels of GABA, and inhibited MAO-A and -B more potently than PEH. Interestingly, unlike PEH, the two analogs caused marked increases in brain levels of glycine; because of the current interest in drugs that increase glycine availability in the brain as potential antipsychotic drugs, these two analogs now warrant further investigation.
Journal of Medicinal Chemistry | 2006
P.N. Praveen Rao; Qiao-Hong Chen; Edward E. Knaus
Bioorganic & Medicinal Chemistry | 2005
Qiao-Hong Chen; P.N. Praveen Rao; Edward E. Knaus
Bioorganic & Medicinal Chemistry | 2006
Anne Moreau; Qiao-Hong Chen; P.N. Praveen Rao; Edward E. Knaus
Bioorganic & Medicinal Chemistry | 2006
Raymond Anana; P.N. Praveen Rao; Qiao-Hong Chen; Edward E. Knaus
Bioorganic & Medicinal Chemistry | 2006
Qiao-Hong Chen; P.N. Praveen Rao; Edward E. Knaus
Bioorganic & Medicinal Chemistry | 2008
Khaled R.A. Abdellatif; Morshed A. Chowdhury; Ying Dong; Qiao-Hong Chen; Edward E. Knaus
Bioorganic & Medicinal Chemistry | 2007
Khaled R.A. Abdellatif; Ying Dong; Qiao-Hong Chen; Morshed A. Chowdhury; Edward E. Knaus
Bioorganic & Medicinal Chemistry Letters | 2005
P.N. Praveen Rao; Qiao-Hong Chen; Edward E. Knaus