Produgs of AMPA potentiators structurally related to IDRA21 : design, preparation, hydrolysis study and pharmacological evaluation

in Fundamental & Clinical Pharmacology (2004)

Effects of recently developed 6-substituted 3-bromophenyl 2-oxo-2H-1-benzopyran-3-carboxylate derivatives on HT1080 cell invasion in vitro

in Fundamental & Clinical Pharmacology (2004)

New developments on thromboxane modulators

in Mini Reviews in Medicinal Chemistry (2004), 4

Pharmacological characterization of N-tert-butyl-N’-[2-(4’-methylphenylamino)-5-nitrobenzenesulfonyl]urea (BM-573), a novel thromboxane A2 receptor antagonist and thromboxane synthase inhibitor in a rat model of arterial thrombosis and its effects on bleeding time

in Journal of Pharmacology and Experimental Therapeutics (The) (2004), 309(2), 498-505

The present study was undertaken to characterize the antiplatelet and antithrombotic effects of BM-573 [N-tert-butyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl] urea], an original combined ... [more ▼]

The present study was undertaken to characterize the antiplatelet and antithrombotic effects of BM-573 [N-tert-butyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl] urea], an original combined thromboxane receptor antagonist and thromboxane synthase inhibitor in rats, and to determine its effects on mice bleeding time. Intraperitoneal injection of a single dose of 5 mg/kg BM-573 to rats inhibited U-46619 (9,11-dideoxy-9,11-methanoepoxy-prostaglandin F-2)-induced washed platelet aggregation 30 min and 1, 2, and 4 h after drug administration with a maximum antiplatelet effect observed after 1 and 2 h. In a rat model of thrombosis induced by ferric chloride application on the abdominal aorta, BM-573 significantly reduced the thrombus weight by 92.53, 80.20, 64.75, and 18.21% at doses of 5, 2, 0.5, and 0.2 mg/kg, respectively. Time to occlusion of abdominal aorta in the BM-573-treated group (41.50+/-5.21 min) was significantly prolonged compared with the vehicle-treated rats (16.16+/-0.79 min). Like furegrelate, seratrodast, and acetylsalicylic acid, BM-573 did not affect the tail bleeding time induced by tail transection in mice compared with vehicle-treated mice. Moreover, BM-573, a close derivative of the loop diuretic torasemide, failed to induce a significant increase in diuresis in rat and did not produce a decrease in blood glucose concentration as observed with the sulfonylurea glibenclamide. In conclusion, we have demonstrated that the nitrobenzenic sulfonylurea BM-573, an original combined thromboxane receptor antagonist and thromboxane synthase inhibitor, is a potent antithrombotic agent that does not affect bleeding time. Moreover, BM-573 lost the diuretic property of torasemide and has no impact on glycemia. [less ▲]

Design and pharmacological evaluation of recently developed 6-substituted 3-bromophenyl 2-oxo-2H-1-benzopyran 3-carboxylate derivatives as putative inhibitors of cell invasion

in Fundamental & Clinical Pharmacology (2004)

New developments on thromboxane modulators

in Mini Reviews in Medicinal Chemistry (2004)

Antithrombotic activity of BM-573, a novel thromboxane modulator, in rat arterial thrombosis model, pig myocardial infarction model and its effect on bleeding time

Poster (2003, December)

Pharmacological evaluation of BM-573, a dual thromboxane A2 receptor antagonist and thromboxane synthase inhibitor, as potential anti-metastatic agent

Poster (2003, December)

Effects of recently developed 6-substituted 3-bromophenyl 2-oxo-2H-1-benzopyran-3-carboxylate derivatives on HT1080 cell invasion in vitro

Poster (2003, November 22)

Pharmacological evaluation of BM-573, a dual thromboxane A(2) receptor antagonist and thromboxane synthase inhibitor, as potential anti-metastatic agent

in Blood (2003, November 16), 102(11, Part 2), 72