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K2S2O8-mediated aerobic oxidative coupling of 6-amino-7-(aminomethyl)-thiazolino-pyridones with aldehydes : Direct access to highly functionalized pyrimidine fused thiazolino-2-pyridones with amyloid fibril binding activity or inhibitors of Amyloid-β fibril formation

Bharate, Jaideep B. (author)
Fredrik Almqvist
Ådén, Jörgen, 1980- (author)
Umeå universitet,Kemiska institutionen
Gharibyan, Anna (author)
Umeå universitet,Institutionen för medicinsk kemi och biofysik
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Adolfsson, Dan E., 1989- (author)
Umeå universitet,Kemiska institutionen,Fredrik Almqvist
Jayaweera, Sanduni Wasana (author)
Anders Olofsson
Vielfort, Katarina (author)
Umeå universitet,Umeå Centre for Microbial Research (UCMR),Institutionen för molekylärbiologi (Medicinska fakulteten),Molekylär Infektionsmedicin, Sverige (MIMS),Sven Bergström
Singh, Pardeep (author)
Umeå universitet,Kemiska institutionen
Tyagi, Mohit (author)
Bergström, Sven (author)
Umeå universitet,Institutionen för molekylärbiologi (Medicinska fakulteten)
Olofsson, Anders, 1970- (author)
Umeå universitet,Institutionen för medicinsk kemi och biofysik
Almqvist, Fredrik (author)
Umeå universitet,Kemiska institutionen,Umeå Centre for Microbial Research (UCMR),Molekylär Infektionsmedicin, Sverige (MIMS)
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English.
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Abstract Subject headings
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  • We herein present the synthesis of diversely functionalized pyrimidine fused thiazolino-2-pyridones via K2S2O8-mediated oxidative coupling of 6-amino-7-(aminomethyl)- thiazolino-2-pyridones with aldehydes. The developed protocol is mild, has wide substrate scope, and does not require transition metal catalyst or base. Some of the synthesized compounds have the ability to inhibit the formation of Amyloid-β fibrils associated with Alzheimer's disease, while others bind to mature Amyloid-β and α-Synuclein fibrils.

Subject headings

NATURVETENSKAP  -- Kemi -- Organisk kemi (hsv//swe)
NATURAL SCIENCES  -- Chemical Sciences -- Organic Chemistry (hsv//eng)

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