Department of Chemistry, Sri Venkateswara University, Tirupati, 517502, India.
Department of Zoology, Sri Venkateswara University, Tirupati, 517502, India.
Mol Divers. 2019 Aug;23(3):723-738. doi: 10.1007/s11030-018-9906-4. Epub 2018 Dec 17.
A series of new urea/thiourea derivatives 3a-j were synthesized by simple addition reaction of functionalized phenyl isocyanates/isothiocyanates 2a-j with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine (imatinib intermediate) (1) in the presence of 1,4-dimethyl piperazine (DMPZ) as a base, and another series of new sulfonamide/carbamate derivatives 5a-k were synthesized by reacting 1 with various substituted aromatic sulfonyl chlorides 4a-f and aromatic/aliphatic chloroformates 4g-k in the presence of DMPZ as a base. The title compounds 3a-j and 5a-k were characterized by IR, H, C NMR and mass spectral data. Antimicrobial, antioxidant and in silico molecular docking studies were made against aromatase.
通过在 1,4-二甲基哌嗪（DMPZ）作为碱的存在下，将功能化的苯基异氰酸酯/异硫氰酸酯 2a-j 与 N-(5-氨基-2-甲基苯基)-4-(3-吡啶基)-2-嘧啶胺（伊马替尼中间体）（1）简单加成反应，合成了一系列新的脲/硫脲衍生物 3a-j；并通过在 DMPZ 作为碱的存在下，将 1 与各种取代的芳基磺酰氯 4a-f 和芳基/脂肪族氯甲酸酯 4g-k 反应，合成了另一系列新的磺酰胺/氨基甲酸酯衍生物 5a-k。标题化合物 3a-j 和 5a-k 通过 IR、H、C NMR 和质谱数据进行了表征。对芳香酶进行了抗菌、抗氧化和计算机分子对接研究。
