5906-30-9Relevant articles and documents
DUAL ACTION CARBONIC ANHYDRASE INHIBITORS
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Page/Page column 77, (2015/03/13)
The present invention is directed to novel carbonic anhydrase IX inhibitors comprising a nitroimidazole moiety substituted with a heterocycle or phosphinate and having sulfonamide, sulfamate or sulfamide groups. The present invention is also related to the use of these novel carbonic anhydrase IX inhibitors in cancer treatment, especially radiotherapy and chemotherapy and the use in treatment of infections.
Insertion of an aspartic acid moiety into cyclic pseudopeptides: Synthesis and biological characterization of potent antagonists for the human tachykinin NK-2 receptor
Fedi, Valentina,Altamura, Maria,Balacco, Giuseppe,Canfarini, Franca,Criscuoli, Marco,Giannotti, Danilo,Giolitti, Alessandro,Giuliani, Sandro,Guidi, Antonio,Harmat, Nicholas J. S.,Nannicini, Rossano,Pasqui, Franco,Patacchini, Riccardo,Perrotta, Enzo,Tramontana, Manuela,Triolo, Antonio,Maggi, Carlo Alberto
, p. 6935 - 6947 (2007/10/03)
A new series of monocyclic pseudopeptide tachykinin NK-2 receptor antagonists has been derived from the lead compound MEN11558. A synthesis for these molecules sharing the same intermediate was designed and performed. The replacement of the succinic moiety with an aspartic acid and the functionalization of its amino group with a wide variety of substituents led to very potent and selective NK-2 antagonists. Best results were obtained through the insertion in position 12 of an amino group with R configuration, linked by a short spacer to a saturated nitrogen heterocycle (morpholine, piperidine, or piperazine). The study led to compounds 54 and 57, endowed with high in vivo potency at very low doses and long duration of action in animal models of bronchoconstriction. In particular 54 and 57 completely inhibited NK-2 agonist induced bronchoconstriction in guinea pig after intratracheal administration at subnanomolar doses (ED50 = 0.27 nmol/kg and 0.15 nmol/kg, respectively).
C-Piperazino-pyridine sulfonamides
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, (2008/06/13)
This invention relates to compounds of the formula: SPC1 Wherein R1 in the 3- or 5-position is preferably a substituted sulfonamido or a carboxamido group whereas R2 in the 2-, 4- or 6-position is preferably an alkyl- or hydroxyalkyl-piperazinyl group. Said compounds may be used as anti-inflammatory and cardiovascular agents.