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Cyclic hexadepsipeptide compound and application thereof in preparing benign prostatic hyperplasia resistant drug

A prostatic hyperplasia, compound technology, application in the preparation of anti-benign prostatic hyperplasia drugs, cyclic hexapeptide compounds and their use in the field of preparation of α1-AR antagonists, can solve problems affecting the quality of life of patients

Inactive Publication Date: 2016-02-03
SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, according to statistics, about 60-70% of men over the age of 60 suffer from benign prostatic hyperplasia (BPH), clinically manifested as lower urinary tract symptoms such as frequent urination, urgency, nocturia, and dysuria, which seriously affects patient's quality of life

Method used

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  • Cyclic hexadepsipeptide compound and application thereof in preparing benign prostatic hyperplasia resistant drug
  • Cyclic hexadepsipeptide compound and application thereof in preparing benign prostatic hyperplasia resistant drug
  • Cyclic hexadepsipeptide compound and application thereof in preparing benign prostatic hyperplasia resistant drug

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Experimental program
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Effect test

Embodiment 1

[0018] Solid phase synthesis and structure identification of compounds 1-5 represented by formula (I)

[0019]

[0020] In formula (I), compound 1: R=Ser / S; or compound 2: R=Asp / D; or compound 3: R=Glu / E; or compound 4: R=His / H; or compound 5: R =Met / M.

[0021] One, the solid-phase synthesis of compound 1-5 as shown in formula (I)

[0022] 1. Solid phase synthesis

[0023] Using solid-phase peptide synthesis technology, N-α-Fmoc-protected amino acid is used as raw material, Fmoc-AA-2CL resin is used as carrier, and HBTU method is used for coupling. The Fmoc-AA-2CL resin (1mmol) was removed with piperidine-DMF (V:V=1:5), and the Fmoc protecting group was removed for 15 minutes. After washing with DCM and DMF, Fmoc protected amino acids (3mmol), HBTU ( 3mmol), DIEA (3mmol) for coupling, 30 minutes, after washing, the steps of removing the Fmoc protecting group-washing-coupling-rewashing are cycled until the last amino acid coupling is completed, and the synthesis of the e...

Embodiment 2

[0044] The cyclic hexapeptide compound-compound 1-5 of embodiment 1 and the same series natural cyclic hexapeptide compound 6 (c(G-W-L-dL-L-allo-Ile-N)) and compound 7 (c(G-W-L-dL-V-N) )) to α 1 -Three subtypes of AR α 1A -, α 1B - and α 1D -AR was tested for selective antagonist activity.

[0045] 1. Compound pair alpha 1 -Investigation on the Selective Inhibition of AR Subtypes

[0046] Strain cultivation and plasmid extraction: The corresponding plasmid (pGL4.29[luc2P / CRE / Hygro] was purchased from PromegaProductIDE8471, which contained the reporter gene luc2p-CRE; pGL4.74[hRluc / TK] was purchased from PromegaProductIDE6921, which contained the reporter gene hRluc -TK; EX-A0967-M29 was purchased from GeneCopoeia ProductIDA0967 containing α 1 The coding gene of A-AR; EX-Y3321-M29 was purchased from GeneCopoeiaProductIDY3321, which contains α 1 The coding gene of B-AR; EX-Y2008-M29 was purchased from GeneCopoeiaProductIDY2008, which contains α 1 D-AR coding gene) strain...

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Abstract

The invention discloses a kind of cyclic hexadepsipeptide compound and an application thereof in preparing a benign prostatic hyperplasia resistant drug. The structural formula of the cyclic hexadepsipeptide compound and a salt thereof for the drug are shown as c(G-W-L-dL-R-N) (formula (I)), wherein in the formula (I), the compound 1: R is equal to Ser / S; compound 2: R is equal to Asp / D; the compound 3: R is equal to Glu / E; the compound 4: R is equal to His / H; or the compound 5: R is equal to Met / M. The cyclic hexadepsipeptide compound has good nonselective anti-junction effect for three hypotypes of alpha1-AR, namely alpha1A-, alpha1B- and alpha1D-AR, for partial hypotypes, the effect is better than a positive reference drug prazosin, and an important significance for developing the benign prostatic hyperplasia resistant drug can be realized..

Description

Technical field: [0001] The invention belongs to the field of natural products, in particular to a class of cyclic hexapeptide compounds and their use in the preparation of α 1 -AR antagonist and its use in the preparation of anti-benign prostatic hyperplasia medicaments. Background technique: [0002] With the development of society, population aging has become an inevitable social problem. Under the population policy with Chinese characteristics, the health status of the elderly is related to the working status and quality of their children, and is related to the healthy development of society. However, according to statistics, about 60-70% of men over the age of 60 suffer from benign prostatic hyperplasia (BPH), clinically manifested as lower urinary tract symptoms such as frequent urination, urgency, nocturia, and dysuria, which seriously affects patients' quality of life. At present, the commonly used drugs for the clinical treatment of BPH are α 1 - AR blockers, 5α-...

Claims

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Application Information

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IPC IPC(8): C07K7/64A61K38/12A61P13/08
Inventor 鞠建华宋永相许芳
Owner SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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