6319-96-6Relevant articles and documents
PRODRUGS OF ABIRATERONE
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Page/Page column 30-31, (2021/05/29)
The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers, or pharmaceutically acceptable salt(s) thereof as prodrugs of abiraterone. The present invention also describes method of making such compounds, pharmaceutical compositions comprising such compounds and the use of the compounds of formula (I).
One-pot synthesis of phenylseleno N-acetyl α-amino acids: Supra-molecular self-assembling in organoselenium compounds
Parashiva Prabhu,Phadnis, Prasad P.,Wadawale, Amey,Priyadarsini, K. Indira,Jain, Vimal K.
, p. 140 - 147 (2013/10/01)
A convenient one-pot synthesis of phenylseleno N-acetyl α-amino acids, PhSeCH2C(O)NHC(R)COOH (R = H (1), Me (2), PhCH2 (3), 4-HOC6H4CH2 (4) and CH2OH (5)) is reported. These compounds have been characterized by microanalyses, UV-Vis, IR and NMR (1H, 13C, 77Se) spectroscopy. The molecular structures of [PhSeCH2CONHCH2COOH] (1), [PhSeCH2CONHCH(CH2C6H4OH-4)COOH] (4) and [PhSeCH2CONHCH(CH2OH)COOH] (5) have been established by X-ray diffraction analyses. These compounds are associated in the solid state through hydrogen bonding to give supra-molecular self-assembled structures. Free radical scavenging activity of these compounds has also been evaluated by DPPH assay.
7-Oxabicycloheptyl Carboxylic Acids as Thromboxane A2 Antagonists: Aza ω-Chain Analogues
Nakane, Masami,Reid, Joyce A.,Han, Wen-Ching,Das, Jagabandhu,Truc, Vu Chi,et al.
, p. 2465 - 2476 (2007/10/02)
A novel bicyclic prostaglandin analogue, >-7-acetyl>amino>methyl>-7-oxabicyclohept-2-yl>-5-heptenoic acid ((-)-7) was found to be a potent and selective thromboxane A2 (TxA2) receptor antagonist.Unlike the related series of ω-chain allylic alcohols, amide 7 and its congeners were uniformly free of direct contractile activity in vitro (bovine coronary) and in vivo (anesthetized guinea pig).Amide 7 was effective in the inhibition of (a) arachidonic acid induced platelet aggregation of human platelet-richplasma (I50 = 0.18 +/- 0.006 μM), (b) 11,9-epoxymethano-PGH2 induced platelet aggregation of human platelet-rich plasma (I50 = 0.24 μM), (c) 11,9-epoxymethano-PGH2 induced contraction of guinea pig trachea (Kb = 3.0 +/- 0.3 nM) or rat aorta (Kb = 8.8 +/- 1.1 nM), and (d) arachidonic acid induced bronchoconstriction in the anesthetized guinea pig (0.1-1.0 mg/kg iv).Amide 7 inhibited the binding of ->-7-hydrazino>methyl>-7-oxabicyclohept-2-yl>-5-heptenoic acid to human platelet membranes in a specific and saturable manner with a Kd = 49.6 +/- 1.4 nM.