2,639 research outputs found
The glycine reuptake inhibitor Org 25935 decreases ethanol intake and preference in male wistar rats
No full textPrevious findings from our group indicate that accumbal glycine receptors (GlyRs) are involved in mediating the dopamine (DA) activating effects of ethanol (EtOH), and that administration of glycine locally into the nucleus accumbens (nAc) reduces EtOH consumption in EtOH high-preferring rats. AIMS: The present study examines the influence of a systemically administered glycine reuptake inhibitor, Org 25935, on EtOH preference and intake, in male Wistar rats with an EtOH preference >60% (during continuous access to a bottle of EtOH, 6% v/v, and a bottle of water), called EP>60 rats, as well as in animals with an EtOH preference 60 and EP<60 rats were limited to drink 2.5 h/day. Org 25935 or vehicle was administered intraperitoneally approximately 40 min before the rats were presented to a choice of drinking EtOH or water. RESULTS: Org 25935 decreased EtOH intake and EtOH preference, as compared with vehicle, whereas water intake was unaffected. This effect was dose-dependent, developed gradually and was sustained for up to 40 days, also after introduction of an alcohol deprivation period. CONCLUSION: It is suggested that Org 25935, and possibly also other GlyT1 inhibitors, can represent a new pharmacological treatment principle for alcohol dependence or abuse
The Pipeline of Enrichment: Supporting Link Creation for Continuous Media
No full textThe application of open hypermedia to temporal media has previously been explored with respect to the link service, in particular link delivery and generic linking. This paper is based on the notion of continuous metadata, in which we use metadata in a temporally significant manner to capture and convey the information required to support linking. With a focus on link creation and live processing, our approach enriches hypermedia content with additional metadata at a number of points between capture and delivery. We illustrate this approach with a tool which assists metadata capture by annotation of continuous media according to a simple ontology
Arylchlorocarbenes in the synthesis of heterocycles containing two nitrogen atoms
No full textSubstituted pyrazoles and pyrrolo[1,2-c]pyrimidines were prepared from the reaction of arylchlorocarbenes with 1,2-diazabuta-1,3-dienes and 4-vinylpyrimidines, respectively.PT: J; CR: ATTANASI A, 1998, J ORG CHEM, V63, P9880 ATTANASI OA, 1977, SYNLETT, P1128 ATTANASI OA, 1999, TETRAHEDRON LETT, V40, P3891 BONINI BF, 1981, J CHEM SOC P1, P2322 BONNEAU R, 1999, J PHOTOCH PHOTOBIO A, V126, P31 GRAHAM WH, 1965, J AM CHEM SOC, V87, P4396 KUEHNE ME, 1964, J ORG CHEM, V29, P1582 LIU MTH, 1994, INT J CHEM KINET, V26, P1179 MAIBORODA DA, 1997, J ORG CHEM, V62, P7100 MINGUEZ JM, 1996, J ORG CHEM, V61, P4655 MOYANO EL, 1998, J ORG CHEM, V63, P8188 OVERBERGER CG, 1954, J AM CHEM SOC, V76, P1879 PERKAMPUS HH, 1972, TETRAHEDRON, V28, P2099 ROMASHIN YN, 1999, CHEM COMMUN 0307, P447 ROMASHIN YN, 1999, TETRAHEDRON LETT, V40, P7163 WONG JL, 1965, J ORG CHEM, V30, P2398; NR: 16; TC: 6; J9: CHEM COMMUN; PG: 2; GA: 324XFSource type: Electronic(1
A general approach to indolizidine alkaloids from 1-benzyloxy-5-(p-toluenesulfonamido)-3-alken-2-ols: synthesis of (+)-monomorine I
No full textA versatile method for the preparation of indolizidine alkaloids from 1-benzyloxy-5-(p-toluenesulfonamido)-3-alken-2-ols as stereodefined key intermediates has been developed. The utility of this approach was demonstrated by the synthesis of (+)-monomorine I.PT: J; CR: BACKVALL JE, 1990, J ORG CHEM, V55, P826 BAILEY AJ, 1993, INORG CHEM, V32, P268 BERRY MB, 1997, CHEM COMMUN 1121, P2141 CUNY GD, 1995, SYNLETT, P519 DALY JW, 1983, SCIENCE, P705 DALY JW, 1986, ALKALOIDS CHEM BIOL, V4, CH1 GAO Y, 1995, J AM CHEM SOC, V117, P5399 GRIFFITH WP, 1987, J CHEM SOC CHEM COMM, P1625 GRIFFITH WP, 1990, ALDRICHIM ACTA, V23, P13 HAMADA Y, 1987, J ORG CHEM, V52, P1252 HOWARD AS, 1986, ALKALOIDS, V28, CH6 ITO M, 1991, TETRAHEDRON, V47, P9329 KROHN K, 1998, J PRAK CHEM-CHEM ZTG, V340, P26 MICHAEL JP, 1995, NAT PROD REP, V12, P535 MOMOSE T, 1997, J CHEM SOC PERK 0507, P1315 MUNCHHOF MJ, 1995, J AM CHEM SOC, V117, P5399 NUMATA A, 1987, ALKALOIDS, V31, CH3 PARIKH JR, 1967, J AM CHEM SOC, V89, P5505 PETTERSSONFASTH H, 1995, J ORG CHEM, V60, P6091 PETTERSSONFASTH P, 1994, THESIS UPPSALA U RITTER FJ, 1973, EXPERIENTIA, V29, P530 ROYER J, 1985, J ORG CHEM, V50, P670 SALIOU C, 1991, TETRAHEDRON LETT, V32, P3365 SHAWE TT, 1994, J ORG CHEM, V59, P5841 SOMFAI P, 1997, ACTA CHEM SCAND, V51, P1024 STEVENS RV, 1982, J CHEM SOC CHEM COMM, P102 STOWELL JC, 1979, SYNTHESIS-STUTTGART, P132 STOWELL JC, 1990, ORG SYNTH COLL, V7, P140 TAKAHATA H, 1993, ALKALOIDS, V44, CH3 TAKAHATA H, 1993, HETEROCYCLES, V36, P2777 TOKUYAMA T, 1986, TETRAHEDRON, V42, P3453 TROST BM, 1978, J AM CHEM SOC, V100, P3426 YAMAGUCHI R, 1987, J ORG CHEM, V52, P2094 YAMAZAKI N, 1988, TETRAHEDRON LETT, V29, P5767 YAMAZAKI N, 1989, J AM CHEM SOC, V111, P1396; NR: 35; TC: 9; J9: EUR J ORG CHEM; PG: 4; GA: 313PNSource type: Electronic(1
Stereoselective route towards 2,5-disubstituted piperidine alkaloids. Synthesis of (+)-pseudoconhydrine and (±)-epi-pseudoconhydrine
No full textThis paper describes a new general approach towards functionalized piperidine alkaloids, based on the stereo- and regioselective palladium(0)-catalyzed nucleophilic ring-opening of vinyl epoxides by nitrogen nucleophiles. The latter reaction provides access to stereo-defined and and syn aminoalcohol derivatives, 1-benzyloxy-5-(p-toluenesulfonamido)-3-alken-2-ols (5), which were transformed to (+)-pseudoconhydrine (3) and (+/-)-epi-pseudoconhydrine (9), respectively, via protection (silyl ether), hydrogenation, debenzylation and cyclization. Detosylation-deprotection gave the final products in good yields and high stereoisomeric purity. (C) 2000 Elsevier Science Ltd. All rights reserved.PT: J; CR: AGAMI C, 1998, TETRAHEDRON, V54, P8783 BACKVALL JE, 1990, J ORG CHEM, V55, P826 BACKVALL JE, 1991, J ORG CHEM, V56, P2988 BERNET B, 1983, TETRAHEDRON LETT, V24, P5491 BOUZIDE A, 1997, TETRAHEDRON LETT, V38, P5945 BROWN E, 1973, TETRAHEDRON, V29, P455 BYSTROM SE, 1985, TETRAHEDRON LETT, V26, P1749 CHRISTOFIDIS I, 1977, TETRAHEDRON, V33, P977 COSSY J, 1997, SYNLETT AUG, P905 CUNICO RF, 1980, J ORG CHEM, V45, P4797 DOCKNER M, 1998, LIEBIGS ANN-RECL, V6, P1267 GAO Y, 1987, J AM CHEM SOC, V109, P5765 HARDING KE, 1984, J ORG CHEM, V49, P40 HASSEBERG HA, 1989, LIEBIGS ANN CHEM, P255 HERDEIS C, 1997, SYNTHESIS-STUTTG DEC, P1405 HIGHET RJ, 1964, J ORG CHEM, V29, P471 HIGHET RJ, 1966, J ORG CHEM, V31, P1275 HILL RK, 1970, CHEM ALKALOIDS, P385 HIRAI Y, 1997, CHEM LETT, P221 JONES TH, 1990, J NAT PRODUCTS, V53, P429 KATSUKI T, 1982, J ORG CHEM, V47, P1373 KOHRT JT, 1998, J ORG CHEM, V63, P5088 LADENBERG A, 1891, BER, V24, P1671 MARION L, 1949, J AM CHEM SOC, V49, P3402 MCDONALD WS, 1997, J ORG CHEM, V62, P1215 MOODY CJ, 1997, J ORG CHEM, V62, P746 OPPOLZER W, 1995, TETRAHEDRON LETT, V36, P2959 PETTERSSONFASTH H, 1995, J ORG CHEM, V60, P6091 RICE WY, 1966, J ORG CHEM, V31, P1010 RIESINGER SW, 1999, EUR J ORG CHEM DEC, P3277 SAKAGAMI H, 1996, J CHEM SOC CHEM COMM, P1433 SCHINK HE, 1991, J ORG CHEM, V56, P2769 SCHLOSS JV, 1980, BIOORG CHEM, V9, P217 SPATH E, 1933, CHEM BER, V66, P591 STRUNZAND GM, 1986, ALKALOIDS, V26, P89 TADANO K, 1985, J CARBOHYD CHEM, V4, P129 TAKAHATA H, 1994, HETEROCYCLES, V38, P269 TENAGLIA A, 1988, TETRAHEDRON LETT, V29, P4851 TOYOOKA N, 1999, J ORG CHEM, V64, P4914 TROST BM, 1978, J AM CHEM SOC, V100, P3426 TROST BM, 1981, J AM CHEM SOC, V103, P5969 TROST BM, 1986, J ORG CHEM, V51, P2332 TROST BM, 1987, J AM CHEM SOC, V109, P3792 TROST BM, 1988, J AM CHEM SOC, V110, P621 TROST BM, 1993, J AM CHEM SOC, V115, P9421 TROST BM, 1996, ANGEW CHEM, V108, P70 TROST BM, 1996, J AM CHEM SOC, V118, P6520 TSUJI J, 1981, TETRAHEDRON LETT, V22, P2575 TSUJI J, 1982, PURE APPL CHEM, V54, P197 YAMAZAKI N, 1989, J AM CHEM SOC, V111, P1396; NR: 50; TC: 8; J9: TETRAHEDRON; PG: 6; GA: 303EZSource type: Electronic(1
Retelling racialized violence, remaking white innocence: the politics of interlocking oppressions in transgender day of remembrance
No full textTransgender Day of Remembrance has become a significant political event among those resisting violence against gender-variant persons. Commemorated in more than 250 locations worldwide, this day honors individuals who were killed due to anti-transgender hatred or prejudice. However, by focusing on transphobia as the definitive cause of violence, this ritual potentially obscures the ways in which hierarchies of race, class, and sexuality constitute such acts. Taking the Transgender Day of Remembrance/Remembering Our Dead project as a case study for considering the politics of memorialization, as well as tracing the narrative history of the Fred F. C. Martinez murder case in Colorado, the author argues that deracialized accounts of violence produce seemingly innocent White witnesses who can consume these spectacles of domination without confronting their own complicity in such acts. The author suggests that remembrance practices require critical rethinking if we are to confront violence in more effective ways. Description from publisher's site: http://caliber.ucpress.net/doi/abs/10.1525/srsp.2008.5.1.2
Elin Org: mikrobioomi uurimisega avanes mulle uus maailm
No full textEesti Arst 2025; 104(6–7):319–32
The Davis-Beirut reaction: N 1, N 2-disubstituted-1 H-indazolones via 1,6-electrophilic addition to 3-alkoxy-2 H-indazoles
No full textA variety of electrophiles (anhydrides, acid chlorides, carbonochloridates, sulfonyl chlorides, and alkyl bromides) react with 3-methoxy-2H-indazole (1a), benzoxazin[3,2-b]indazole (1d), and oxazolino[3,2-b]indazole (1e) - substrates available by the Davis-Beirut reaction - to yield a diverse set of N 1,N2-disubstituted-1H-indazolones. With certain electrophiles, an AERORC (Addition of the Electrophile, Ring Opening, and Ring Closure) process on indazole 1d results in indazoloindazolone formation. An intriguing aspect of these N1,N2-disubstituted-1H- indazolones is that they are poised for diversification through, for example, azide-alkyne cycloaddition chemistry reported here. © 2011 American Chemical Society.Avila B, 2011, ORG LETT, V13, P1060, DOI 10.1021-ol103108z; Butler JD, 2008, J ORG CHEM, V73, P234, DOI 10.1021-jo702067z; Cerecetto H, 2005, MINI-REV MED CHEM, V5, P869, DOI 10.2174-138955705774329564; Donald MB, 2010, ORG LETT, V12, P2524, DOI 10.1021-ol100751n; ELGUERO I, 1996, COMPREHENSIVE HETERO, V3, P1; Feldman AK, 2004, ORG LETT, V6, P3897, DOI 10.1021-ol048859z; Goddard-Borger ED, 2007, ORG LETT, V9, P3797, DOI 10.1021-ol701581g; Halland N, 2009, ANGEW CHEM INT EDIT, V48, P6879, DOI 10.1002-anie.200902323; Hein JE, 2010, CHEM SOC REV, V39, P1302, DOI 10.1039-b904091a; Huang LJ, 2006, BIOORGAN MED CHEM, V14, P528, DOI 10.1016-j.bmc.2005.08.032; Kawanishi N, 2006, BIOORG MED CHEM LETT, V16, P5122, DOI 10.1016-j.bmcl.2006.07.026; Kurth MJ, 2005, J ORG CHEM, V70, P1060, DOI 10.1021-jo048153i; Liu YX, 2010, J AGR FOOD CHEM, V58, P2685, DOI 10.1021-jf902541w; Meldal M, 2008, CHEM REV, V108, P2952, DOI 10.1021-cr0783479; Mills AD, 2007, J COMB CHEM, V9, P171, DOI 10.1021-cc060109o; Mills AD, 2006, J ORG CHEM, V71, P2687, DOI 10.1021-jo0524831; Oakdale JS, 2009, ORG LETT, V11, P2760, DOI 10.1021-ol900891s; Fletcher SR, 2006, BIOORG MED CHEM LETT, V16, P2872, DOI 10.1016-j.bmcl.2006.03.004; Rostovtsev VV, 2002, ANGEW CHEM INT EDIT, V41, P2596, DOI 10.1002-1521-3773(20020715)41:142596::AID-ANIE25963.0.CO;2-4; Schmidt A, 2008, EUR J ORG CHEM, P4073, DOI 10.1002-ejoc.200800227; Solano D. M., 2010, ORG SYNTH, V87, P339; Stadlbauer W., 2002, SCI SYNTH, V12, P227; Tornoe CW, 2002, J ORG CHEM, V67, P3057, DOI 10.1021-jo011148j; VANDERPLAS HC, 1978, ACCOUNTS CHEM RES, V11, P462, DOI 10.1021-ar50132a005; van der Plas HC, 1999, ADV HETEROCYCL CHEM, V74, P1; Vina D, 2007, ORG LETT, V9, P525, DOI 10.1021-ol062890e12131
Reactivity and selectivity in intermolecular insertion reactions of chlorophenylcarbene
No full textPT: J; CR: DOYLE MP, 1987, CHEM DIAZIRINES, CH8 DOYLE MP, 1987, J ORG CHEM, V52, P1619 GOULD IR, 1985, TETRAHEDRON, V41, P1587 GRAHAM WH, 1965, J AM CHEM SOC, V87, P4396 KIRMSE W, 1964, CARBENE CHEM MOSS RA, 1985, REACTIVE INTERMEDIAT, V3, CH3 MOSS RA, 1986, J AM CHEM SOC, V108, P7028 PADWA A, 1969, J ORG CHEM, V34, P2728 SEYFERTH D, 1967, J ORGANOMET CHEM, V7, P405 SEYFERTH D, 1968, J AM CHEM SOC, V90, P2944 SEYFERTH D, 1970, J ORG CHEM, V35, P1989 SEYFERTH D, 1973, J AM CHEM SOC, V75, P6763 SOUNDARARAJAN N, IN PRESS J AM CHEM S STANG PJ, 1987, J AM CHEM SOC, V109, P5019 STEINBECK K, 1978, TETRAHEDRON LETT, P1103 STEINBECK K, 1981, ANGEW CHEM INT EDIT, V20, P773; NR: 16; TC: 18; J9: TETRAHEDRON LETT; PG: 4; GA: R2217Source type: Electronic(1
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