156603-13-3Relevant academic research and scientific papers
H-Bond Self-Assembly: Folding versus Duplex Formation
Nú?ez-Villanueva, Diego,Iadevaia, Giulia,Stross, Alexander E.,Jinks, Michael A.,Swain, Jonathan A.,Hunter, Christopher A.
, p. 6654 - 6662 (2017)
Linear oligomers equipped with complementary H-bond donor (D) and acceptor (A) sites can interact via intermolecular H-bonds to form duplexes or fold via intramolecular H-bonds. These competing equilibria have been quantified using NMR titration and dilution experiments for seven systems featuring different recognition sites and backbones. For all seven architectures, duplex formation is observed for homo-sequence 2-mers (AA·DD) where there are no competing folding equilibria. The corresponding hetero-sequence AD 2-mers also form duplexes, but the observed self-association constants are strongly affected by folding equilibria in the monomeric states. When the backbone is flexible (five or more rotatable bonds separating the recognition sites), intramolecular H-bonding is favored, and the folded state is highly populated. For these systems, the stability of the AD·AD duplex is 1-2 orders of magnitude lower than that of the corresponding AA·DD duplex. However, for three architectures which have more rigid backbones (fewer than five rotatable bonds), intramolecular interactions are not observed, and folding does not compete with duplex formation. These systems are promising candidates for the development of longer, mixed-sequence synthetic information molecules that show sequence-selective duplex formation.
Substituted quinuclidines as substance P antagonists
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, (2008/06/13)
Certain novel substituted quinuclidine compounds having the ability to antagonize substance P and having the following formula: STR1 wherein Ar1 and Ar2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; X is --CONR3 R4, --CO2 R3, --CH2 OR3, --CH2 NR3 R4 or --CONR3 OR4 ; R1, R3 and R4 are each, independently, hydrogen or alkyl having 1 to 4 carbon atoms; R2 is alkyl having 1 to 4 carbon atoms; Y is alkylsulfonyl having 1 to 4 carbon atoms, N-alkyl-N-alkanoylamino (which may be substituted by halogen in the alkanoyl moiety) having 1 to 4 carbon atoms in the alkyl and the alkanoyl moieties, N-alkyl-N-alkylsulfonylamino (which may be substituted by halogen in the alkylsulfonyl moiety) having 1 to 4 carbon atoms in the alkyl and the alkyl sulfonyl moieties, alkenyl having 2 to 4 carbon atoms, alkynyl having 2 to 4 carbon atoms, halosubstituted alkyl having 1 to 4 carbon atoms, alkylamino having 1 to 4 carbon atoms, alkanoylamino (which may be substituted by halogen) having 1 to 4 carbon atoms or alkylsulfonylamino (which may be substituted by halogen) having 1 to 4 carbon atoms. These compounds are useful in the treatment gastrointestinal or central nervous system disorders and the alleviation of inflammatory diseases, asthma, pain and migraine in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
