Antiaggregating and Antithrombotic Activities of new 1, 2, 3‐Triazolecarboxamides

Abstract

Twenty five new triazolecarboxamides related to YC-1 were prepared and tested for their antiplatelet (in vitro) and antithrombotic (in vivo) activities. Five of them inhibited the aggregation of blood platelets (Born test, inducer collagen) with IC50 values between 90 and 130 microM. Nine compounds exhibited significant antithrombotic properties with an inhibition of thrombus formation between 11 and 7%. Only one compound (8c) showed both, in vitro and in vivo effects. In vitro, the most active compounds were 11c and 12d. They inhibit platelet aggregation with IC50 = 90 and 95 microM. In vivo, 10a showed the strongest inhibition of thrombus formation with 11% in arterioles (5% in venules) after a single oral dose of 60 mg/kg. With serotonin as inducer both, 11c and 12d, showed lower IC50 values namely 25 or 30 microM, respectively. Additional antiplatelet activities were found for 11c against adrenaline (IC50 = 25 microM) and for 12d against platelet activating factor (PAF) (IC50 = 15 microM) as inducer.

Synthesis and Anticonvulsant Activity of 1-Substituted-7-Benzyloxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline

“…The derivatives of triazole exhibit a variety of activities such as antitumor, 4) antiinflammatory, 5) antimicrobial, 6,7) antifugal, 8) antithrombotic, 9) antiplatelet, 10) antiviral, 11) and anticonvulsant activities. [12][13][14] In our search for new compounds with anticonvulsant activity, 6-benzyloxy-3,4-dihydro-1H-quinoline-2-one was found although its activity is low.…”

New Oxadiazole Derivatives Showing partly Antiplatelet, Antithrombotic and Serotonin Antagonistic Properties

“…After stirring for 64 h at a temperature of 30 to 40°C the mixture was filtered off. The filtrate was concentrated in vacuo at a temperature of less [9] modified)…”

“…In the row of the type 6 compounds the lipophilic biphenyl rest R 1 which already had proven to be very suitable for antiplatelet activities [9,10] was held constant (6a؊g, 6j) and R 2 was varied. Especially substituents with a basic moiety (pK B~5 ) were chosen according to former experiences with ether heterocycles [9,10]. The exception is 6f with neutral R 2 (i.e.…”

Smectic liquid crystals comprising triazole banana shaped achiral molecules: Synthesis and characterization

“…They are generally used in medicinal chemistry [15][16], organic chemistry, materials chemistry [17] and other fields, but they are rarely used in liquid crystal. In the linear molecule, a negative dielectric anisotropy can be obtained by introducing substituent group, such as cyanogroup [18], nitro [19], fluorine [20] and chlorine [21] to the side of the molecule.…”