24155-85-9Relevant academic research and scientific papers
HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 -HYDROXYSTEROID DEHYDROGENASE
-
Page/Page column 47-48, (2010/08/07)
Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein X is O or S, a broken line and a wavy line represent the presence or the absence of a bond, (i) when a broken line represents the presence of a bond, a wavy line represents the absence of a bond, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, (ii) when a broken line represents the absence of a bond, a wavy line represents the presence of a bond, R1 and R4 are each independently hydrogen, halogen or the like, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, and R5 and R6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like.
Substituent effects on the reactivity of benzo-1,2-dithiolan-3-one 1-oxides and their possible application to the synthesis of DNA-targeting drugs
Sawwan, Nahed,Brzostowska, Edyta M.,Greer, Alexander
, p. 6968 - 6971 (2007/10/03)
The efficiency of polysulfane product generation has been investigated for n-propyl thiol reactions with ortho- and para-substituted benzo-1,2-dithiolan-3- one 1-oxides in acetonitrile-water (7:3) mixtures. The reaction is facilitated by reducing the electron density at the para position or by placing substituents bearing lone pair electrons ortho to the dithiolanone-oxide (S1) reaction center. Through-space and through-bond effects both contribute to the conversion of polysulfane products.
Conformational Behaviour of Medium-sized Rings. Part 10. Dithiosalicylides and Trithiosalicylides
Guise, G. Bruce,Ollis, W. David,Peacock, Judith A.,Stephanatou, Julia Stephanidou,Stoddart, J. Fraser
, p. 1637 - 1648 (2007/10/02)
The trithiosalicylide derivatives (8)-(11) have been synthesised and shown by temperature-dependent 1H n.m.r. spectroscopy to exist in solution as ring inverting (35a)(35b) enantiomeric helical conformations with trans-thioester linkages.The free energies of activation for these conformational changes are ca. 10 kcal mol-1 higher than those for the similar process in the corresponding trisalicylides.In contrast with the trisalicylides, the trithiosalicylides can only ring invert between enantiomeric helical conformations via intermediates containing a cis-thioester linkage.The dithiosalicylide derivatives (3)-(7) have been synthesised; the temperature dependence of the 1H n.m.r. spectrum of di-o-thiothymotide (7) has been interpreted in terms of ring inversion (40a)(40b) between enantiomeric boat conformations.Comparison of the ΔG value of 24.6 kcal mol-1 for this conformational change with that of 17.7 kcal mol-1 previously obtained for di-o-thymotide (41) suggests that cis-thioester linkages are subject to more resonance stabilisation than are cis-ester linkages.
DITHIOSALICYLIDES AND TRITHIOSALICYLIDES. THEIR CONFORMATIONAL BEHAVIOUR IN SOLUTION
Guise, Bruce G.,Ollis, David W.,Peacock, Judith A.,Stephanatou, Julia Stephanidou,Stoddart, Fraser J.
, p. 4203 - 4206 (2007/10/02)
The trithiosalicylide derivatives (11)-(14) have been synthesised and shown to exist in solution as ring inverting (15-15*) enantiomeric helical conformations.
Intermediates for preparing hipolipemic agents and method of lowering the blood lipid level in mammals with said agents
-
, (2008/06/13)
Intermediates for preparing benzylthio-, benzylsulfinyl-, and benzylsylfonyl-benzoic acids, and method of lowering the blood lipid level in mammals employing said acids.
