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Zajdel P Marciniec K Maślankiewicz A Satała G Duszyńska B Bojarski AJ Partyka A Jastrzębska-Więsek M Wróbel D Wesołowska A Pawłowski M 《Bioorganic & medicinal chemistry》2012,20(4):1545-1556
Two series of arylpiperazinyl-alkyl quinoline-, isoquinoline-, naphthalene-sulfonamides with flexible (13-26) and semi-rigid (33-36) alkylene spacer were synthesized and evaluated for 5-HT(1A), 5-HT(2A), 5-HT(6), 5-HT(7) and selected compounds for D(2), D(3), D(4) receptors. The compounds with a mixed 5-HT and D receptors profile 16 (N-{4-[4-(3-chlorophenyl)-piperazin-1-yl]-butyl}-3-quinolinesulfonamide) and 36 (4-(4-{2-[4-(4-chloro-phenyl)-piperazin-1-yl]-ethyl}-piperidine-1-sulfonyl)-isoquinoline), displaying antagonistic activity at 5-HT(7), 5-HT(2A), D(2) postsynaptic sites, produced antidepressant-like effects in the forced swim test in mice and showed significant anxiolytic activity in the plus-maze test in rats. The lead compound 36, a multi-receptor 5-HT(2A)/5-HT(7)/D(2)/D(3)/D(4) agent, also displayed significant antipsychotic properties in the MK-801-induced hyperlocomotor activity in mice. 相似文献
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We provide the first multilocus molecular phylogeny of a group corresponding to the former subfamily Staphylininae. Results are corroborated by the morphological, biogeographical and palaeobiological evidence to serve as a baseline for an updated suprageneric classification. The former subfamily Staphylininae is proven to be a lineage sister to the monophyletic Paederinae and reclassified according to a robust phylogeny resolving a number of long-standing controversies. The subfamily Xantholininae (revised status) is reinstated to contain the tribes Xantholinini, Othiini, Maorothiini and Diochini. Subfamily Platyprosopinae (revised status) is reinstated for the tribes Platyprosopinini, Arrowinini and †Thayeralinini. For a highly peculiar genus Coomania Cameron, formerly in Diochini, a new subfamily Coomaniinae subfam.n. is established and the composition of Diochini (revised status) is changed accordingly. The subfamily Staphylininae (revised status) is reduced to contain the former tribe Staphylinini only. Elevating this mega-diverse tribe to the subfamily rank opened up an opportunity for its more fractional classification by raising several subtribes to the tribal level as follows: Acylophorini, Afroquediini, Amblyopinini, Antimerini, †Baltognathini, Cyrtoquediini, Erichsoniini, Hyptiomini, Indoquediini, Quediini and Tanygnathinini (revised status for all). As a result, the most species-rich tribe Staphylinini (revised status) is reduced to the more homogeneous lineage containing the subtribes Algonina, Anisolinina, Philonthina, Philothalpina, Staphylinina and Xanthopygina. Morphological synapomorphies and diagnostic characters supporting all newly defined higher taxa are provided. This published work has been registered on ZooBank, http://zoobank.org/urn:lsid:zoobank.org:pub:DED8B042-83C9-4D10-B0CB-B50372B067A9 . 相似文献
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Dagmara McGuinness Johannes Leierer Olivier Shapter Suhaib Mohammed Marc Gingell-Littlejohn David B. Kingsmore Ann-Margaret Little Julia Kerschbaum Stefan Schneeberger Manuel Maglione Silvio Nadalin Sylvia Wagner Alfred K?nigsrainer Emma Aitken Henry Whalen Marc Clancy Alex McConnachie Christian Koppelstaetter Karen S. Stevenson Paul G. Shiels 《PloS one》2016,11(3)
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Zlotkowska D Maddaloni M Riccardi C Walters N Holderness K Callis G Rynda-Apple A Pascual DW 《PloS one》2012,7(4):e36182
Ovalbumin (OVA) genetically fused to protein sigma 1 (pσ1) results in tolerance to both OVA and pσ1. Pσ1 binds in a multi-step fashion, involving both protein- and carbohydrate-based receptors. To assess the relative pσ1 components responsible for inducing tolerance and the importance of its sialic binding domain (SABD) for immunization, modified OVA-pσ1, termed OVA-pσ1(short), was deleted of its SABD, but with its M cell targeting moiety intact, and was found to be immunostimulatory and enhanced CD4(+) and CD8(+) T cell proliferation. When used to nasally immunize mice given with and without cholera toxin (CT) adjuvant, elevated SIgA and serum IgG responses were induced, and OVA-pσ1(s) was more efficient for immunization than native OVA+CT. The immune antibodies (Abs) were derived from elevated Ab-forming cells in the upper respiratory tissues and submaxillary glands and were supported by mixed Th cell responses. Thus, these studies show that pσ1(s) can be fused to vaccines to effectively elicit improved SIgA responses. 相似文献
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The studies of ParA and ParB dynamics reveal asymmetry of chromosome segregation in mycobacteria 下载免费PDF全文
Isabella Santi Djenet Bousbaine Jolanta Zakrzewska‐Czerwińska Dagmara Jakimowicz John McKinney 《Molecular microbiology》2017,105(3):453-468
Active segregation of bacterial chromosomes usually involves the action of ParB proteins, which bind in proximity of chromosomal origin (oriC) regions forming nucleoprotein complexes – segrosomes. Newly duplicated segrosomes are moved either uni‐ or bidirectionally by the action of ATPases – ParA proteins. In Mycobacterium smegmatis the oriC region is located in an off‐centred position and newly replicated segrosomes are segregated towards cell poles. The elimination of M. smegmatis ParA and/or ParB leads to chromosome segregation defects. Here, we took advantage of microfluidic time‐lapse fluorescent microscopy to address the question of ParA and ParB dynamics in M. smegmatis and M. tuberculosis cells. Our results reveal that ParB complexes are segregated in an asymmetrical manner. The rapid movement of segrosomes is dependent on ParA that is transiently associated with the new pole. Remarkably in M. tuberculosis, the movement of the ParB complex is much slower than in M. smegmatis, but segregation as in M. smegmatis lasts approximately 10% of the cell cycle, which suggests a correlation between segregation dynamics and the growth rate. On the basis of our results, we propose a model for the asymmetric action of segregation machinery that reflects unequal division and growth of mycobacterial cells. 相似文献
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The structure, conformation and configuration of methyl 3-amino-2,3-dideoxy-alpha-d-arabino-hexopyranoside were confirmed by (1)H NMR, (13)C NMR and IR spectroscopy, as well as by optical rotation. The structure of the compound studied was also determined by single crystal X-ray crystallography at 293 K and refined to a final R=0.0521 based on 1798 independent reflections. The title compound crystallized in the tetragonal space group P4(3) with a=6.572(1) angstrom, b=6.572(1) angstrom, c=41.161(8) angstrom, D(c)=1.324 Mgcm(-3) and V=1777.8(5) angstrom(3) for Z=8. The packing arrangement in the unit cell displayed a stratified structure. Moreover, medium-strength N-H. . .O and O-H. . .O hydrogen bonds, which stabilized the 3-D structure of compound I, were observed. 相似文献
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Podolak Irma Grabowska Karolina Sobolewska Danuta Wróbel-Biedrawa Dagmara Makowska-Wąs Justyna Galanty Agnieszka 《Phytochemistry Reviews》2023,22(1):113-167
Phytochemistry Reviews - Saponins make up an important group of natural glycosidic compounds which are distinguished by triterpene or steroidal aglycone. Although widely distributed in terrestrial... 相似文献