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Application of thiadiazolidinedione compound in treatment of pathogenic infection

A technology of thiadiazolidines and compounds, applied in the field of design medicinal chemistry, can solve the problem of lack of bacterial biofilm inhibitors

Pending Publication Date: 2021-12-24
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In summary, this area still lacks a kind of efficient bacterial biofilm inhibitor

Method used

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  • Application of thiadiazolidinedione compound in treatment of pathogenic infection
  • Application of thiadiazolidinedione compound in treatment of pathogenic infection
  • Application of thiadiazolidinedione compound in treatment of pathogenic infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Example 1 4-(2-Hydroxybenzyl)-2-(1-naphthyl)-1,2,4-thiadiazole-3,5-dione

[0095]

[0096] white solid, the yield is 14.6%, 1 H NMR (400MHz, DMSO) δ9.78(s, 1H), 8.10(t, J=7.2Hz, 2H), 7.93(d, J=7.6Hz, 1H), 7.80(d, J=7.3Hz, 1H ),7.77–7.55(m,3H),7.13(d,J=7.3Hz,2H),6.85(dd,J=15.4,7.6Hz,2H),4.86(s,2H).

Embodiment 2

[0097] Example 2 4-(3-Hydroxybenzyl)-2-(1-naphthyl)-1,2,4-thiadiazole-3,5-dione

[0098]

[0099] White solid, yield is 5.0%, 1 H NMR (400MHz, DMSO) δ9.54 (s, 1H), 8.10 (t, J = 8.2Hz, 2H), 7.98–7.84 (m, 1H), 7.79 (d, J = 7.1Hz, 1H), 7.74 –7.51(m,3H),7.19(t,J=8.0Hz,1H),6.82(d,J=6.5Hz,2H),6.73(d,J=8.8Hz,1H),4.81(s,2H) .

Embodiment 3

[0100] Example 3 4-(4-Hydroxybenzyl)-2-(1-naphthyl)-1,2,4-thiadiazole-3,5-dione

[0101]

[0102] White solid, the yield is 18.4%, 1 H NMR (400MHz, DMSO) δ9.51(s, 1H), 8.09(dd, J=10.0, 5.9Hz, 2H), 7.85(dd, J=6.1, 3.5Hz, 1H), 7.77(d, J= 7.0Hz, 1H), 7.69–7.57(m, 3H), 7.23(d, J=8.5Hz, 2H), 6.78(d, J=8.5Hz, 2H), 4.77(s, 2H).

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Abstract

The invention discloses an application of a thiadiazolidinedione compound in the treatment of pathogenic infection. Specifically, the invention relates to application of the thiadiazolidinedione compound or pharmaceutically acceptable salt or hydrate thereof in the aspects of bacteriostasis and sterilization.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, and specifically relates to a thiadiazolidinedione-based compound or a pharmaceutically acceptable salt thereof, as well as its preparation method and application. The thiadiazolidinedione-based compound can be used to treat infections, such as staphylococcus and methicillin-resistant staphylococcus infections, so it may be used in preventive medicines for bacterial infections. Background technique [0002] Since Fleming discovered penicillin in 1928, the discovery and clinical use of antibiotics have extended the average life expectancy by 10-15 years, which is a great invention in the history of human medicine. The commonly used clinical antibiotics include β-lactams, aminoglycosides, macrolides, lincomycins, polypeptides, quinolones, sulfonamides, etc. Its mechanism of action mainly includes inhibiting the synthesis of nucleic acid, inhibiting the synthesis of protein, inhibiting the synthe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/433A61P31/04
CPCA61K31/433A61P31/04
Inventor 杨财广张涛关向娜董泽
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI