Protein Information

Name NK 2
Synonyms BCH; TEBP; BHC; Homeobox protein NK 2 homolog A; Homeobox protein Nkx 2.1; NK 2; NKX2 1; NKX2.1…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
12372524 Blythin DJ, Chen X, Piwinski JJ, Shih NY, Shue HJ, Anthes JC, McPhail AT: Synthesis and NK (1)/NK (2) binding activities of a series of diacyl-substituted 2-arylpiperazines. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3161-5.

X-ray crystallographic analysis of the crystalline di-BOC derivative of the NK (2) active piperazine (15) showed that the 2R configuration was associated with NK (2) activity.
34(0,1,1,4) Details
15615542 Fedi V, Altamura M, Balacco G, Canfarini F, Criscuoli M, Giannotti D, Giolitti A, Giuliani S, Guidi A, Harmat NJ, Nannicini R, Pasqui F, Patacchini R, Perrotta E, Tramontana M, Triolo A, Maggi CA: Insertion of an aspartic acid moiety into cyclic pseudopeptides: synthesis and biological characterization of potent antagonists for the human Tachykinin NK-2 receptor. J Med Chem. 2004 Dec 30;47(27):6935-47.

The replacement of the succinic moiety with an aspartic acid and the functionalization of its amino group with a wide variety of substituents led to very potent and selective NK-2 antagonists.
Best results were obtained through the insertion in position 12 of an amino group with R configuration, linked by a short spacer to a saturated nitrogen heterocycle (morpholine, piperidine, or piperazine).
2(0,0,0,2) Details