| Title : The first total synthesis of (+\/-)-cyclophostin and (+\/-)-cyclipostin P: inhibitors of the serine hydrolases acetyl cholinesterase and hormone sensitive lipase - Malla_2011_Org.Lett_13_3094 |
| Author(s) : Malla RK , Bandyopadhyay S , Spilling CD , Dutta S , Dupureur CM |
| Ref : Org Lett , 13 :3094 , 2011 |
|
Abstract :
Cyclophostin, a structurally unique and potent naturally occurring acetyl cholinesterase (AChE) inhibitor, and its unnatural diastereomer were prepared in 6 steps and 15% overall yield from hydroxymethyl butyrolactone. The unnatural diastereomer of cyclophostin was converted into cyclipostin P, a potent naturally occurring hormone sensitive lipase (HSL) inhibitor, using a one pot dealkylation-alkylation process. The inhibition [IC(50)] of human AChE by cyclophostin and its diastereomer are reported, as well as constituent binding (K(I)) and reactivity (k(2)) constants. |
| PubMedSearch : Malla_2011_Org.Lett_13_3094 |
| PubMedID: 21591624 |
| Inhibitor | Cyclophostin Cyclipostin Cyclipostin-P |
Malla RK, Bandyopadhyay S, Spilling CD, Dutta S, Dupureur CM (2011)
The first total synthesis of (+\/-)-cyclophostin and (+\/-)-cyclipostin P: inhibitors of the serine hydrolases acetyl cholinesterase and hormone sensitive lipase
Org Lett
13 :3094
Malla RK, Bandyopadhyay S, Spilling CD, Dutta S, Dupureur CM (2011)
Org Lett
13 :3094