Treatment of infectious diseases

A disease, anti-infective agent technology, applied in the field of chemosensitizing compounds, can solve problems without mentioning anti-infection or anti-drug resistance activity

Inactive Publication Date: 2007-06-06
BKG PHARMA APS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But no mention of any anti-infection or anti-resistance activity

Method used

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  • Treatment of infectious diseases
  • Treatment of infectious diseases
  • Treatment of infectious diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0227] The influence of embodiment 1-modification promethazine

[0228] Table 1 shows that with different R 1 , R 2 , R 7 and R 8 Structures, MIC values ​​and DR ratios of a series of promethazine derivatives with substituents.

[0229] The anti-infective agent used was ciprofloxacin, and the bacterial strain was Escherichia coli LN 3164.

[0230] Chemosensitizing compounds (promethazine and its derivatives) have the following general structures:

[0231]

[0232] R 1

R 2

R 7

R 8

name

Mic

(μg / ml)

DR ratio

h

Cl

h

h

h

h

h

h

h

Cl

Cl

Cl

S-CH 3

CF 3

h

h

h

Oh

Oh

h

h

h

h

h

h

Oh

h

h

promethazine

1-Chlorpromazine

Chlorpromazine

7-Hydroxychlorpromazine

7,8-Dihydroxychlorpromazine

Methiopromazine

Triflupromazine

64

64

32

1...

Embodiment 2

[0246] Example 2 - Effect of Stereochemistry

[0247] name

Mic

(μg / ml)

DR ratio

trans-flupenthixol

cis-flupenthixol

trans-clopenthixol

32

32

16

64

32

128

[0248] Table 4

[0249] The above results indicate that stereoisomeric configuration is necessary for optimal anti-DR activity. For example, trans-flupenthixol is a more potent anti-DR agent than cis-flupenthixol, which is the most potent anti-DR agent. Thus, the orientation of the side chain amines relative to the tricyclic core appears to be an important determinant of anti-DR activity.

Embodiment 3

[0250] Example 3 - Effect of Hydrophobicity

[0251] To determine whether the differences in anti-DR potency among side chain-altered chemosensitizer compounds were also due to changes in overall hydrophobicity, the octanol:buffer partition coefficients for each drug in Tables 1, 2, 3, and 4 were compared with their The DR ratios were compared. No statistically significant correlation (P > 0.5) was found between hydrophobicity and anti-DR activity (data not shown).

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PUM

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Abstract

The present invention is directed to the use of chemosensitising compounds, in particular thioxanthene derivatives and phenothiazine derivatives, for treatment of infectious diseases in combination with an anti-infective agent. The invention furthermore relates to compositions comprising said chemosensitising compounds and anti-infective agents.

Description

field of invention [0001] The present invention relates to the use of chemosensitizing compounds, especially thioxanthene derivatives and phenothiazine derivatives, in combination with anti-infective agents for the treatment of infectious diseases. Background of the invention [0002] Resistance to chemotherapy is a common clinical problem in patients with infectious diseases. During the treatment of infections, drug targeting of prokaryotic or eukaryotic microbial cells is often found to be resistant to multiple drugs with different structures and functions. This phenomenon is known as multidrug resistance (MDR). Organisms from bacteria to humans possess transmembrane transporters that enable them to resist toxic compounds. Based on their biological significance, the structures and functions of prokaryotic and eukaryotic multidrug transporters are very similar. In addition, other types of important resistance mechanisms may co-operate with efflux pumps, resulting in high...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61P31/00A61P33/00A61K31/5415
CPCA61K45/06A61K31/352A61P31/00A61P31/04A61P31/12A61P33/00A61P43/00A61K2300/00
Inventor K·G·比吉特
Owner BKG PHARMA APS
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