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
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[0021] Example 1
[0022] A carbonic anhydrase inhibitor with the chemical name {5-[N,N-(4-methylbenzyl), benzenesulfonyl-amino]-1,3,4-thiadiazol-2-yl } Sulfonamide, its chemical structure is:
[0023]
[0024] For the preparation method, refer to Example 40 of the CN201010266763.2 specification. The specific preparation method is:
[0025] (1) Add 12.15g (55mmol) of N-[5-(sulfamoyl)-1,3,4-thiadiazol-2-yl]acetamide (acetazolamide) and 180ml in a 250ml round bottom flask. Water ethanol, heat to 80-90℃ and reflux, add 12ml of concentrated HCl under stirring, reflux for 5 hours to become a transparent solution; vaporize most of the ethanol to obtain a white slurry, after cooling, filter to obtain a white powdery solid, water recrystallization Colorless granular crystals (5-amino-1,3,4-thiadiazol-2-yl)sulfonamide, weighed 7.23g after drying, 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), Ta...
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[0028] Example 2
[0029] 1. Experimental materials
[0030] 1. Test strain
[0031] The test strains were provided by the Fungus Species Bank of the New Drug Research Center, 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 three distilled water to dissolve, adjust the pH to 7.0 (25℃) with 1M NaOH, set the volume to 1000ml, filter and sterilize ,Store at 4℃;
[0036] (2) YEPD culture solution: 10g yeast extract, 20g peptone, 20g glucose, dissolved in 900ml of three-distilled water, add 50ml of 2mg / ml chloramphenicol aqueous solution, dilute to 1000ml, and store at 4℃ after autoclaving;
[0037] (3) Sabouraud dextrose agar (SDA): peptone 10g, glucose 40g, agar 18g, dissolved in 900ml ...
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