23753-42-6Relevant articles and documents
Activation of carbonic anhydrases from human brain by amino alcohol oxime ethers: towards human carbonic anhydrase VII selective activators
Nocentini, Alessio,Cuffaro, Doretta,Ciccone, Lidia,Orlandini, Elisabetta,Nencetti, Susanna,Nuti, Elisa,Rossello, Armando,Supuran, Claudiu T.
, p. 48 - 57 (2020/11/03)
The synthesis and carbonic anhydrase (CA; EC 4.2.1.1) activating effects of a series of oxime ether-based amino alcohols towards four human (h) CA isoforms expressed in human brain, hCA I, II, IV and VII, are described. Most investigated amino alcohol derivatives induced a consistent activation of the tested CAs, with KAs spanning from a low micromolar to a medium nanomolar range. Specifically, hCA II and VII, putative main CA targets when central nervous system (CNS) diseases are concerned, were most efficiently activated by these oxime ether derivatives. Furthermore, a multitude of selective hCA VII activators were identified. As hCA VII is one of the key isoforms involved in brain metabolism and other brain functions, the identified potent and selective hCA VII activators may be considered of interest for investigations of various therapeutic applications or as lead compounds in search of even more potent and selective CA activators.
Synthesis and β-Adrenergic Blocking Activity of New Aliphatic Oxime Ethers
Leclerc, Gerard,Bieth, Nicole,Schwartz, Jean
, p. 620 - 624 (2007/10/02)
New β-adrenergic blocking agents, most of which do not contain an aromatic nucleus, were synthesized.They were derived either from alkylamino-aliphatic oxime ethers, or alkylamino-aliphatic ethers.Most active among these are O-acetoxime (8; trachea pA2=7.65) and 1-isobutoxy-3-(tert-butylamino)-2-propanol (15, trachea pA2=7.49), both of which displayed bronchoselectivity (β2/β1 ratio ca. 15).The role and importance of the aromatic nucleus in this class of compounds are discussed
