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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TL;DR: The palladium-promoted cyclization of allyl ethers to benzofurans has been studied in this paper, where palladium is used to speed up the cyclization process.
74 citations
TL;DR: The combination of Cp 2 TiCl 2 with 2 equiv of EtMgBr provides an effective reagent for the reductive cyclization of enynes, including ester-containing ennes, to bicyclic titanacyclopentenes as discussed by the authors.
Abstract: The combination of Cp 2 TiCl 2 with 2 equiv of EtMgBr provides an effective reagent for the reductive cyclization of enynes, including ester-containing enynes, to bicyclic titanacyclopentenes. These metallacycles may then be transformed into bicyclic cyclopentenones or iminocyclopentens in good yields by reaction with CO or an isocyanide, respectively
74 citations
TL;DR: Using a combination of quantitative proteomics and whole genome sequencing of susceptible and drug-resistant parasites, a putative NAD(P)H oxidase is identified as the activating nitroreductase (NTR2) and NTR2 is necessary and sufficient for activation of these bicyclic nitro- drugs.
Abstract: Drug discovery pipelines for the "neglected diseases" are now heavily populated with nitroheterocyclic compounds. Recently, the bicyclic nitro-compounds (R)-PA-824, DNDI-VL-2098 and delamanid have been identified as potential candidates for the treatment of visceral leishmaniasis. Using a combination of quantitative proteomics and whole genome sequencing of susceptible and drug-resistant parasites we identified a putative NAD(P)H oxidase as the activating nitroreductase (NTR2). Whole genome sequencing revealed that deletion of a single cytosine in the gene for NTR2 that is likely to result in the expression of a non-functional truncated protein. Susceptibility of leishmania was restored by reintroduction of the wild-type gene into the resistant line, which was accompanied by the ability to metabolise these compounds. Overexpression of NTR2 in wild-type parasites rendered cells hyper-sensitive to bicyclic nitro-compounds, but only marginally to the monocyclic nitro-drugs, nifurtimox and fexinidazole sulfone, known to be activated by a mitochondrial oxygen-insensitive nitroreductase (NTR1). Conversely, a double knockout NTR2 null cell line was completely resistant to bicyclic nitro-compounds and only marginally resistant to nifurtimox. Sensitivity was fully restored on expression of NTR2 in the null background. Thus, NTR2 is necessary and sufficient for activation of these bicyclic nitro-drugs. Recombinant NTR2 was capable of reducing bicyclic nitro-compounds in the same rank order as drug sensitivity in vitro. These findings may aid the future development of better, novel anti-leishmanial drugs. Moreover, the discovery of anti-leishmanial nitro-drugs with independent modes of activation and independent mechanisms of resistance alleviates many of the concerns over the continued development of these compound series.
74 citations
Patent•
21 Sep 1987TL;DR: A curable thiol-ene formulation comprising polythiol and a poly-ene compound having a plurality of groups of the formula is described in this paper, where Q is CH 2, CHCH 3, C(Ch 3 ) 2, O, S, NR 1 or SO 2 R 1 is H or alkyl, and m is 0-10.
Abstract: A curable thiol-ene formulation comprising (a) a polythiol (b) a 'ene compound having a plurality of groups of the formula: ##STR1## where Q is CH 2 , CHCH 3 , C(Ch 3 ) 2 , O, S, NR 1 or SO 2 R 1 is H or alkyl, and m is 0-10, and (c) an effective amount of a free radical initiator.
74 citations
TL;DR: In this article, the acidite thermodynamique du tetracarbonyl phosphine carbene complexes is analyzed. And the reaction of tetrac-baronyl-phosphine-carbene complexes with carbenes is shown to be 6 fois moins important than celle du (methoxymethylmethylene) pentacaronylchrome.
Abstract: L'acidite thermodynamique du (methoxymethylmethylene)tetracarbonyl(tributylphosphine) chrome est 6 fois moins importante que celle du (methoxymethylmethylene) pentacarbonylchrome. On etudie quelques reactions de tetracarbonyl phosphine carbene complexes parmi lesquelles la benzannelation avec des acetyleniques, la reaction d'acetyleniques avec des complexes alkylsubstitues pour donner des vinylcetenes stables, et une annelation avec l'heptadiyne-1,6 qui conduit a des bicyclo [4.3.0] nonadienones-2
74 citations