- Biomimetic hydrogen-bonding cascade for chemical activation: telling a nucleophile from a base
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Hydrogen bonding-assisted polarization is an effective strategy to promote bond-making and bond-breaking chemical reactions. Taking inspiration from the catalytic triad of serine protease active sites, we have devised a conformationally well-defined benzimidazole platform that can be systematically functionalized to install multiple hydrogen bonding donor (HBD) and acceptor (HBA) pairs in a serial fashion. We found that an increasing number of interdependent and mutually reinforcing HBD-HBA contacts facilitate the bond-forming reaction of a fluorescence-quenching aldehyde group with the cyanide ion, while suppressing the undesired Br?nsted acid-base reaction. The most advanced system, evolved through iterative rule-finding studies, reacts rapidly and selectively with CN- to produce a large (>180-fold) enhancement in the fluorescence intensity at λmax = 450 nm.
- Park, Hyunchang,Lee, Dongwhan
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p. 590 - 598
(2021/01/28)
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- NEW PYRIDOPYRIMIDINES DERIVATIVES COMPOUNDS
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The present invention describes new pyridopyrimidine derivatives compounds with structure represented by General Formula (I): or pharmaceutically acceptable salts thereof, or their mixtures (in any ratio), a pharmaceutical composition containing them, a method for using the new pyridopyrimidine derivatives compounds as inhibitor of the cyclic nucleotide synthesis or as inhibitor of the cAMP and cGMP synthesis, and their uses in the prophylactic and/or curative treatment of diarrhea, colitis and irritable bowel syndrome.
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Paragraph 0117-0120
(2016/04/09)
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- An original way for synthesis of new nitro-benzothiadiazole derivatives
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The C-alkylation reaction of 4-chloromethyl-7-nitro-2,1,3-benzothiadiazole with 2-nitropropane anion which is shown to proceed by an SRN1 mechanism is an original way for the synthesis of new 2,1,3-benzothiadiazoles.
- Vanelle, Patrice,Liegeois, Celine Tremblais,Meuche, Jacobine,Maldonado, Jose,Crozet, Michel P.
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p. 955 - 962
(2007/10/03)
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- Synthesis of a new type of "bent" heterocyclic benzimidazolo-pyridazinones
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The synthesis of some new heterocyclic benzimidazolo-pyridazinines starting from 2,1,3-benzothiadiazole-4-carboxaldehyde 2 is described.Biological evaluation of all new compounds proved them to be inhibitors of phosphodiesterase III with no marked positiv
- Jonas, R,Pruecher, H,Wurziger, H
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p. 141 - 148
(2007/10/02)
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