合成肼基噻唑酯衍生物及其抗锥虫和利什曼原虫活性。
Synthesis of hydrazinyl-thiazole ester derivatives, trypanocidal and leishmanicidal activities.
机构信息
Department of Chemistry & Biochemistry, Miami University, 651 E High Street, Oxford, OH 45056, USA.
Department of Chemistry, Mirpur University of Science & Technology (MUST), 10250-Mirpur (AJK), Pakistan.
出版信息
Future Med Chem. 2024 Feb;16(3):221-238. doi: 10.4155/fmc-2023-0255. Epub 2024 Jan 25.
To synthesize novel more potent trypanocidal and leishmanicidal agents. Hantzsch's synthetic strategy was used to synthesize 1,3-thiazole-4-carboxylates and their -benzylated derivatives. 28 new thiazole-carboxylates and their -benzylated derivatives were established to test their trypanocidal and leishmanicidal activities. From both series, compounds , , , and exhibited a better or comparable trypanocidal profile to benznidazole. Among all tested compounds, was found to be the most potent and was better than benznidazole. Further variation of substituents around 1,3-thiazole-4-carboxylates and or hydrazinyl moiety may assist in establishing better and more potent trypanocidal and leishmanicidal agents.
为了合成新型更有效的杀锥虫和杀利什曼原虫药物。采用 Hantzsch 的合成策略合成了 1,3-噻唑-4-羧酸酯及其苄基衍生物。建立了 28 种新的噻唑羧酸酯及其苄基衍生物,以测试它们的杀锥虫和杀利什曼原虫活性。在这两个系列中,化合物 、 、 、 和 对锥虫的杀灭活性优于或与苯并硝唑相当。在所测试的所有化合物中, 被发现是最有效的,优于苯并硝唑。进一步改变 1,3-噻唑-4-羧酸酯和/或肼基部分周围的取代基可能有助于建立更好和更有效的杀锥虫和杀利什曼原虫药物。