- Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors α/γ dual agonists
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PPARs are transcription factors that govern lipid and glucose homeostasis and play a central role in cardiovascular disease, obesity, and diabetes. Thus, there is significant interest in developing new agonists for these receptors. Given that the introduc
- Fracchiolla, Giuseppe,Laghezza, Antonio,Piemontese, Luca,Parente, Mariagiovanna,Lavecchia, Antonio,Pochetti, Giorgio,Montanari, Roberta,Giovanni, Carmen Di,Carbonara, Giuseppe,Tortorella, Paolo,Novellino, Ettore,Loiodice, Fulvio
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experimental part
p. 2141 - 2151
(2012/05/05)
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- Carboxylic acids and skeletal muscle chloride channel conductance: Effects on the biological activity induced by the introduction of an aryloxyalkyl group α to the carboxylic function of 4-chloro-phenoxyacetic acid
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2-(4-Chloro-phenoxy)propanoic and 2-(4-chloro-phenoxy)butanoic acids are compounds known to block chloride membrane conductance in rat striated muscle by interaction with a specific receptor. In the present study, a series of chiral analogues has been prepared and tested to evaluate the influence of a second aryloxy moiety introduced in the side-chain at a variable distance from the stereogenic centre. The results show that this chemical modification is detrimental for biological activity which, however, is increased by lengthening the alkyl chain up to three methylenic groups, then decreases to remain constant in the next analogues of the series. A possible explanation for this is proposed on the basis of steric effects and/or different approach of the molecules to the receptor.
- Carbonara, Giuseppe,Fracchiolla, Giuseppe,Loiodice, Fulvio,Tortorella, Paolo,Conte-Camerino, Diana,De Luca, Annamaria,Liantonio, Antonella
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p. 749 - 754
(2007/10/03)
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- Compounds having one or more aminosulfaonyloxy radicals useful as pharmaceuticals
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Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O) 2 NR 1 R 2 ] zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O) 2 NR 1 R 2 groups and is always at least one; R 1 and R 2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.
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- POTENTIAL CEREBRAL STIMULANTS: ESTERS OF 2-DIMETHYLAMINOETHANOL WITH SOME LIPOPHILIC CARBOXYLIC ACIDS
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2-Dimethylaminoethyl esters of 2,2-dimethylpropanoic, heptanoic, octanoic, decanoic, hexadecanoic, cyclopentylacetic, cycloheptylacetic, 2-cyclopenthylhexanoic, (4-chlorophenoxy)fumaric, and 2-(4-chlorophenoxy)succinic acid were prepared by reactions of the acid chlorides with 2-dimethylaminoethanol and were transformed to crystalline salts for pharmacological testing.The ester IX (hydrogen fumarate VUFB-14005) was found to antagonize significantly halothan amnesia in rats and the ester X (hydrogen fumarate VUFB-14004) proved to be an anticholinergic spasmolytic agent.
- Protiva, Miroslav,Valenta, Vladimir,Kopicova, Zdenka,Lukac, Juraj,Holubek, Jiri,Krejci, Ivan
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p. 1278 - 1289
(2007/10/02)
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