Protein Information

Name thrombin
Synonyms Coagulation factor II; Coagulation factor II variant; F2; F2 protein; F2 protein precursor; Factor II; PT; Prothrombin…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
15189031 Alexopoulos K, Fatseas P, Melissari E, Vlahakos D, Roumelioti P, Mavromoustakos T, Mihailescu S, Paredes-Carbajal MC, Mascher D, Matsoukas J: Design and synthesis of novel biologically active thrombin receptor non-peptide mimetics based on the pharmacophoric cluster Phe/Arg/NH2 of the Ser42-Phe-Leu-Leu-Arg46 motif sequence: platelet aggregation and relaxant activities. J Med Chem. 2004 Jun 17;47(13):3338-52.

The identification of the thrombin receptor has promoted the interest for the development of new therapeutic agents capable of selectively inhibiting unwanted biological effects of thrombin on various cell types.
N-(6-Guanidohexanoyl)-N'-(phenylacetyl) piperazine (1), N-(phenylacetyl)-4-(6-guanidohexanoylamidomethyl) piperidine (2), and N-(phenylacetyl)-3-(6-guanidohexanoylamido) pyrrolidine (3) (group A) carry the two pharmacophoric side chains of Phe and Arg residues incorporated on three different templates (piperazine, 4-aminomethylpiperidine, and 3-aminopyrrolidine).
3(0,0,0,3) Details
11824472 Maragoudakis ME, Kraniti N, Giannopoulou E, Alexopoulos K, Matsoukas J: Modulation of angiogenesis and progelatinase a by thrombin receptor mimetics and antagonists. Endothelium. 2001;8(3):195-205.

FPR and the piperazine derivatives caused suppression of angiogenesis and in combination with thrombin antagonized its angiogenic effect.
85(1,1,1,5) Details
16390138 Radi AE, Acero Sanchez JL, Baldrich E, O'Sullivan CK: Reagentless, reusable, ultrasensitive electrochemical molecular beacon aptasensor. J Am Chem Soc. 2006 Jan 11;128(1):117-24.

A bifunctional derivative of the thrombin-binding aptamer with a redox-active Fc moiety and a thiol group at the termini of the aptamer strand was synthesized.
The modified electrode showed a voltammetric signal due to a one-step redox reaction of the surface-confined ferrocenyl moiety of the aptamer immobilized on the electrode surface in 10 mM N-(2-hydroxyethyl) piperazine-N'-2-ethanesulfonic acid (HEPES) buffer of pH 8.0.
4(0,0,0,4) Details
11498991 Zhu FM, Wen ZB, He XF, Li JC, He SL: [Expression of tissue factor of astrocytes and its signal transductional pathways]. Sheng Li Xue Bao. 1999 Jun;51(3):291-6.

The aim of this study was to observe the expression of tissue factor (TF) of astrocytes in basic culture medium and under the condition stimulated by thrombin and to explore the relevant signal transduction pathways.
The results showed that 4-bromo calcium ionophore (A23187) and phorbol 12-myristate 13-acetate (PMA) enhanced significantly the TF expression of astrocytes, but the expression was decreased markedly by trifluoperazine (TFP) and 1-(5-isoquinolinyl sulfonyl)-3-methyl-piperazine (H7) in the basic medium.
3(0,0,0,3) Details
15456260 Haginoya N, Kobayashi S, Komoriya S, Yoshino T, Suzuki M, Shimada T, Watanabe K, Hirokawa Y, Furugori T, Nagahara T: Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo [5,4-c] pyridine as S4 binding element. J Med Chem. 2004 Oct 7;47(21):5167-82.


Among this series, 5-methyl-4,5,6,7-tetrahydrothiazolo [5,4-c] pyridine type 61 displayed orally potent anti-fXa activity and evident prolongation of prothrombin time (PT) with the moderate bioavailability in rats.
1(0,0,0,1) Details