Topic
Bicyclic molecule
About: Bicyclic molecule is a research topic. Over the lifetime, 29587 publications have been published within this topic receiving 451252 citations. The topic is also known as: bicyclic molecule.
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105 citations
TL;DR: In this paper, a synthese traitant de la synthetes catalysee par le palladium complex or Pd II (OAc) 2 d'intermediaires heterocycliques tels que des indoles, quinoleines, isoquinoleines et d'autres heterocycles oxygene- ou soufre azote
Abstract: Article de synthese traitant de la synthese catalysee par le palladium complexe ou Pd II (OAc) 2 d'intermediaires heterocycliques tels que des indoles, quinoleines, isoquinoleines et d'autres heterocycles oxygene- ou soufre azote
105 citations
Patent•
16 Mar 1993TL;DR: The pharmaceutically active bicyclic heterocyclic amines (XXX) as discussed by the authors are useful as pharmaceuticals in treating mild and/or moderate to severe head injury, subarachnoid hemorrhage and subsequent ischemic stroke, asthma and reduction of mucous formation/secretion in the lung and other diseases and injuries.
Abstract: The pharmaceutically active bicyclic heterocyclic amines (XXX), where W1 is -N= or -CH=; W3 is -N= or -CH=; W5 is -N= or -CR5- with the proviso that W5 is -CR5- when both W1 and W3 are -N= which are useful as pharmaceuticals in treating mild and/or moderate to severe head injury, subarachnoid hemorrhage and subsequent ischemic stroke, asthma and reduction of mucous formation/secretion in the lung and other diseases and injuries.
105 citations
TL;DR: A series of analogues of acyclovir and ganciclovir were prepared in which conformational constraints were imposed by incorporation of a cyclopropane ring or unsaturation into the side chain, showing significant antiherpetic activity in vitro and modest antiviral activity despite an apparent inability to be enzymatically phosphorylated.
Abstract: A series of analogues of acyclovir and ganciclovir were prepared in which conformational constraints were imposed by incorporation of a cyclopropane ring or unsaturation into the side chain. In addition, several related base-modified compounds were synthesized. These acyclonucleosides were evaluated for enzymatic phosphorylation and DNA polymerase inhibition in a staggered assay and for inhibitory activity against herpes simplex virus types 1 and 2 in vitro. Certain of the guanine or 8-azaguanine derivatives were good substrates for the viral thymidine kinase and were further converted to triphosphate, but none was a potent inhibitor of the viral DNA polymerase. Nevertheless, one member of this group, (+/-)-9-[[(Z)-2-(hydroxymethyl)cyclopropyl]methyl]guanine (3a), displayed significant antiherpetic activity in vitro, superior to that of the corresponding cis olefin 4a. Another group, typified by (+/-)-9-[[(E)-2-(hydroxymethyl)cyclopropyl]methyl]adenine (17b), possessed modest antiviral activity despite an apparent inability to be enzymatically phosphorylated. The relationship of side-chain conformation and flexibility to biological activity in this series is discussed.
105 citations
104 citations