Identification and synthesis of [1, 2, 4] triazolo [3, 4-a] phthalazine derivatives as high-affinity ligands to the α 2 δ-1 subunit of voltage gated calcium channel

…, J Gunzner, B Wang, R Pracitto, H Schaffhauser…

Index: Lebsack, Alec D.; Gunzner, Janet; Wang, Bowei; Pracitto, Richard; Schaffhauser, Herve; Santini, Angelina; Aiyar, Jayashree; Bezverkov, Robert; Munoz, Benito; Liu, Wensheng; Venkatraman, Shankar Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 10 p. 2463 - 2467

Full Text: HTML

Citation Number: 35

Abstract

We have identified and synthesized a series of [1, 2, 4] triazolo [3, 4-a] phthalazine derivatives as high-affinity ligands to α2δ-1 subunit of voltage gated calcium channels. Structure–activity relationship studies directed toward improving the potency and physical properties of 2 lead to the discovery of 20 (IC50= 15nM) and (S)-22 (IC50= 30nM). A potent and selective radioligand,[3H]-(S)-22 was also synthesized to demonstrate that this ligand ...

Related Articles:

Synthesis and antimicrobial activities of novel 1, 2, 4-triazolo [3, 4-a] phthalazine derivatives

[Zhang, Qiu-Rong; Xue, Deng-Qi; He, Peng; Shao, Kun-Peng; Chen, Peng-Ju; Gu, Yi-Fei; Ren, Jing-Li; Shan, Li-Hong; Liu, Hong-Min Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 4 p. 1236 - 1238]

6-(Alkylamino)-3-aryl-1, 2, 4-triazolo [3, 4-a] phthalazines. A new class of benzodiazepine receptor ligands

[Tarzia, Giorgio; Occelli, Emilio; Toja, Emilio; Barone, Domenico; Corsico, Nerina; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 6 p. 1115 - 1123]

6-(Alkylamino)-3-aryl-1, 2, 4-triazolo [3, 4-a] phthalazines. A new class of benzodiazepine receptor ligands

[Tarzia, Giorgio; Occelli, Emilio; Toja, Emilio; Barone, Domenico; Corsico, Nerina; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 6 p. 1115 - 1123]

Synthesis and antimicrobial activities of novel 1, 2, 4-triazolo [3, 4-a] phthalazine derivatives

[Zhang, Qiu-Rong; Xue, Deng-Qi; He, Peng; Shao, Kun-Peng; Chen, Peng-Ju; Gu, Yi-Fei; Ren, Jing-Li; Shan, Li-Hong; Liu, Hong-Min Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 4 p. 1236 - 1238]

Synthesis and antimicrobial activities of novel 1, 2, 4-triazolo [3, 4-a] phthalazine derivatives

[Zhang, Qiu-Rong; Xue, Deng-Qi; He, Peng; Shao, Kun-Peng; Chen, Peng-Ju; Gu, Yi-Fei; Ren, Jing-Li; Shan, Li-Hong; Liu, Hong-Min Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 4 p. 1236 - 1238]

More Articles...