Reference

Preparation of tetrahydroisoquinolinylcarbonyl-containing peptides as bradykinin antagonists

Preparation of tetrahydroisoquinolinylcarbonyl-containing peptides as bradykinin antagonists. Breipohl, Gerhard; Henke, Stephan; Knolle, Jochen; Schoelkens, Bernward; Hock, Franz (Hoechst A.-G., Germany). Ger. Offen. DE 4013270 A1 31 Oct 1991, 13 pp. (Germany). CODEN: GWXXBX. CLASS: ICM: C07K007-06. ICS: C07K007-02; C07K001-04; A61K037-02. APPLICATION: DE 90-4013270 26 Apr 1990. DOCUMENT TYPE: Patent CA Section: 34 (Amino Acids, Peptides, and Proteins) Section cross-reference(s): 1 R1-X1-X2-X3-X4-X5-D-Ti-X6-X7-X8-R2 [R1 = H, (substituted) alkyl, alkanoyl, alkoxycarbonyl, alkylsulfonyl, cycloalkyl, carbamoyl, aminomethylcarbamoyl, etc.; R2 = OH, NH2, NHEt; X1 = (side chain substituted) basic D- or L-amino acid residue; X2 = X9-X9-Gly, X9-NH-(CH2)nCO; X3 = neutral, acid, or basic aliph. or alicyclic amino acid residue; X4, X7 = bond (side chain substituted) neutral, acidic, or basic aliph. or arom. amino acid residue; X5 = NH-(CH2)m-CO, bond; X6 = X9, bond X8 = X4, NH-(CH2)n-; X9 = NR4CHR5CO; R4R5 - atoms to complete a mono-, bi-, or tricyclic ring system; m = 1-4; n = 2-8; Tic = Q1], were prepd. Thus, H-D-Arg-Arg-Hyp-Pro-Gly-Leu-Ser-D-Tic-Oic-Arg-OH (Hyp-hydroxyprpolyl, Oic = cis-endo-octahydroindole-2-carbonyl) (I) was prepd. using fluoromethylmethoxycarbonyl-protected amino acids using benzyloxybenzyl alc. 130309-37-4 and 139113-82-9 which are cas registry numbers of substances are two of reagents here. resin. I inhibited bradykinin-induced contraction of guinea pig arterial pulmonalis strips with IC50 = 5.9 ′ 10-9 M. .