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1973 1
1983 1
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A systematic exploration of boceprevir-based main protease inhibitors as SARS-CoV-2 antivirals.
Alugubelli YR, Geng ZZ, Yang KS, Shaabani N, Khatua K, Ma XR, Vatansever EC, Cho CC, Ma Y, Xiao J, Blankenship LR, Yu G, Sankaran B, Li P, Allen R, Ji H, Xu S, Liu WR. Alugubelli YR, et al. Eur J Med Chem. 2022 Oct 5;240:114596. doi: 10.1016/j.ejmech.2022.114596. Epub 2022 Jul 8. Eur J Med Chem. 2022. PMID: 35839690 Free PMC article.
A unique observation was made with an inhibitor that contains a P4 N-terminal isovaleramide. In its M(Pro) complex structure, the P4 N-terminal isovaleramide is tucked deep in a small pocket of M(Pro) that originally recognizes a P4 alanine side chain in a substrate …
A unique observation was made with an inhibitor that contains a P4 N-terminal isovaleramide. In its M(Pro) complex structure, the P4 …
New antiepileptic drugs that are second generation to existing antiepileptic drugs.
Bialer M. Bialer M. Expert Opin Investig Drugs. 2006 Jun;15(6):637-47. doi: 10.1517/13543784.15.6.637. Expert Opin Investig Drugs. 2006. PMID: 16732716 Review.
This article focuses on the second category and thus critically reviews the following second-generation compounds: eslicarbazepine acetate or BIA-2-093 and 10-hydroxy carbazepine (carbamazepine derivatives); valrocemide and NPS 1776 (isovaleramide; valproic acid derivative …
This article focuses on the second category and thus critically reviews the following second-generation compounds: eslicarbazepine acetate o …
Diverse mechanisms of antiepileptic drugs in the development pipeline.
Rogawski MA. Rogawski MA. Epilepsy Res. 2006 Jun;69(3):273-94. doi: 10.1016/j.eplepsyres.2006.02.004. Epub 2006 Apr 18. Epilepsy Res. 2006. PMID: 16621450 Free PMC article. Review.
Follow-on agents include the levetiracetam analogs brivaracetam and seletracetam that act as SV2A-ligands; the valproate-like agents valrocemide, valnoctamide, propylisopropyl acetamide, and isovaleramide; the felbamate analog flurofelbamate, a dicarbamate, and the unrelat …
Follow-on agents include the levetiracetam analogs brivaracetam and seletracetam that act as SV2A-ligands; the valproate-like agents valroce …
The N -Terminal Carbamate is Key to High Cellular and Antiviral Potency for Boceprevir-Based SARS-CoV-2 Main Protease Inhibitors.
Alugubelli YR, Geng ZZ, Yang KS, Shaabani N, Khatua K, Ma XR, Vatansever EC, Cho CC, Ma Y, Blankenship L, Yu G, Sankaran B, Li P, Allen R, Ji H, Xu S, Liu WR. Alugubelli YR, et al. bioRxiv [Preprint]. 2021 Dec 21:2021.12.18.473330. doi: 10.1101/2021.12.18.473330. bioRxiv. 2021. PMID: 34981058 Free PMC article. Preprint.
A unique observation was made with an inhibitor that contains an P4 N -terminal isovaleramide. In its M (Pro) complex structure, the P4 N -terminal isovaleramide is tucked deep in a small pocket of M (Pro) that originally recognizes a P4 alanine side chain in a subs …
A unique observation was made with an inhibitor that contains an P4 N -terminal isovaleramide. In its M (Pro) complex structure, the …
Inhibition by carboxamides and sulfoxides of liver alcohol dehydrogenase and ethanol metabolism.
Chadha VK, Leidal KG, Plapp BV. Chadha VK, et al. J Med Chem. 1983 Jun;26(6):916-22. doi: 10.1021/jm00360a024. J Med Chem. 1983. PMID: 6343601
The most promising compounds, tetramethylene sulfoxide and isovaleramide, were essentially uncompetitive inhibitors of purified horse and rat liver alcohol dehydrogenases with respect to ethanol as substrate. ...The differences in the values may be due to metabolism or dis …
The most promising compounds, tetramethylene sulfoxide and isovaleramide, were essentially uncompetitive inhibitors of purified horse …
New CNS-active drugs which are second-generation valproic acid: can they lead to the development of a magic bullet?
Isoherranen N, Yagen B, Bialer M. Isoherranen N, et al. Curr Opin Neurol. 2003 Apr;16(2):203-11. doi: 10.1097/01.wco.0000063774.81810.30. Curr Opin Neurol. 2003. PMID: 12644750 Review.
SUMMARY: At present there are three compounds in clinical trials in patients with epilepsy that can be regarded as second-generation VPA: valproyl glycinamide, 3-methylbutanamide or isovaleramide and SPD421 (DP-VPA). For any one of these second-generation valproic acids to …
SUMMARY: At present there are three compounds in clinical trials in patients with epilepsy that can be regarded as second-generation VPA: va …
[Isovaleramide, an anticonvulsant molecule isolated from Valeriana pavonii].
Giraldo SE, Rincón J, Puebla P, Marder M, Wasowski C, Vergel N, Guerrero MF. Giraldo SE, et al. Biomedica. 2010 Apr-Jun;30(2):245-50. Biomedica. 2010. PMID: 20890571 Spanish.
OBJECTIVE: Description of the isolation and identification of isovaleramide, an active principle on central nervous system from Valeriana pavonii. ...CONCLUSION: Isovaleramide is one of the active anticonvulsant constituents of Valeriana pavonii, for the first time …
OBJECTIVE: Description of the isolation and identification of isovaleramide, an active principle on central nervous system from Valer …
Could valerian have been the first anticonvulsant?
Eadie MJ. Eadie MJ. Epilepsia. 2004 Nov;45(11):1338-43. doi: 10.1111/j.0013-9580.2004.27904.x. Epilepsia. 2004. PMID: 15509234 Free article.
Valerian preparations yield isovaleric acid, a substance analogous to valproic acid and likely to possess anticonvulsant properties, as isovaleramide does. In favorable circumstances, high valerian doses can be calculated to have sometimes provided potentially effective am …
Valerian preparations yield isovaleric acid, a substance analogous to valproic acid and likely to possess anticonvulsant properties, as i …
Synthesis of N4-(2-acetamido-2-deoxy-beta-D-glucopyranosyl)-L-asparagine analogues. n-Butyramide, 3-chloropropionamide, 3-aminopropionamide, and isovaleramide analogues.
Kaylor JJ, Risley JM. Kaylor JJ, et al. Carbohydr Res. 2001 Apr 23;331(4):439-44. doi: 10.1016/s0008-6215(01)00057-x. Carbohydr Res. 2001. PMID: 11398986
Succinimidyl isovalerate was synthesized and gave N-(2-acetamido-2-deoxy-beta-D-glucopyranosyl)-isovaleramide....
Succinimidyl isovalerate was synthesized and gave N-(2-acetamido-2-deoxy-beta-D-glucopyranosyl)-isovaleramide....
Temperature dependence of nonelectrolyte permeation across red cell membranes.
Galey WR, Owen JD, Solomon AK. Galey WR, et al. J Gen Physiol. 1973 Jun;61(6):727-46. doi: 10.1085/jgp.61.6.727. J Gen Physiol. 1973. PMID: 4708405 Free PMC article.
The temperature dependence of permeation across human red cell membranes has been determined for a series of hydrophilic and lipophilic solutes, including urea and two methyl substituted derivatives, all the straight-chain amides from formamide through valeramide and the two isom …
The temperature dependence of permeation across human red cell membranes has been determined for a series of hydrophilic and lipophilic solu …
11 results