Microwave assisted efficient Hantzsch reaction via four-component coupling reactions of tetrazolo[1,5-α]quinoline-4-carbal-dehyde, dimedone/cyclohexane-1,3-dione,ethyl/methyl acetoacetate and ammonium acetate was des...Microwave assisted efficient Hantzsch reaction via four-component coupling reactions of tetrazolo[1,5-α]quinoline-4-carbal-dehyde, dimedone/cyclohexane-1,3-dione,ethyl/methyl acetoacetate and ammonium acetate was described as the preparation of tetrazolo[1,5-α]quinoline based 1,4-dihydropyridines,acridine-1,8-diones and polyhydroquinolines.The process presented here is simple,rapid,environmentally welcoming and high yielding.All the derivatives were subjected to an in vitro antimicrobial screening against a representative panel of bacteria and fungi and results worth further investigations.展开更多
A series of some new tetrazolo[1,5-a]quinoline based tetrasubstituted imidazole derivatives 6a-i have been synthesized by a reaction of tetrazolo[ 1,5-a]quinoline-4-carbaldehyde 3a-d, benzil 4, aromatic amine 5a--c an...A series of some new tetrazolo[1,5-a]quinoline based tetrasubstituted imidazole derivatives 6a-i have been synthesized by a reaction of tetrazolo[ 1,5-a]quinoline-4-carbaldehyde 3a-d, benzil 4, aromatic amine 5a--c and ammonium acetate in the presence of iodine through one-pot multi-component reaction （MCR） approach. All the derivatives were screened for antimicrobial and antituberculosis activities and results worth further investigations.展开更多
为了评价4,5-二氢-7-(4-氯苯氧基)-四唑[1,5-a]喹啉(S2011017)的抗癫痫活性,采用最大电惊厥(Maximum Electron Shock,MES)实验、多种化学致惊实验及急性神经毒性实验,测定了其作用时间和剂量关系。MES实验结果表明,腹腔给药5 min后,S201...为了评价4,5-二氢-7-(4-氯苯氧基)-四唑[1,5-a]喹啉(S2011017)的抗癫痫活性,采用最大电惊厥(Maximum Electron Shock,MES)实验、多种化学致惊实验及急性神经毒性实验,测定了其作用时间和剂量关系。MES实验结果表明,腹腔给药5 min后,S2011017表现出较好的抗癫痫活性(ED50=11.8 mg·kg-1)。在化学致惊实验中,S2011017对异烟肼(ISO),3-巯基丙酸(3-MP),荷包牡丹碱(BIC)和硫代氨基脲(THIO)引起的惊厥有效。因此,由于S2011017表现出广谱的抗惊厥活性,并且能够快速地达到抗惊厥活性的峰值,可以作为一种潜在抗癫痫药,进行深入的成药性评价。展开更多
文摘Microwave assisted efficient Hantzsch reaction via four-component coupling reactions of tetrazolo[1,5-α]quinoline-4-carbal-dehyde, dimedone/cyclohexane-1,3-dione,ethyl/methyl acetoacetate and ammonium acetate was described as the preparation of tetrazolo[1,5-α]quinoline based 1,4-dihydropyridines,acridine-1,8-diones and polyhydroquinolines.The process presented here is simple,rapid,environmentally welcoming and high yielding.All the derivatives were subjected to an in vitro antimicrobial screening against a representative panel of bacteria and fungi and results worth further investigations.
文摘A series of some new tetrazolo[1,5-a]quinoline based tetrasubstituted imidazole derivatives 6a-i have been synthesized by a reaction of tetrazolo[ 1,5-a]quinoline-4-carbaldehyde 3a-d, benzil 4, aromatic amine 5a--c and ammonium acetate in the presence of iodine through one-pot multi-component reaction （MCR） approach. All the derivatives were screened for antimicrobial and antituberculosis activities and results worth further investigations.
文摘开展了取代5-(2-卤代苯基)-1 H四唑与炔烃为原料在镍(Ⅱ)盐催化串联反应生成四氮唑[5,1-α]异喹啉衍生物的微波辅助合成研究。结果表明:相同反应时间,在镍催化微波辅助条件下,生成四氮唑[5,1-α]异喹啉衍生物的效率较常规加热条件下增强。一系列四氮唑[5,1-α]异喹啉衍生物被高效地合成出来,最高产率达到88%。产物结构经1H NMR、13 C NMR及MS得到确证。该方法具有产率高、操作简单、环境友好等优点。
文摘为了评价4,5-二氢-7-(4-氯苯氧基)-四唑[1,5-a]喹啉(S2011017)的抗癫痫活性,采用最大电惊厥(Maximum Electron Shock,MES)实验、多种化学致惊实验及急性神经毒性实验,测定了其作用时间和剂量关系。MES实验结果表明,腹腔给药5 min后,S2011017表现出较好的抗癫痫活性(ED50=11.8 mg·kg-1)。在化学致惊实验中,S2011017对异烟肼(ISO),3-巯基丙酸(3-MP),荷包牡丹碱(BIC)和硫代氨基脲(THIO)引起的惊厥有效。因此,由于S2011017表现出广谱的抗惊厥活性,并且能够快速地达到抗惊厥活性的峰值,可以作为一种潜在抗癫痫药,进行深入的成药性评价。
