40575-74-4Relevant academic research and scientific papers
CONTROLLED RELEASE OF BIOLOGICALLY ACTIVE COMPOUNDS
-
, (2009/04/24)
The present invention relates to biodegradable polymers (e.g., polyesters and polyester amides) derived from functionalized biologically active compounds that can provide site specific delivery of bioactive compounds upon biodegradation in a controlled manner.
FUNCTIONALIZED PHENOLIC COMPOUNDS AND POLYMERS THEREFROM
-
Page/Page column 35; 37, (2009/07/17)
The present invention relates to compounds of formula I, which are functionalized phenolic compounds, and polymers formed from the same. Ar—[O—(X)p—R′]q??I Polymers formed from the functionalized phenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
Synthesis of potential antidipsotropic isoflavones: Inhibitors of the mitochondrial monoamine oxidase - Aldehyde dehydrogenase pathway
Gao,Li,Ming Keung
, p. 3320 - 3328 (2007/10/03)
Recently we have shown that daidzin, the major active principle of an ancient herbal treatment for quot;alcohol addictionquot; suppresses ethanol intake in alcohol-preferring laboratory animals. Further, we have identified the monoamine oxidase (MAO) - aldehyde dehydrogenase (ALDH-2) pathway of the mitochondria as the potential site of action of daidzin. Daidzin analogues that potently inhibit ALDH-2 but have no or little effect on MAO are most antidipsotropic, whereas those that also inhibit MAO exhibit little, if any, antidipsotropic activity. Therefore, in the design and synthesis of more potent antidipsotropic analogues, structural features important for the inhibition of both ALDH-2 and MAO must be taken into consideration. To gain further information on the structure-activity relationships at the inhibitor binding sites of ALDH-2 and MAO, we prepared 44 analogues of daidzin and determined their potencies for ALDH-2 and MAO inhibition. Results indicate that a sufficient set of criteria for a potent antidipsotropic analogue is an isoflavone with a free 4′-OH function and a straight-chain alkyl substituent at the 7 position that has a terminal polar function such as -OH, -COOH, or -NH2. The preferable chain lengths for the 7-O-ω-hydroxy, 7-O-ω-carboxy, and 7-O-ω-amino subsitutents are 2 ≤ n ≤ 6, 5 ≤ n ≤ 10, and n ≥ 4, respectively. Analogues that meet these criteria have increased potency for ALDH-2 inhibition and/or decreased potency for MAO inhibition and therefore are likely to be potent antidipsotropic agents.
