- Design, synthesis and evaluation of 5-substituted 1-H-tetrazoles as potent anticonvulsant agents
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Abstract: A series of 5-substituted 1-H-tetrazoles were designed and synthesized as potent anticonvulsant agents. Their preliminary anticonvulsant activities were evaluated using maximal electroshock and subcutaneous pentylenetetrazole (scPTZ) seizure tests. Neurotoxicity was determined using rotarod test. The results indicated that the compound 2j in scPTZ model exhibited the ED50 values of 83.3?mg/kg, superior to the standard drug ethosuximide with the maximum activity. In addition, compound 2k showed the most potent activity in MES model with ED50 value of 9.6?mg/kg and TD50 value of 189.5?mg/kg after intraperitoneal injection in mice, and displayed a high protective index (TD50/ED50) of 19.7 compared to reference antiepileptic drugs. Graphical Abstract: [Figure not available: see fulltext.]
- Liao, Ai-Mei,Wang, Tiantian,Cai, Bangrong,Jin, Yi,Cheon, Seunghoon,Chun, Chang Ju,Wang, Zengtao
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p. 435 - 443
(2017/04/13)
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- A comparative study between heterogeneous stannous chloride loaded silica nanoparticles and a homogeneous stannous chloride catalyst in the synthesis of 5-substituted 1: H -tetrazole
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Heterogeneous SnCl2-nano-SiO2 efficiently catalyzed 5-substituted 1H-tetrazole synthesis with excellent yield. The catalyst was characterized by using FT-IR, TGA, TEM, and EDX. It is widely applicable on aliphatic, aromatic, heteroaromatic and sterically hindered nitriles with five time recyclability. Being simple and an economically viable approach for the synthesis of SnCl2-nano-SiO2 are additional advantages.
- Kumar, Arvind,Kumar, Satyanand,Khajuria, Yugal,Awasthi, Satish Kumar
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p. 75227 - 75233
(2016/08/24)
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- An efficient and economical synthesis of 5-substituted 1 H -tetrazoles via Pb(II) salt catalyzed [3+2] cycloaddition of nitriles and sodium azide
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A simple, mild and efficient method is developed for the synthesis of 5-substituted 1H-tetrazoles. Out of three used Pb(II) catalysts, lead chloride (PbCl2) has been found to be an efficient catalyst for [3+2] cycloaddition of NaN3 with aromatic and aliphatic nitriles to afford 5-substituted 1H-tetrazoles. The catalyst is reusable up to four cycles with consistent activity. The cost effectiveness and easy availability of the catalyst, simple methodology, excellent yield and easy work-up are the additional advantages.
- Kant, Rama,Singh, Vishal,Agarwal, Alka
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p. 305 - 312
(2016/04/20)
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- Synthetic application of gold nanoparticles and auric chloride for the synthesis of 5-substituted 1H-tetrazoles
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An effective one-pot, convenient gold catalyzed synthesis of 5-substituted 1H-tetrazoles has been discussed. The study demonstrated the comparative overview for utilization of gold(iii) and gold nano-particles (spheres) as a catalyst. Detailed understandi
- Kumar, Satyanand,Kumar, Arvind,Agarwal, Alka,Awasthi, Satish Kumar
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p. 21651 - 21658
(2015/03/30)
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- OSU-6: A highly efficient, metal-free, heterogeneous catalyst for the click synthesis of 5-benzyl and 5-aryl-1H-tetrazoles
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OSU-6, an MCM-41 type hexagonal mesoporous silica with mild Br?nsted acid properties, has been used as an efficient, metal-free, heterogeneous catalyst for the click synthesis of 5-benzyl and 5-aryl-1H-tetrazoles from nitriles in DMF at 90 °C. This catalyst offers advantages including ease of operation, milder conditions, high yields, and reusability. Studies are presented that demonstrate the robust nature of the catalyst under the optimized reaction conditions. OSU-6 promotes the 1,3-dipolar addition of azides to nitriles without significant degradation or clogging of the nanoporous structure. The catalyst can be reused up to five times without a significant reduction in yield, and it does not require treatment with acid between reactions.
- Nammalwar, Baskar,Muddala, Nagendra Prasad,Pitchimani, Rajasekar,Bunce, Richard A.
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p. 22757 - 22766
(2016/01/25)
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- (NH4)2Ce(NO3)6 as an inexpensive, eco-friendly, efficient catalyst for the synthesis of 5-substituted 1-H tetrazoles from nitriles
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Ceric ammonium nitrate (CAN) is found to be a suitable, inexpensive, and effective non-toxic catalyst for a smooth (3+2) cycloaddition of organic nitriles with NaN3 to afford 5-substituted 1H-tetrazoles in excellent yields. Shorter reaction times, easy work-up, and substantial and pure product formation are the key advantages of the present method.
- Kumar, Satyanand,Dubey, Shristy,Saxena, Nisha,Awasthi, Satish Kumar
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p. 6034 - 6038
(2015/01/08)
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