e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521

Thiadiazole carbamates: potent inhibitors of lysosomal acid lipase and potential Niemann− Pick type C disease therapeutics

AI Rosenbaum, CC Cosner, CJ Mariani…

Index: Rosenbaum, Anton I.; Cosner, Casey C.; Mariani, Christopher J.; Maxfield, Frederick R.; Wiest, Olaf; Helquist, Paul Journal of Medicinal Chemistry, 2010 , vol. 53, # 14 p. 5281 - 5289

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Citation Number: 34

Abstract

Niemann− Pick type C (NPC) disease is a lysosomal storage disorder characterized at the cellular level by abnormal accumulation of cholesterol and other lipids in lysosomal storage organelles. Lysosomal acid lipase (LAL) has been recently identified as a potential therapeutic target for NPC. LAL can be specifically inhibited by a variety of 3, 4-disubstituted thiadiazole carbamates. An efficient synthesis of the C (3) oxygenated/C (4) aminated ...

2-(4-morpholinyl)-2-(N,N-bis(trimethylsilyl)aminothio)iminoacetonitrile Structure

2-(4-morpholiny...

ethyl acetate Structure

~%

N/A Structure

Ethyl acetoacetate Structure

Ethyl acetoacetate

Azepane Structure

3,4-Dichloro-1,2,5-thiadiazole Structure

3,4-Dichloro-1,...

~95%

1-(4-chloro-1,2,5-thiadiazol-3-yl)azepane Structure

1-(4-chloro-1,2...

Methyl propanoate Structure

Methyl propanoate

2-(4-morpholinyl)-2-(N,N-bis(trimethylsilyl)aminothio)iminoacetonitrile Structure

2-(4-morpholiny...

~%

Methyl 2-methyl-3-oxopentanoate Structure

Methyl 2-methyl...

N/A Structure

3-Chloro-4-morpholino-1,2,5-thiadiazole Structure

3-Chloro-4-morp...

~91%

4-morpholino-1,2,5-thiadiazol-3-ol Structure

4-morpholino-1,...

Simple, fast and efficient synthesis of β-keto esters from t...

[Venkat Ragavan; Vijayakumar; Rajesh; Palakshi Reddy; Karthikeyan; Suchetha Kumari Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 12 p. 4193 - 4197]

Simple, fast and efficient synthesis of β-keto esters from t...

[Venkat Ragavan; Vijayakumar; Rajesh; Palakshi Reddy; Karthikeyan; Suchetha Kumari Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 12 p. 4193 - 4197]

Simple, fast and efficient synthesis of β-keto esters from t...

[Venkat Ragavan; Vijayakumar; Rajesh; Palakshi Reddy; Karthikeyan; Suchetha Kumari Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 12 p. 4193 - 4197]

Simple, fast and efficient synthesis of β-keto esters from t...

[Venkat Ragavan; Vijayakumar; Rajesh; Palakshi Reddy; Karthikeyan; Suchetha Kumari Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 12 p. 4193 - 4197]

Simple, fast and efficient synthesis of β-keto esters from t...

[Venkat Ragavan; Vijayakumar; Rajesh; Palakshi Reddy; Karthikeyan; Suchetha Kumari Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 12 p. 4193 - 4197]