da Silva Emerson T, da Silva Araújo Adriele, Moraes Adriana M, de Souza Leidiane A, Silva Lourenço Maria Cristina, de Souza Marcus V N, Wardell James L, Wardell Solange M S V
Fundação Oswaldo Cruz (Fiocruz), Instituto de Tecnologia em Fármacos Farmanguinhos, Rua Sizenando Nabuco, 100, Manguinhos 21041-250, Rio de Janeiro, Brazil.
Instituto de Pesquisa Clínica Evandro Chagas (IPEC)Av. Brasil, 4365, Fiocruz, 21040-900 Rio de Janeiro, Brazil.
Sci Pharm. 2015 Oct 18;84(3):467-483. doi: 10.3390/scipharm84030467.
Both sonochemical and classical methodologies have been employed to convert camphor, 1,7,7-trimethylbicyclo[2.2.1]heptan-2-one, C₉HC=O, into a number of derivatives including hydrazones, C₉HC=N-NHAr , imines, C₉HC=N-R , and the key intermediate nitroimine, C₉HC=N-NO₂ . Reactions of nitroamine with nucleophiles by classical methods provided the desired compounds in a range of yields. In evaluations of activity against , compound exhibited the best activity (minimal inhibitory concentration (MIC) = 3.12 µg/mL), comparable to that of the antitubercular drug ethambutol. The other derivatives displayed modest antimycobacterial activities at 25-50 µg/mL. In in vitro tests against cancer cell lines, none of the synthesized camphor compounds exhibited cytotoxic activities.
声化学方法和传统方法都已被用于将樟脑（1,7,7 - 三甲基双环[2.2.1]庚 - 2 - 酮，C₉HC=O）转化为多种衍生物，包括腙（C₉HC=N - NHAr）、亚胺（C₉HC=N - R）以及关键中间体硝基亚胺（C₉HC=N - NO₂）。通过传统方法使硝胺与亲核试剂反应，以一系列产率得到了所需化合物。在针对[具体对象未提及]的活性评估中，化合物表现出最佳活性（最低抑菌浓度（MIC）= 3.12 µg/mL），与抗结核药物乙胺丁醇相当。其他衍生物在25 - 50 µg/mL时表现出适度的抗分枝杆菌活性。在针对癌细胞系的体外试验中，所合成的樟脑化合物均未表现出细胞毒性活性。
