Novel application of rifamycin-quinolizidone double target molecule

A technology of rifamycin and quinazinone, which is applied in the field of medicinal chemistry and achieves good application prospects

Active Publication Date: 2017-06-30
TENNOR THERAPEUTICS (SUZHOU) LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] At present, Chinese patent ZL200580031655.4 "Rifamycin Derivatives for Treating Microbial Infection" discloses the compound (R)-3-[(4-{1-[1-(3-carboxy-1-cyclopropyl-7 -Fluoro-9-methyl-4-oxo-4H-quinazin-8-yl)-pyrrolidin-3-yl-cyclopropyl]-methylamino}-piperidin-1-ylimino)-ylidene Methyl]-rifamycin SV, the compound has antimicrobial activity against various bacteria such as Gram-positive bacteria and Escherichia coli, but there is no documented antibacterial activity against anaerobic flora

Method used

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  • Novel application of rifamycin-quinolizidone double target molecule
  • Novel application of rifamycin-quinolizidone double target molecule
  • Novel application of rifamycin-quinolizidone double target molecule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] This example provides the application of the rifamycin-quinazinone dual target molecule represented by formula I in inhibiting anaerobic bacteria;

[0032]

[0033]Among them, anaerobic bacteria include Actinomyces naeseri, Anaerobic coccus praustzii, Atobo vaginalis, Bacteroides fragilis (including metronidazole-resistant type), Bacteroides polymorpha (including metronidazole-resistant type ), Bacteroides cellulosus, Bacteroides monomorpha, Bacteroides vulgaris, Bacteroides ovale (including metronidazole-resistant types), Bifidobacterium breve, Bifidobacterium longum, Clostridium sporeformans, Perfringens Clostridium difficile (including metronidazole-resistant type), Eubacterium rectum, Fusobacterium nucleatum, Gardnerella vaginalis, Lactobacillus crispatus, Lactobacillus gasseri, Lactobacillus jansnii, Mobilis kervii, Campylobacter shy, Peptococcus (Niger), Glycopeptophilus (including metronidazole-resistant), Peptostreptococcus large, Peptostreptococcus anaerobic...

Embodiment 2

[0053] This example provides the prescription and preparation method of a fast-release oral preparation of the rifamycin-quinazinone dual target molecule represented by formula I.

[0054]

[0055] Weigh the rifamycin-quinazinone dual-target molecule and excipients represented by formula I according to the above prescription. Dissolve povidone K30 (PVP K30) and sodium dodecyl sulfate (SDS) in purified water, stir for 1 hour, and use it as an adhesive for later use; Pass through a 30-mesh sieve, add to the granulator, and pre-mix, the impeller stirring speed is 700rpm, and the time is about 15 minutes. Then use a peristaltic pump to add an appropriate amount of purified water and binder to the mixture of the granulator at a fixed speed (145-165g / min). The stirring speed of the impeller of the granulator is 400rpm, and the time is about 1 to 2 minutes. After the binder is added , continue mixing for 0.5 to 1 minute; use a fluidized bed to dry the wet granules, set the inlet ...

Embodiment 3

[0058] This example provides a method for preparing an injection of the rifamycin-quinazinone dual target molecule represented by formula I.

[0059]

[0060] Add mannitol, acetaldehyde sodium sulfoxylate, and Tween-80 to an appropriate amount of water for injection under nitrogen protection, add the rifamycin-quinazinone dual-target molecule shown in formula I, and stir at a medium speed for 10-15 minutes. Wet the rifamycin-quinazinone dual-target molecule shown in formula I, and slowly add 1N NaOH dropwise, which takes about 175 minutes (fast at the beginning and slow at the end), to the rifamycin-quinazinone shown in formula I The dual-target molecules are completely dissolved, filtered through two microporous membranes of 0.45+0.22μm, and the filtrate is filled into 10mL glass bottles, each containing 3.5mL, and the glass bottles are transferred to a lyophilizer for lyophilization, and the formula is obtained after capping The freeze-dried powder injection of the rifamy...

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Abstract

The invention discloses an application of a rifamycin-quinolizidone double target molecule shown in formula I in inhibition of anaerobic flora. The rifamycin-quinolizidone double target molecule shown in formula I has broad spectrum antimicrobial activity comprising activity for anaerobic bacteria including most pathogenic bacteria of vaginae, has the in-vitro antibacterial activity superior to that of metronidazole, clindamycin and other first-tier bacterial vaginosis resisting drugs and has good application prospects in the aspects of prevention and treatment of bacterial vaginosis or other related diseases caused by anaerobic bacteria.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a new application of a rifamycin-quinazinone dual-target molecule. Background technique [0002] Anaerobic bacteria are a group of bacteria that grow better in the absence of oxygen than in aerobic environments, but cannot grow on the surface of solid media at air (18% oxygen) and / or 10% carbon dioxide concentrations . This type of bacteria lacks a complete metabolic enzyme system, and its energy metabolism is carried out by anaerobic fermentation. [0003] Anaerobic bacteria include the following categories: [0004] 1. Gram-positive anaerobic cocci (GPAC) [0005] Including Peptostreptococcus, Finegoldia, Anaerococcus, Peptoniphilus, Veillonella, etc., are the human oral cavity, upper respiratory tract, gastrointestinal tract and Part of the microbial flora of the female genitourinary system, it is an opportunistic pathogen that can cause various degrees of in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4545A61P31/04A61P15/02
CPCA61K31/4545
Inventor 马振坤袁鹰刘宇王晓梅
Owner TENNOR THERAPEUTICS (SUZHOU) LTD
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