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New application of carbonic anhydrase inhibitor

A carbonic anhydrase and inhibitor technology, applied in the field of carbonic anhydrase inhibitors, can solve the problems of discovering β-CAs, which have not been seen, and achieve the effect of avoiding toxicity

Inactive Publication Date: 2012-10-10
INST OF HYGIENE & ENVIRONMENTAL MEDICINE PLA ACAD OF MILITARY MEDICAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the research on β-CAs has been reported in recent years, and the existence of β-CAs has been identified from plants, prokaryotes and fungi, but no β-CAs has been found in humans.
There is no report on the effect of β-CA and its inhibitor on the pathogenic bacteria of dermatophytosis

Method used

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  • New application of carbonic anhydrase inhibitor
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  • New application of carbonic anhydrase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] A carbonic anhydrase inhibitor, the chemical name is {5-[N, N-(4-methylbenzyl), benzenesulfonyl-amino]-1,3,4-thiadiazol-2-yl }sulfonamide, its chemical structure is:

[0023]

[0024] For the preparation method, see Example 40 of CN201010266763.2 specification, the specific preparation method is:

[0025] (1) In a 250ml round bottom flask, add 12.15g (55mmol) N-[5-(sulfamoyl)-1,3,4-thiadiazol-2-yl]acetamide (acetazolamide) and 180ml without Water and ethanol, heated to 80-90°C to reflux, add 12ml of concentrated HCl under stirring, reflux for 5 hours to become a transparent solution; evaporate most of the ethanol to obtain a white slurry, filter after cooling to obtain a white powdery solid, recrystallize from water Colorless granular (5-amino-1,3,4-thiadiazol-2-yl)sulfonamide, weighed after drying to obtain 7.23g, yield 73.4%, mp216-219°C. 1 H NMR (400MHz, DMSO-d 6 , TMS), δ(ppm): 7.81(s), 2H; 8.05(s), 2H; ESI-MS, m / z: Target[M+H] + (calcd.) 180.90 (180.98), Targ...

Embodiment 2

[0029] 1. Experimental materials

[0030] 1. Test strains

[0031] The experimental strains were provided by the fungal strain bank of the New Drug Research Center of the School of Pharmacy, Second Military Medical University (see Table 1).

[0032] Table 1. Test strains for in vitro screening of antifungal activity

[0033]

[0034] 2. Fungal culture medium

[0035] (1) RPMI 1640 culture medium: RPMI1640 (Gibco BRL, Invitrogen) 10g, NaHCO 3 2.0g, 34.5g (0.165M) of morpholinepropanesulfonic acid (MOPS, Sigma), add 900ml of triple distilled water to dissolve, adjust the pH to 7.0 (25°C) with 1M NaOH, dilute to 1000ml, and filter to sterilize , stored at 4°C;

[0036] (2) YEPD culture medium: yeast extract 10g, peptone 20g, glucose 20g, add 900ml of three-distilled water to dissolve, add 2mg / ml chloramphenicol aqueous solution 50ml, dilute to 1000ml, store at 4°C after autoclaving;

[0037] (3) Sabouraud dextrose agar medium (sabouraud dextrose agar, SDA): peptone 10g, ...

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PUM

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Abstract

The invention provides application of a carbonic anhydrase inhibitor in preparation of antifungal medicaments. The carbonic anhydrase inhibitor can be used as an inhibiting medicament for skin pathogenic fungi beta-CA serving as a target, is specifically used for identifying and neutralizing the pathogenic fungi, and plays a specific antifungal role; because the beta-CA does not exist in human body, the carbonic anhydrase inhibitor does not harm related functions of the human body, and avoids toxicity to a host after long-term medication; and the carbonic anhydrase inhibitor is a specific, low-toxicity and efficient ideal skin fungal disease resistant medicament, can be widely applied to grass-roots units and broad masses, and is suitable for large-scale industrialized production.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to a new application of a carbonic anhydrase inhibitor. Background technique [0002] Dermatomycosis is an infectious disease caused by fungal infection of the skin, mucous membranes, hair and nails. Fungi are usually conditional pathogens for healthy humans, but when the body's resistance is reduced and external factors are unfavorable, it may cause systemic or local fungal infections. Important strategic locations such as the southeast coast of China and islands and reefs in the South China Sea are located in the tropics and subtropics. These areas have high temperature and high humidity all year round, which is conducive to the reproduction of fungi. Troops in hot areas have a high incidence of skin mycoses, especially when performing special tasks in hot areas (such as flood fighting) Rescue, etc.) troops, due to fatigue, decreased body resistance, so that the prevalence of fungal ...

Claims

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Application Information

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IPC IPC(8): A61K31/433A61P31/10A61P17/00
Inventor 汪海赵小玲肖忠海杨永林石永平王尚王静王涛李佩尧崔文玉张雁芳龙超良段瑞峰
Owner INST OF HYGIENE & ENVIRONMENTAL MEDICINE PLA ACAD OF MILITARY MEDICAL
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