6008-74-8Relevant academic research and scientific papers
Novel Dithiolane-Based Ligands Combining Sigma and NMDA Receptor Interactions as Potential Neuroprotective Agents
Franchini, Silvia,Linciano, Pasquale,Puja, Giulia,Tait, Annalisa,Borsari, Chiara,Denora, Nunzio,Iacobazzi, Rosa Maria,Brasili, Livio,Sorbi, Claudia
supporting information, p. 1028 - 1034 (2020/07/21)
Sigma receptors (SRs) are recognized as valuable targets for the treatment of neurodegenerative disorders. A series of novel SRs ligands were designed by combining key pharmacophoric amines (i.e., benzylpiperidine or benzylpiperazine) with new 1,3-dithiolane-based heterocycles and their bioisosters. The new compounds exhibited a low nanomolar affinity for sigma-1 and sigma-2 receptors. Five selected compounds were evaluated for their neuroprotective capacity on SH-SY5Y neuroblastoma cell line. They were able to counteract the neurotoxicity induced by rotenone, oligomycin and NMDA. Competition studies with PB212, a S1R antagonist, confirmed the involvement of S1R in neuroprotection from the oxidative stress induced by rotenone. Electrophysiological experiments performed on cortical neurons in culture highlighted the compounds ability to reduce NMDA-evoked currents, suggesting a negative allosteric modulator activity toward the NMDA receptor. Altogether these results qualify our novel dithiolane derivatives as potential agents for fighting neurodegeneration.
Herbicidal 1-aryl-delta2-1,2,4-triazolin-5-ones
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, (2008/06/13)
Aryltriazolinones of the formula STR1 in which W is oxygen or sulfur; X1 and X2 are independently selected from halogen, haloalkyl, and alkyl; R is a three- to eight-membered ring heterocyclic group of one or two, same or different, ring heteroatoms selected from oxygen, sulfur, and nitrogen, or an alkyl radical substituted with said heterocyclic group; R1 is alkyl, haloalkyl, cyanoalkyl, alkenyl, alkynyl, or a group of the formula -alkyl-Y--R3 ; R2 is halogen, alkyl, cyanoalkyl, haloalkyl, arylalkyl, or a group of the formula -alkyl-Y--R3 ; R3 is alkyl, alkenyl, or alkynyl; and Y is oxygen or S(O)r in which r is 0 to 2 are disclosed and exemplified.
Comparative radioprotective activity of various pentagonal compounds with two heteroatomes
Robbe,Fernandez,Dubief,et al.
, p. 235 - 243 (2007/10/02)
Various heterocyclic compounds with two heteroatomes were synthesized and their potential radioprotective activity was tested. This study shows the interest of phenylthiazolidines derivatives in chemical radioprotection.
O-Ethyl-s-propyl derivatives of 1,3-dithiolan-4-yl phosphorodithioates-methyl
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, (2008/06/13)
Compounds characterized by the following formula: SPC1 Wherein R and R' can be selected from the group consisting of C1 to C15 hydrocarbyl, preferably C1 to C6 alkyl, C3 to C7 cycloalkyl, phenyl optionally substituted by chlorine, bromine, nitro, cyano, C1 to C6 alkyl, C1 to C6 alkoxy or C1 to C6 alkylthio; R and R' may form together a carbocyclic ring of from 3 to 8 carbon atoms. In addition, R can also be hydrogen. R" can be a C1 to C6 alkyl group optionally substituted by chlorine, bromine or cyano; phenyl optionally substituted by chlorine, bromine or nitro, R"' can have the same definition as R" and can be in addition a C1 to C6 alkoxy, C1 to C4 alkylthio and phenoxy optionally substituted by chlorine, bromine or nitro; X can be oxygen or sulfur. These compounds have been found to possess pesticidal activity, particularly insecticidal, miticidal and nematocidal activity.
