Conformational analysis of 5-lipoxygenase inhibitors: role of the substituents in chiral recognition and on the active conformations of the (methoxyalkyl)thiazole and methoxytetrahydropyran series

1994 ◽  
Vol 37 (1) ◽  
pp. 113-124 ◽  
Author(s):  
Christine Lambert-van der Brempt ◽  
Pierre Bruneau ◽  
Maryannick A. Lamorlette ◽  
Stephen J. Foster
Keyword(s):  
Conformational Analysis ◽  
Chiral Recognition ◽  
Lipoxygenase Inhibitors

scholarly journals Conformational Analysis of CmH2m+1OCH2CH2OH (m = 1-4): The Role of CH.cntdot..cntdot..cntdot.O Intramolecular Interactions

1995 ◽  
Vol 99 (20) ◽  
pp. 8066-8070 ◽  
Author(s):  
Francisco P. S. C. Gil ◽  
A. M. Amorim Da Costa ◽  
J. J. C. Teixeira-Dias
Keyword(s):  
Conformational Analysis ◽  
Intramolecular Interactions

An Investigation into the Role of Solvation in a Well Characterized Chiral Recognition System

1991 ◽  
Vol 14 (11) ◽  
pp. 2027-2042 ◽  
Author(s):  
William H. Pirkle ◽  
Christopher J. Welch
Keyword(s):  
Chiral Recognition ◽  
Recognition System

Crystal and Molecular Structure of the [6-Deoxy-6-[(2-(4-imidazolyl)ethyl)amino]- cyclomaltoheptaose]copper(II) Ternary Complex withl-Tryptophanate. Role of Weak Forces in the Chiral Recognition Process Assisted by a Metallocyclodextrin

1996 ◽  
Vol 35 (15) ◽  
pp. 4497-4504 ◽  
Author(s):  
Raffaele P. Bonomo ◽  
Benedetto Di Blasio ◽  
Giuseppe Maccarrone ◽  
Vincenzo Pavone ◽  
Carlo Pedone ◽  
...  
Keyword(s):  
Molecular Structure ◽  
Chiral Recognition ◽  
Ternary Complex ◽  
Crystal And Molecular Structure ◽  
Recognition Process ◽  
Weak Forces

Role of eicosanoids in vasopressin-induced calcium mobilization in A7r5 vascular smooth muscle cells

1993 ◽  
Vol 265 (1) ◽  
pp. E108-E114 ◽  
Author(s):  
M. Thibonnier ◽  
A. L. Bayer ◽  
C. L. Laethem ◽  
D. R. Koop ◽  
M. S. Simonson
Keyword(s):  
Smooth Muscle ◽  
Smooth Muscle Cells ◽  
High Performance ◽  
Muscle Cells ◽  
Calcium Mobilization ◽  
Metabolite Formation ◽  
Lipoxygenase Inhibitors ◽  
A7r5 Cells ◽  
Cytochrome P 450

The role of arachidonic acid (AA) and its metabolites in vasopressin (AVP)-induced calcium mobilization in A7r5 aortic smooth muscle cells was explored by intracellular calcium monitoring, [14C]AA labeling, and high-performance liquid chromatography (HPLC) techniques. In fura 2-loaded A7r5 cells, AA potentiated AVP-stimulated increase in intracellular free Ca2+ ([Ca2+]i). The cyclooxygenase inhibitor indomethacin reduced both the AA- and AVP-induced influx of extracellular Ca2+. AVP-induced [Ca2+]i transients were not altered by lipoxygenase inhibitors but were reduced in a dose-dependent fashion by ketoconazole, an inhibitor of cytochrome P-450 monooxygenases. Among several epoxygenase metabolites of AA tested, 5,6-epoxyeicosatrienoic acid potentiated AVP-induced [Ca2+]i transients. Reverse-phase HPLC analysis of lipid extracts from A7r5 cells prelabeled with [14C]AA isolated a radioactive peak that did not coelute with established products of cyclooxygenase-, lipoxygenase-, or cytochrome P-450-catalyzed oxidations of AA. This peak was significantly increased after AVP stimulation and was completely blocked by preincubation with ketoconazole. Thus the stimulation of V1-vascular AVP receptors of A7r5 cells triggers several cytoplasmic signaling pathways involving AA metabolite formation through the cyclooxygenase and epoxygenase pathways.

The role of the generalized anomeric effect in the conformational analysis of 1,3-dioxacycloalkanes. Conformational analysis of 3,5-dioxabicyclo[5.1.0]octanes and 3,5,8-trioxabicyclo[5.1.0]octanes

1977 ◽  
Vol 42 (2) ◽  
pp. 365-368 ◽  
Author(s):  
Michael H. Gianni ◽  
Robert Cody ◽  
Mohan R. Asthana ◽  
Karl Wursthorn ◽  
Patrick Patanode ◽  
...  
Keyword(s):  
Conformational Analysis ◽  
Anomeric Effect

The “Bridge” Game: Role of the Fourth Player in Chiral Recognition

2011 ◽  
Vol 17 (11) ◽  
pp. 3078-3081 ◽  
Author(s):  
Caterina Fraschetti ◽  
Marco Pierini ◽  
Claudio Villani ◽  
Francesco Gasparrini ◽  
Stefano Levi Mortera ◽  
...  
Keyword(s):  
Chiral Recognition

scholarly journals Effects of calmodulin and lipoxygenase inhibitors on LH (lutropin)- and LHRH (luliberin)-agonist-stimulated steroidogenesis in rat Leydig cells

1985 ◽  
Vol 232 (1) ◽  
pp. 55-59 ◽  
Author(s):  
M H Sullivan ◽  
B A Cooke
Keyword(s):  
Arachidonic Acid ◽  
Leydig Cells ◽  
Acid Metabolism ◽  
Arachidonic Acid Metabolism ◽  
Ionophore A23187 ◽  
Lhrh Agonist ◽  
Lipoxygenase Pathway ◽  
Lipoxygenase Inhibitors ◽  
Testosterone Production

The results of this study, carried out with purified rat Leydig cells, indicate that there are no major differences in the stimulating effects of lutropin (LH) and luliberin (LHRH) agonists on steroidogenesis via mechanisms that are dependent on Ca2+. This was demonstrated by using inhibitors of calmodulin and the lipoxygenase pathways of arachidonic acid metabolism. All three calmodulin inhibitors used (calmidazolium, trifluoperazine and chlorpromazine) were shown to block LH- and LHRH-agonist-stimulated steroidogenesis. This probably occurred at the step of cholesterol transport to the mitochondria. Similarly, three lipoxygenase inhibitors (nordihydroguaiaretic acid, BW755c and benoxaprofen), inhibited both LH- and LHRH-agonist-stimulated steroidogenesis. The amounts of the inhibitors required were similar for LH- and LHRH-agonist-stimulated steroidogenesis. Steroidogenesis stimulated by the Ca2+ ionophore A23187 was also inhibited, but higher concentrations of the inhibitors were required. Indomethacin (a cyclo-oxygenase inhibitor) increased LHRH-agonist-stimulated steroidogenesis;this is consistent with the role of the products of arachidonic acid metabolism via the alternative, lipoxygenase, pathway. The potentiation of LH-stimulated testosterone production by LHRH agonist was unaffected by indomethacin or by lipoxygenase inhibitors at concentrations that inhibited LH-stimulated testosterone production by 75-100%. It was not possible to eliminate a role of calmodulin in modulating the potentiation, although higher concentrations of the inhibitors were generally required to negate the potentiation than to inhibit LH- or LHRH-agonist-stimulated testosterone production.

ChemInform Abstract: THE ROLE OF THE GENERALIZED ANOMERIC EFFECT IN THE CONFORMATIONAL ANALYSIS OF 1,3-DIOXACYCLOALKANES. CONFORMATIONAL ANALYSIS OF 3,5-DIOXABICYCLO(5.1.0)OCTANES AND 3,5,8-TRIOXABICYCLO(5.1.0)OCTANES

1977 ◽  
Vol 8 (22) ◽  
pp. no-no
Author(s):  
M. H. GIANNI ◽  
R. CODY ◽  
M. R. ASTHANA ◽  
K. WURSTHORN ◽  
P. PATANODE ◽  
...  
Keyword(s):  
Conformational Analysis ◽  
Anomeric Effect

ChemInform Abstract: Synthesis and Conformational Analysis of an Analogue of the Antithrombin-Binding Region of Heparin: The Role of the Carboxylate Function of α-L-Idopyranuronate.

ChemInform ◽  
1988 ◽  
Vol 19 (13) ◽  
Author(s):  
C. A. A. VAN BOECKEL ◽  
H. LUCAS ◽  
S. F. VAN AELST ◽  
M. W. P. VAN DEN NIEUWENHOF ◽  
G. N. WAGENAARS ◽  
...  
Keyword(s):  
Conformational Analysis ◽  
Binding Region
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