薩博·卡門
抽象的：
根據國際多基因疾病聯合會(IDF) 的報告，我們進一步發現了一種糖尿病，因為其併發症導致2019 年約420 萬成年人死亡。 ，導致慢性糖尿病。 疾病，通常隨著年齡的增長，在有氧壓力和細胞大分子的非酶糖化作用下發生。糖尿病伴隨嚴重的慢性併發症，如視網膜病變、腎臟病、病理和血管疾病。
雙型不適可能是一種慢性疾病。其特徵是血液中糖分含量高。雙多基因疾病又稱為雙糖尿病和非胰島素依賴型糖尿病。這是因為它幾乎總是在成年中後期開始。然而，很多很多的青少年和年輕人都患有這種情況。類雙多基因疾病比類單多基因疾病常見得多，而且實際上是一種特殊的疾病。但它與一種多基因疾病高血糖有共同之處，也有高血糖的併發症。
儘管目前有幾種有效的藥物可供使用，但它們的不同且通常嚴重的副作用需要新的、更安全的多種療法2。單醣酶（AR）蛋白的抑制將緩解或可能阻止諸如腎衰竭、失明或血管疾病等多基因疾病的長期併發症的發生。 4-噻唑烷酮衍生物被設計為潛在的 AR 抑制劑3；但是，在將這些化合物用作藥物之前，應該對其混雜性質進行調查。
The thiazolidinediones square measure the heterocyclic compounds consisting of a membered C3NS ring additionally called glitazones, this is often primarily used for the treatment of diabetes. Thiazolidinones square measure a legendary category of prospective drug-like molecules, particularly within the style of recent antitumor agents. 2 of the foremost outstanding subtypes of those compounds square measure 5-ene-2-amino(amino)-4-thiazolidinones and thiopyrano[2,3-d]thiazoles. The latter square measure thought of to be cyclic mimetics of biologically active 5-ene-4-thiazolidinones with similar medicine profiles. Therefore, the aim of this study was to guage the impact of 4-thiazolidinone-based compounds on toxicity, the apoptotic method, and metabolism within the human squamous malignant neoplastic disease (SCC-15) cell line. The SCC-15 cells were polite in phenol red-free DMEM/F12 medium supplemented with 100 percent FBS, cortisol, and exposed to rising concentrations (1 nM-100 μM) of the studied compounds for six, twenty four and forty eight h. Afterwards, reactive O species (ROS) formation, cell viability, caspase-3 activity, and cell metabolism were measured. The obtained results showed that every one of the studied compounds during a wide selection of concentrations (1 nM-100 μM) exaggerated DCF light that suggests a stimulation of ROS production. Still, these new compounds showed cytotoxic and proapoptotic properties solely at high (10-100 μM) concentrations. Our studies square measure the primary to be administered on these compounds and need any investigation to clarify the mechanism of action of their antitumor potential.
PHYSICAL PROPERTIES ANDSTEREOCHEMISTRY
Physical properties of thiazolidinones. The 3-unsubstituted-4-thiazolidinones square measure typically solids, however theattachment of associate chemical group to the N at position three lowers the temperature, creating the compound oily Polymorphism is ascertained within the case of 3-phenyl-2,4-thiazolidione and with 3-aminorhodanine (derivative ofthiazolidinones). Thermal analysis disclosed that 3-phenyl-2,4-thiazolidione exists in 2 2 one type melts at 143–144°C (usuallyobtained from glacial ethanoic acid solution) and is stable atroom temperature, whereas the opposite type, that melts at147–148°C (obtained from binary compound media), is stableabove 100°C. The 4-thiazolidinones having no aryl or alkylsubstituents square measure rather soluble in water, whereas theintroduction of substituents decreases the water solubilityto such associate extent that the utility of the compounds inaqueous media is restricted. Polarity is additionally observedfor some derivatives: a pair of,4-thiazolidinedione (1A) shows adipole moment of two.03 D; rhodanine (1B): a pair of.20 D; and 3-ethylrhodanine.
Methodology & Theoretical Orientation:
我們的分析旨在弄清楚這些 4-噻唑烷酮衍生物是否符合文獻中發現的性活動因素。這些標準衡量如下：（1）時間依賴性，（2）對蛋白質濃度變化的敏感性進一步取決於去污劑的存在，以及（3）對具有相當不同的酶的正軌酶的顯著抑制結果機制和/或功能4-5。使用含髮色團的底物和豬外分泌腺作為蛋白質，以分光光度法進行活性測量。由於聚集是性活動的一個原因，因此在這些抑制劑變得混雜的情況下，我還透過 HPLC 檢測了它們的聚集傾向。
結果：
噻唑烷酮屬於重要的雜環化合物簇，在藥物領域的應用已得到了廣泛的探索。噻唑烷酮類，化學基團位於一對 (I)、四個 (II) 或五個 (III) 位。雜環化學是藥物發現的核心1。 4-噻唑烷酮是五元雜環2,3 中最受深入研究的類別之一。 4-噻唑烷酮類化合物是含有氮原子和硫原子的雜環化合物，因其具有多種引人注目的生物活性，特別是藥物活性、抗發炎活性、抗結核活性、驅蟲活性而長期享有盛譽。
七個測試的抑制劑中的三個被發現是混雜的。在這些情況下，由於去污劑的存在以及不同蛋白質濃度的使用，IC50值被誇大，它們能夠迅速抑制3種不相關的酶，並且IC50值在酶抑製劑預孵育的影響下降低。
結論及意義：
4-噻唑烷酮衍生物被評估為單醣酶抑制劑。在測試的化合物中，大多數 N-未取代的類似物被發現在低微摩爾劑量下具有抑製作用，其中 2 種表現出比用作參考藥物的索比尼更高的效率。七種合成的 AR 抑制劑中有 3 種不打算用作
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