- Design and synthesis of novel sulfonamide-containing bradykinin hB 2 receptor antagonists. Synthesis and structure-relationships of α,α-tetrahydropyranylglycine
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A series of α,α-cycloalkylglycine sulfonamide compounds of general formula 1 has previously been identified by our group as selective human B2(hB2) receptor antagonists. Here we report the in vitro and in vivo BK antagonist activity
- Fincham, Christopher I.,Bressan, Alessandro,D'Andrea, Piero,Ettorre, Alessandro,Giuliani, Sandro,Mauro, Sandro,Meini, Stefania,Paris, Marielle,Quartara, Laura,Rossi, Cristina,Squarcia, Antonella,Valenti, Claudio,Daniela, Fattori,Maggi, Carlo Alberto
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supporting information; experimental part
p. 2091 - 2100
(2012/05/05)
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- Dihydropyridine derivatives as bradykinin antagonist
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Compound of formula (1) and their pharmaceutically acceptable salts wherein A1,A2,R1, R2,R3,R4,X are as defined in the specification have excellent bradykinin antagonistic activity. STR1
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- Anti-leishmanial lepidine derivatives
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The subject 8-[6-(N-heterocyclic-substituted)hexylamino]-6-methoxy lepidineerivatives have the formula: STR1 wherein Z represents methyl or, together with the two contiguous carbon atoms, the benzo moiety of a benzopiperazinyl derivative when Y is --N(R')--, n is an integer from 0 to 2; Y represents --O--, --S--, --S(O)--, --S(O)2 --, and --N(R')--; R' represents hydrogen, alkyl, lower alkyl, R" substituted lower alkyl, cycloalkyl, aryl, sulfonyl, saturated 1,4-diazepinyl, lower alkyl N-cyanocarboximidothioate, or --C(O)R'"; R" represents at least one of hydroxy, alkoxy, aralkoxy, amino, lower alkyl substituted amino, phenyl, halogenated phenyl, or sufonyl; and R'" represents lower alkyl, alkoxy, aralkoxy, amino, lower alkyl substituted amino or aryl substituted amino; and pharmaceutically acceptable salts thereof. These derivatives afford improvement in means for the chemotherapy of leishmaniasis when administered parenterally or orally to infected animals.
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