Doctorado en Ciencias Biológicas y de la Salud, Universidad Autónoma Metropolitana (UAM), Ciudad de México 04960, Mexico.
Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, UMAE Hospital de Pediatría, Centro Médico Siglo XXI, Instituto Mexicano del Seguro Social, Ciudad de México 06720, Mexico.
Molecules. 2021 Apr 8;26(8):2145. doi: 10.3390/molecules26082145.
Indazole is an important scaffold in medicinal chemistry. At present, the progress on synthetic methodologies has allowed the preparation of several new indazole derivatives with interesting pharmacological properties. Particularly, the antiprotozoal activity of indazole derivatives have been recently reported. Herein, a series of 22 indazole derivatives was synthesized and studied as antiprotozoals. The 2-phenyl-2-indazole scaffold was accessed by a one-pot procedure, which includes a combination of ultrasound synthesis under neat conditions as well as Cadogan's cyclization. Moreover, some compounds were derivatized to have an appropriate set to provide structure-activity relationships (SAR) information. Whereas the antiprotozoal activity of six of these compounds against , , and had been previously reported, the activity of the additional 16 compounds was evaluated against these same protozoa. The biological assays revealed structural features that favor the antiprotozoal activity against the three protozoans tested, e.g., electron withdrawing groups at the 2-phenyl ring. It is important to mention that the indazole derivatives possess strong antiprotozoal activity and are also characterized by a continuous SAR.
吲唑是药物化学中的一个重要结构。目前，合成方法学的进展已经允许制备具有有趣的药理性质的几种新的吲唑衍生物。特别是，吲唑衍生物的抗原生动物活性最近已被报道。本文合成了一系列 22 种吲唑衍生物并对其作为抗原生动物药物进行了研究。2-苯基-2-吲唑支架通过一锅法获得，该方法包括在无水条件下超声合成与 Cadogan 环化的组合。此外，一些化合物被衍生化以提供合适的结构-活性关系（SAR）信息。虽然这些化合物中有六种对 、 和 的抗原生动物活性先前已有报道，但对另外 16 种化合物的活性进行了评估。生物测定揭示了有利于对三种原生动物测试的抗原生动物活性的结构特征，例如，2-苯基环上的吸电子基团。值得一提的是，吲唑衍生物具有很强的抗原生动物活性，并且还具有连续的 SAR 特征。
