3‑Benzoyl‑5,7‑diphenyl‑5h‑thiazolo[3,2‑a]pyrimidine derivatives and their applications

A technology based on benzoyl and diphenyl groups, applied in the field of preparation of antibacterial drugs, can solve problems such as the crisis of effective clinical application of antibacterial drugs

Inactive Publication Date: 2017-01-25
SHIJIAZHUANG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The emergence of these drug-resistant strains puts the effective clinical use of existing antibacterial drugs in crisis

Method used

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  • 3‑Benzoyl‑5,7‑diphenyl‑5h‑thiazolo[3,2‑a]pyrimidine derivatives and their applications
  • 3‑Benzoyl‑5,7‑diphenyl‑5h‑thiazolo[3,2‑a]pyrimidine derivatives and their applications
  • 3‑Benzoyl‑5,7‑diphenyl‑5h‑thiazolo[3,2‑a]pyrimidine derivatives and their applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Preparation of 4-(4-methoxyphenyl)-6-(4-chlorophenyl)-3,4-dihydropyrimidine-2(1H)-thione

[0020] Add 0.1 mol of 4-methoxybenzaldehyde, 0.1 mol of thiourea, 0.11 mol of 4-chloroacetophenone, 0.1 mol of trimethylchlorosilane and 30 mL of acetonitrile into a 250 ml round bottom flask, stir, and reflux for 10 h. Cool, filter with suction, and recrystallize the filter cake from absolute ethanol to obtain 20.5 g of yellow crystals, with a yield of 62.1%. ESI-MS (m / z): 331.2 (M+H) + .

Embodiment 2

[0022] Preparation of 4-(4-hydroxyphenyl)-6-(4-chlorophenyl)-3,4-dihydropyrimidine-2(1H)-thione

[0023] Add 0.1 mol of 4-hydroxybenzaldehyde, 0.1 mol of thiourea, 0.11 mol of 4-chloroacetophenone, 0.1 mol of trimethylchlorosilane, and 30 mL of acetonitrile into a 250 ml round bottom flask, stir, and reflux for 10 h. Cool, filter with suction, and recrystallize the filter cake from absolute ethanol to obtain 24.2 g of yellow crystals, with a yield of 76.4%. ESI-MS (m / z): 316.8 (M+H) + .

Embodiment 3

[0025] Preparation of 4-(4-chlorophenyl)-6-(4-chlorophenyl)-3,4-dihydropyrimidine-2(1H)-thione

[0026] Add 0.1 mol of 4-chlorobenzaldehyde, 0.1 mol of thiourea, 0.11 mol of 4-chloroacetophenone, 0.1 mol of trimethylchlorosilane, and 30 mL of acetonitrile into a 250 ml round bottom flask, stir, and reflux for 10 h. After cooling, suction filtration, and recrystallization of the filter cake from absolute ethanol, 24.8 g of yellow crystals were obtained, with a yield of 74.0%. ESI-MS (m / z): 335.3 (M+H) + .

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Abstract

The invention discloses application of 3-benzoyl-5, 7-diphenyl-5H-thiazole [3, 2-a] pyrimidine derivatives shown in a general formula to antibacterial drugs, wherein R1, R2 and R3 are hydrogen, methyl, halogen, hydroxyl, methoxyl, nitryl, ethanoyl, propionyl or alkoxyl which are separated from each other respectively. The compound has an obvious inhibiting effect in the plurality of bacteria such as meticillin-resistant staphylococcus aureus, escherichia colim, pseudomonas aeruginosa and the like, and can be used for preparing the antibacterial drugs.

Description

technical field [0001] The present invention relates to the field of chemical and pharmaceutical technology, in particular to 3-benzoyl-5,7-diphenyl-5 H -Thiazolo[3,2-a]pyrimidine derivatives and their application in the preparation of antibacterial drugs. Background technique [0002] Since penicillin was used clinically in the 1940s, antibiotics have saved countless lives, and penicillin has thus become one of the greatest human discoveries in the 20th century, and opened up a new era of antibiotic research. Cephalosporins, quinolones, Various types of antibiotics such as macrolides and aminoglycosides. It is true that we have such a wide variety of antibacterial drugs, but with the abuse of antibiotics, the problem of bacterial drug resistance has become increasingly prominent. In fact, almost all antibiotics have been challenged by corresponding drug-resistant strains. Since New Grinea discovered penicillin-resistant Streptococcus pneumoniae in 1967, a variety of dru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D513/04A61P31/04
CPCC07D513/04Y02A50/30
Inventor 刘斯婕张宝华史兰香何敬宇贾鹏飞
Owner SHIJIAZHUANG UNIVERSITY
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