20143-50-4Relevant academic research and scientific papers
Synthesis and analgesic activity of some 1-benzofurans, 1-benzothiophenes and indoles
Radl, Stanislav,Hezky, Petr,Urbankova, Jitka,Vachal, Petr,Krejci, Ivan
, p. 280 - 296 (2000)
3-Unsubstituted 1-benzofurans 1e and 1f, 3-methyl-1-benzofurans 1a-1d, and 3-amino-1-benzofurans 2a-21, as well as 3-amino-1-benzothiophenes 3a, 3b and 3-aminoindoles 4a-4f, 11a, and 11b were prepared and tested as analgesics. The 3-amino-1-benzofurans 2 were prepared from the corresponding 2-hydroxybenzonitriles 5 and phenacyl bromides 6 via intermediates 7. Similar treatment of 2-sulfanylbenzonitrile (8) provided 3-amino-1-benzothiophenes 3. Appropriately substituted 2-aminobenzonitriles 9 then provided N-substituted 3-aminoindoles 4. 1-(Ethoxycarbonyl)indoles 4e and 4f were successfully deprotected giving indoles 11a and 11b, respectively.
Synthesis and evaluation of some novel essential amino acid-benzofuran-acetamide/propanamide/butanamide hybrids as potential anticonvulsant agents
Kamal, Mehnaz
, p. 283 - 289 (2020/09/18)
In this study, some new essential amino acid-benzofuran-acetamide/propanamide/butanamide hybrid derivatives were synthesized. The structures of the synthesized compounds were confirmed on the basis of their elemental and spectral analyses. Their anti-seizure activity was investigated using maximal electroshock seizure (MES) and subcutaneous metrazol (scMET) seizure tests in mice. Neurotoxicity (NT) of the synthesized compounds was also determined by the rotarod test. Derivatives exhibited favorable protection in both MES and scMET tests with high safety levels in NT test. The derivatives have proven significant activity in mice and could be suggested as potential anticonvulsant lead compounds. All leucine-chlorobenzoyl benzofuran-acetamide/propanamide/ butanamide hybrid derivatives (6b, 7b, and 8b) showed significant anticonvulsant activity in MES model. Compound 8b also demonstrated potent anticonvulsant activity against scMET test. The compound 8b showed maximum activity and would be considered as a lead for further optimization as anticonvulsant agent.
Synthesis, anticonvulsant and neurotoxicity evaluation of novel n-(2-benzoylbenzofuran-3-yl)-4-(substituted) butanamides
Kamal, Mehnaz,Shakya, Ashok K.
, p. 17 - 20 (2013/12/04)
A series of N-(2-benzoylbenzofuran-3-yl)-4-(substituted) butanamides (IVa-f) were synthesized and evaluated for anticonvulsant activity and neurotoxicity. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. All the compounds was found active in MES tests. Compounds IVb, IVc, IVd and IVf were found to be potent and had activity at lower dose of 30mg/ kg in MES-test. Compounds IVa and IVe were less toxic as compared with the standard drug phenytoin.
