Sulfonamides compound for inhibiting carbonic anhydrase II and synthesis method and application thereof

Abstract

The invention relates to a sulfonamides compound for inhibiting carbonic anhydrase II and a synthesis method and an application thereof. The compound has the structure as shown in the specification. The invention features economical and reasonable synthetic route and high utilization of resources. The synthesis method is simple and easy to carry out and is more suitable for large-scale industrialized production. With human carbonic anhydrase II (Human Carbonic Anhydrase II, hCA II) expressed by procaryotic cell as an enzyme source, the invention establishes an in-vitro carbonic anhydrase inhibitor screening model. In addition, the compound of the invention has inhibitive effect on activity of the human carbonic anhydrase II.

Description

technical field The invention relates to a sulfonamide compound for inhibiting carbonic anhydrase II, a synthesis method and application. Background technique Plateau areas account for about 26% of my country's land area, and most of them are strategically important areas, mainly concentrated in Qinghai, Xinjiang and Tibet. With the rapid development of plateau economic construction and tourism and the intensification of the Sino-Indian border tension, more and more people (including troops) have entered the plateau area. Acute altitude sickness is a common and frequently-occurring disease when the plain enters the plateau (altitude > 2500m) or enters a higher altitude area from the plateau, and the incidence rate reaches 50% to 70%. It is characterized by sudden onset and rapid development, and the pathogenesis is currently unknown. If the treatment is not timely, it is often life-threatening. Acute altitude sickness caused by plateau hypoxia and other factors has beco...

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Problems solved by technology

However, acetazolamide is likely to cause adverse reactions such as hyperchloremic metabolic acidosis, numbness of limbs, gastrointestinal discomfort, confusion, nausea, anorexia, drowsiness, polyuria, and tinnitus. Taking it can aggravate the symptoms of hypokalemia, hyponatremia, electrolyte disturbance and metabolic acidosis

The incidence rate of one adverse reaction is 64.1%, which seriously affects the working ability of plateau practitioners (including troops), and limits its promotion and use as a preventive drug

In addition, the effect of acetazolamide in the prevention and treatment of acute altitude sickness in the Chinese population is not good

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