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1.
J Med Chem ; 51(11): 3077-80, 2008 Jun 12.
Article in English | MEDLINE | ID: mdl-18459730

ABSTRACT

Recently, FXIIa was highlighted as an original attractive target for the development of new anticoagulant drugs with low rates of therapy-related hemorrhages. In this work, we describe the development of a new series of 3-carboxamide-coumarins that are the first potent and selective nonpeptidic inhibitors of FXIIa.


Subject(s)
Amides/chemical synthesis , Anticoagulants/chemical synthesis , Coumarins/chemical synthesis , Factor XIIa/antagonists & inhibitors , Amides/chemistry , Anticoagulants/chemistry , Coumarins/chemistry , Factor XIIa/chemistry , Structure-Activity Relationship
2.
Bioorg Med Chem Lett ; 18(6): 1855-8, 2008 Mar 15.
Article in English | MEDLINE | ID: mdl-18296049

ABSTRACT

Beta-cyclodextrin (beta-CD) was monofunctionalized into its carboxylic derivative and then conjugated to the N-side of oxytocin (OT), a nonapeptide involved in human behavior and myometrium contraction. On isolated rat myometrium, this conjugate (beta-CD-OT) partly preserves the contracting activity of OT (EC(50) = 0.40 microM vs 1.7 nM). Moreover, the contraction induced frequency is also lowered by beta-CD-OT. This novel hydrophilic targeted carrier could form a host-guest complex with prostaglandins and their derivatives used as labor inducers or with anticancer drugs used in cervix and endometrial cancer. This strategy can improve the solubility, the stability, and/or the biological activity of these drugs as well as reducing their side-effects.


Subject(s)
Myometrium/drug effects , Oxytocics/pharmacology , Oxytocin/pharmacology , Uterine Contraction/drug effects , beta-Cyclodextrins/chemistry , beta-Cyclodextrins/chemical synthesis , beta-Cyclodextrins/pharmacology , Animals , Chromatography, High Pressure Liquid , Drug Carriers , Female , Magnetic Resonance Spectroscopy , Molecular Structure , Myometrium/cytology , Oxytocin/chemical synthesis , Rats
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