Even though there are new classes of compounds now frequently used in treatment of fungal infections, the density of deeply invasive candidiasis has increased at least 10-fold during the past decade. Furthermore, many infections due to Candida species are actually refractory to antifungal therapy. In this present study, it was aimed to synthesize, new hydrazide derivatives of tetrahydroimidazo[1,2-a]pyridine and evaluate their anticandidal activity and cytotoxicity in vitro. The reaction of tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid hydrazides with various benzaldehydes gave tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid benzylidene hydrazide derivatives. The chemical structures of the compounds were elucidated and confirmed by IR, ¹H NMR, MS-FAB⁺ spectroscopy and elemental analyses. Eight new tetrahydroimidazo[1,2-a]pyridine derivatives were synthesized and screened for their antifungal effects against a panel of ten human pathogenic Candida albicans, Candida glabrata, Candida krusei, Candida parapsilosis, Candida tropicalis, Candida utilis, and Candida zeylanoides using agar diffusion and broth microdilution assays, respectively. Furthermore, their cytotoxicity was tested against six mammalian cell lines. Among the analogues, the compound 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid-(4-cyanobenzylidene) showed very strong inhibitory activity (up to MIC 0.016 mg/mL) against the screened Candida species. The same compound showed no in vitro toxicity up to 25 μg/mL concentration suggesting that its antifungal activity (MICs 0.016–1 mg/mL) is selective.

即使现在有新种类的化合物经常用于治疗真菌感染，但在过去的十年中，深度侵袭性念珠菌病的密度至少增加了10倍。此外，由于念珠菌引起的许多感染实际上对抗真菌治疗是难治的。在本研究中，其目的是合成四氢咪唑并[1,2-a]吡啶的新酰肼衍生物，并评估其体外的抗候选活性和细胞毒性。四氢咪唑并[1,2-a]吡啶-2-羧酸酰肼与各种苯甲醛的反应，得到四氢咪唑并[1,2-a]吡啶-2-羧酸苄叉酰肼衍生物。通过IR，¹ H NMR，MS-FAB阐明并确认了化合物的化学结构⁺光谱学和元素分析。八个新四氢咪唑并[1,2-a]吡啶衍生物的合成和筛选其对抗10人类致病的面板的抗真菌效果白色念珠菌，光滑念珠菌，克柔念珠菌，近平滑念珠菌，热带念珠菌，产朊假丝，和假丝酵母zeylanoides分别使用琼脂扩散法和肉汤微稀释法。此外，针对六种哺乳动物细胞系测试了它们的细胞毒性。在类似物中，化合物5,6,7,8-四氢咪唑并[1,2-a]吡啶-2-羧酸-（4-氰基苄叉）显示出非常强的抑制活性（最高达MIC 0.016 mg / mL）。筛选念珠菌物种。同一化合物在浓度高达25μg/ mL时无体外毒性，表明其抗真菌活性（MICs 0.016-1-1 mg / mL）具有选择性。