Tiyoürelerin tüberküloz tedavisinde kullanımı

Abstract

İnsan sağlığı için tüberküloz prevalansı, özellikle immün yetmezlik virüsü enfeksiyonu ve AIDS oldukça ciddi sorunlardandır. Aynı derecede ciddi bir halk sağlığı sorunu çoklu ilaca karşı direncin tüberküloz oranınını artırmasıdır. Çoklu ilaca dirençli tüberküloz hastaları arasındaki oranlar incelendiğinde şu anda sadece birkaç alternatif kemoterapötik rejim mevcut olup düşük terapötik sonuçlar ve yüksek ölüm oranı ile sonuçlanmaktadır. Tüberkülozun tedavisinde kullanılan birinci kuşak ilaçlar izoniazid, etambutol, pirazinamid ve rifampindir. Tüberküloz basili ilaç direnci kazanmaktadır. Buna karşın ikinci kuşak ilaçlar olarak tiyoüre türevlerinden etiyonamid (ETA), protiyonamid (PTA), tiasetazon (TAZ) ve izoksil (ISO), flurokinolonlar, amikasin, kanamisin, kapreomisin ve benzeri ilaçlar kullanılmaktadır. Ancak bu ilaçlara da direnç gelişimi gözlemlenmektedir. Bunlardan farklı bakterisidal mekanizmalara sahip yeni, etkili antitüberküloz ilaçları geliştirmeye acil ihtiyaç duyulmaktadır. Tiyoüreler, olağanüstü biyolojik uygulamalara sahip çok yönlü kimyasallardır. Tiyoürelerin en belirgin biyolojik uygulamaları enfeksiyon tedavisidir. Antioksidan, karınca alerjenleri, anti bakteriyel ajanlar, anti-inflamatuar, anti-tiroid ilaçları, anti-epileptik ilaçlar, anti-hipertansif, rodentisit, kanser önleyici ilaç, DNA bağlayıcı ve üreaz inhibitörleri olarak kullanılmaktadırlar. Bu ligandlar, oksijen, nitrojen ve kükürt atomları aracılığıyla bir dizi metal merkezini koordine etme konusunda belirgin bir yetenek göstermektedir. Bu türevler, nötral tek dişli (S), monobazik iki dişli (O,S) ve iki dişli (N,S) gibi çeşitli bağlanma modlarına sahiptir. Sert ve yumuşak donör bölgelerinin varlığından dolayı seçici bağlayıcılar olarak iyi bilinmektedir. Çalışmalar, bu bileşiklerin mikrobiyal enfeksiyonlar, tüberküloz, karsinomlar, sıtma, üreaz inhibitörleri ve anti-inflamatuar gibi insan hastalıklarını tedavi etmek için ilaç olarak kullanılabileceğini göstermiştir.

Keywords

• tiyoüre
• tiyoüre kompleksleri
• tüberküloz
• mycrobacterium tüberküloz

The use of thioureas in the treatment of tuberculosis

Abstract

The prevalence of tuberculosis, especially immunodeficiency virus infection and AIDS, are serious problems for human health. An equally serious public health concern is that multidrug resistance increases the rate of tuberculosis. Examining the proportions among multidrug-resistant tuberculosis patients, only a few alternative chemotherapeutic regimens are currently available, resulting in low therapeutic outcomes and high mortality. First generation drugs used in the treatment of tuberculosis are isoniazid, ethambutol, pyrazinamide and rifampin. Tuberculosis bacillus is gaining drug resistance. On the other hand, thiourea derivatives such as ethionamide (ETA), prothionamide (PTA), thiacetazone (TAZ) and isoxyl (ISO), fluoroquinolones, amikacin, kanamycin, capreomycin and similar drugs are used as second generation drugs. However, resistance to these drugs is also observed. There is an urgent need to develop new, effective antituberculosis drugs with different bactericidal mechanisms than these. Thioureas are versatile chemicals with extraordinary biological applications. The most prominent biological applications of thioureas are the treatment of infections. They are used as antioxidants, ant allergens, antibacterial agents, anti-inflammatory, anti-thyroid drugs, anti-epileptic drugs, anti-hypertensive, rodenticide, anti-cancer drug, DNA binding and urease inhibitors. These ligands determine a particular ability to target metal centers with a range of lightning, nitrogen and sulfur atoms. These derivatives have modes that can pass neutral single digits (S), monobasic two digits (O,S), and two digits (N,S). They are well known as custom made for garments of hard and cloth donors. These students' microbials can be used as medicine to sicken human diseases such as practice, urea inoperable and anti-inflammatory.

Keywords

• thiourea
• thiourea derivative complexes
• tuberculosis
• mycobacterium tuberculosis

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