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首页> 外文期刊>Zeitschrift fur Naturforschung, B. A Journal of Chemical Sciences >Synthesis and anti-HIV activity of new benzimidazole, benzothiazole and carbohyrazide derivatives of the anti-inflammatory drug indomethacin
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Synthesis and anti-HIV activity of new benzimidazole, benzothiazole and carbohyrazide derivatives of the anti-inflammatory drug indomethacin

机译：抗炎药吲哚美辛的新苯并咪唑，苯并噻唑和碳酰肼衍生物的合成及抗HIV活性

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摘要

There is an urgent need for the design and development of new and safer drugs for the treatment of HIV infection, active against the currently resistant viral strains. New derivatives of the non-steroidal anti-inflammatory drug indomethacin bearing benzimidazoles, benzothiazole, purine and pyridine residues 8-13 were synthesized with the aim of developing new non-nucleoside reverse transcriptase inhibitors (NNRTIs). Alternatively, new imine analogs 16-20 were synthesized from condensation of indomethacinyl hydrazide 15, prepared from the ester 14, with various ketone precursors. Treatment of 15 with phenyl isothiocyanate or triethyl orthoformate afforded the phenylcarbonothioyl and the oxadiazole derivatives 21 and 22, respectively. The new compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compounds 9 and 10 were the most active in inhibiting HIV-2 and HIV-1, respectively, with EC_(50) ≥ 17.60 μg mL~(-1) and > 1.15 μg mL~(-1) (therapeutic indexes (SI) of ≥ 3 and < 1, respectively), and are leading candidates for further development.
机译：迫切需要设计和开发用于治疗HIV感染，对目前耐药的病毒株有活性的新型和更安全的药物。合成具有苯并咪唑，苯并噻唑，嘌呤和吡啶残基8-13的非甾体抗炎药消炎痛的新衍生物，其目的是开发新的非核苷逆转录酶抑制剂（NNRTIs）。或者，从由酯14制备的吲哚美辛酰肼15与各种酮前体的缩合合成新的亚胺类似物16-20。用异硫氰酸苯基酯或原甲酸三乙酯处理15，分别得到苯基硫代羰基和恶二唑衍生物21和22。测定了新化合物对MT-4细胞中的HIV-1和HIV-2的抵抗力。化合物9和10分别以EC_（50）≥17.60μgmL〜（-1）和> 1.15μgmL〜（-1）（治疗指数（SI））分别最有效地抑制HIV-2和HIV-1。分别≥3和<1），并且是进一步开发的主要候选对象。

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