Department of Chemistry, Faculty of Science and Literature, Harran University, Sanliurfa 63300, Turkey.
Bioorg Chem. 2011 Jun;39(3):114-9. doi: 10.1016/j.bioorg.2011.02.004. Epub 2011 Mar 2.
Novel sulfanilamide derivatives were synthesized and evaluated for carbonic anhydrase inhibitory activity as a target for the treatment of glaucoma, and antibacterial properties for use in chemotherapy. Synthesized compounds were characterized by FT-IR, (1)H NMR, (13)C NMR and photoluminescence. In vitro inhibitory activities were measured by UV-Vis and some of the compounds were found have greater inhibitory effects than the lead compound sulfanilamide. The correlation between inhibitory activity, biological properties and the physicochemical properties of water solubility and partition coefficients was also investigated. Sulfanilamide derivatives gave intense emissions upon irradiation by UV light and a dimethyl substituted compound and a cyclic analog have photoluminescence quantum yields 42% and 31% and long excited-state lifetimes of 3.92 and 2.91 ns, respectively.
新型磺胺类衍生物被合成并评价为碳酸酐酶抑制活性，作为治疗青光眼的靶点，以及用于化疗的抗菌特性。合成的化合物通过傅里叶变换红外光谱（FT-IR）、（1）H 核磁共振（1H NMR）、（13）C 核磁共振（13C NMR）和光致发光进行了表征。通过紫外-可见分光光度计测量了体外抑制活性，一些化合物的抑制效果比先导化合物磺胺更强。还研究了抑制活性、生物性质以及水溶性和分配系数等物理化学性质之间的相关性。磺胺衍生物在紫外光照射下会发出强烈的光，一个二甲基取代的化合物和一个环状类似物的光致发光量子产率分别为 42%和 31%，激发态寿命分别为 3.92 和 2.91 ns。
