The Experts below are selected from a list of 303 Experts worldwide ranked by ideXlab platform
Xinxing Gong - One of the best experts on this subject based on the ideXlab platform.
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synthesis of pyrazolo 5 1 a isoquinolines via a silver i catalyzed reaction of 1 arylethylidene Hydrazides with n 2 alkynylbenzylidene Hydrazides
Organic and Biomolecular Chemistry, 2015Co-Authors: Xinxing GongAbstract:A silver(I)-catalyzed reaction of (1-arylethylidene)Hydrazides with N′-(2-alkynylbenzylidene)Hydrazides is reported, which provides an efficient approach for the synthesis of pyrazolo[5,1-a]isoquinolines. During the reaction process, azo-alkene and isoquinolinium-2-yl amide acted as the key intermediates, which then underwent [3 + 2] cycloaddition and intramolecular rearrangement leading to the corresponding pyrazolo[5,1-a]isoquinolines. Azo-alkene would be formed in situ from (1-arylethylidene)hydrazide in the presence of I2 and TBHP, and isoquinolinium-2-yl amide would be generated in situ via a silver(I)-promoted 6-endo cyclization of N′-(2-alkynylbenzylidene)hydrazide. This transformation proceeds smoothly under mild conditions and tolerates a broad range of functional groups.
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Synthesis of pyrazolo[5,1-a]isoquinolines via a silver(I)-catalyzed reaction of (1-arylethylidene)Hydrazides with N′-(2-alkynylbenzylidene)Hydrazides
Organic and Biomolecular Chemistry, 2015Co-Authors: Xinxing Gong, Jie WuAbstract:A silver(I)-catalyzed reaction of (1-arylethylidene)Hydrazides with N′-(2-alkynylbenzylidene)Hydrazides is reported, which provides an efficient approach for the synthesis of pyrazolo[5,1-a]isoquinolines. During the reaction process, azo-alkene and isoquinolinium-2-yl amide acted as the key intermediates, which then underwent [3 + 2] cycloaddition and intramolecular rearrangement leading to the corresponding pyrazolo[5,1-a]isoquinolines. Azo-alkene would be formed in situ from (1-arylethylidene)hydrazide in the presence of I2 and TBHP, and isoquinolinium-2-yl amide would be generated in situ via a silver(I)-promoted 6-endo cyclization of N′-(2-alkynylbenzylidene)hydrazide. This transformation proceeds smoothly under mild conditions and tolerates a broad range of functional groups.
Jie Wu - One of the best experts on this subject based on the ideXlab platform.
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Synthesis of pyrazolo[5,1-a]isoquinolines via a silver(I)-catalyzed reaction of (1-arylethylidene)Hydrazides with N′-(2-alkynylbenzylidene)Hydrazides
Organic and Biomolecular Chemistry, 2015Co-Authors: Xinxing Gong, Jie WuAbstract:A silver(I)-catalyzed reaction of (1-arylethylidene)Hydrazides with N′-(2-alkynylbenzylidene)Hydrazides is reported, which provides an efficient approach for the synthesis of pyrazolo[5,1-a]isoquinolines. During the reaction process, azo-alkene and isoquinolinium-2-yl amide acted as the key intermediates, which then underwent [3 + 2] cycloaddition and intramolecular rearrangement leading to the corresponding pyrazolo[5,1-a]isoquinolines. Azo-alkene would be formed in situ from (1-arylethylidene)hydrazide in the presence of I2 and TBHP, and isoquinolinium-2-yl amide would be generated in situ via a silver(I)-promoted 6-endo cyclization of N′-(2-alkynylbenzylidene)hydrazide. This transformation proceeds smoothly under mild conditions and tolerates a broad range of functional groups.
Vipan Kumar - One of the best experts on this subject based on the ideXlab platform.
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Design, synthesis, anti‐mycobacterial and cytotoxic evaluation of C‐4 functionalized 1,8‐naphthalimide‐heterocyclic hydrazide conjugates
Chemical Biology and Drug Design, 2019Co-Authors: Shalini Shalini, Matt Johansen, Laurent Kremer, Vipan KumarAbstract:This manuscript discloses the design and synthesis of a series of C-4 functionalized 1,8-naphthalimide-heterocyclic hydrazide conjugates along with their anti-mycobacterial and cytotoxic evaluation. The present work assumes significance as it describes the first report on the amalgamation of C-4 substituted naphthalimides with various heterocyclic Hydrazides. However, contrary to the rationale behind the synthesis of the conjugates, none of them inhibited the growth of Mycobacterium tuberculosis at the tested concentrations though these were non-cytotoxic towards the Vero kidney epithelial cell line.
James A. Bain - One of the best experts on this subject based on the ideXlab platform.
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Convulsive Effect of Hydrazides: Relationship to Pyridoxine12
International Review of Neurobiology, 2008Co-Authors: Harry L. Williams, James A. BainAbstract:Publisher Summary This chapter concerns with the pharmacology of the convulsant Hydrazides and more specifically with their probable relations to pyridoxine (PN) metabolism. It is shown that PN can reverse the convulsant effect of semicarbazide (SC) and that pyridoxine antagonists would enhance the toxicity of SC. Convulsions produced by Hydrazides are found to be accompanied by inhibition of vitamin B 6 -requiring enzymes in the brain. Hydrazide treatment is shown to produce xanthenmia, an indication of Pyridoxine deficiency, in tryptophan-loaded dogs. The failure of reasonable doses of a variety of other metabolites to antagonize SC and thiosemicarbazide (TSC) effects accentuated the specificity of the pyridoxine reversal. Despite certain anomalous observations, such as the failure of pyridoxine-deficient diets to enhance the toxicity of TSC and the failure of isoniazid (INH) to produce xantlienuria in rats, a relationship of vitamin B 6 to hydrazide-induced convulsions seemed clearly indicated. The chapter also discusses parallel developments in the biochemical and clinical aspects of hydrazide action.
Konstantin Majorov - One of the best experts on this subject based on the ideXlab platform.
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synthesis and antituberculosis activity of indole pyridine derived Hydrazides hydrazide hydrazones and thiosemicarbazones
Bioorganic & Medicinal Chemistry Letters, 2016Co-Authors: V S Velezheva, Albert G Kornienko, Konstantin Kazarian, B V Nikonenko, Patrick J. Brennan, Sergey E. Lyubimov, P. A. Ivanov, Konstantin MajorovAbstract:Abstract We describe the design, synthesis, and in vitro antimycobacterial activity of a series of novel simple hybrid Hydrazides and hydrazide–hydrazones combining indole and pyridine nuclei. The compounds are derivatives of 1-acetylindoxyl or substituted indole-3-carboxaldehydes tethered via a hydrazine group by simple C N or double C N bonds with 3- and 4-pyridines, 1-oxide 3- and 4-pyridine carboHydrazides. The most active of 15 compounds showed MICs values against an INH-sensitive strain of Mycobacterium tuberculosis H37Rv equal to that of INH (0.05–2 μg/mL). Five compounds demonstrated appreciable activity against the INH-resistant M. tuberculosis CN-40 clinical isolate (MICs: 2–5 μg/mL), providing justification for further in vivo studies.
