- Convenient synthesis of primary sulfonamides
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An efficient protocol for a one-pot synthesis of mono-sulfonamides has been developed. It features utilization of excess of sulfonylating agent followed by base mediated recovery of the primary sulfonamide.
- Greenfield, Alexander,Grosanu, Cristina
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p. 6300 - 6303
(2009/04/06)
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- Microwave-induced rapid access to aromatic and heteroaromatic sulfonamides under solvent-free conditions without using external base
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Microwave-induced syntheses of sulfonamides, without using base under solvent-free conditions, have been developed. The process finds its utility because of its simple operational procedure and high yields. Moreover, the process is fast and accommodative to different substituents on aromatic as well as heteroaromatic rings rendering sulfonamides (28 examples).
- Sharma, Ashwani Kumar,Das, Saibal Kumar
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p. 3807 - 3819
(2007/10/03)
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- Compounds useful as reversible inhibitors of cysteine proteases
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Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.
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- A convenient reductive deamination (hydrodeamination) of aromatic amines
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Reductive deamination (hydrodeamination) of aromatic amines can be conveniently carried out by amination of the corresponding arylamine methanesulfonamides using chloroamine under alkaline conditions. The intermediate aryl methanesulfonylhydrazines directly eliminate methanesulfinic acid, affording diazenes which extrude nitrogen affording the desired deaminated products. Both sulfonamide formation and reduction reactions occur in high yield and are compatible with a variety of functional groups.
- Wang,Guziec Jr.
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p. 8293 - 8296
(2007/10/03)
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- Synthesis and protein kinase C inhibitory activities of balanol analogues with modification of 4-hydroxybenzamido moiety
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A series of racemic balanol analogues with modification of the benzamido moiety of balanol have been synthesized and evaluated for their inhibitory activities against human protein kinase C isozymes (PKC-alpha, -beta I, -beta II, -gamma, -delta, -epsilon, and -eta). The structural modification includes replacement of the 4-hydroxyphenyl group with variously substituted phenyl rings, substitution of the amide linkage with a sulfonamide or an ester, and replacement of the 4-hydroxyphenyl substructure with a hydroxyl substituted indole or a hydroxybenzyl group. In general, these analogues were found to be less potent than balanol, but a number of analogues were identified with improved isozyme selectivity. The structure-activity relationship studies of these analogues also indicated that (1) the optimal general PKC inhibition requires a free 4-hydroxyl group in the benzamido portion of the molecule, (2) the amide linkage of the benzamido moiety is important for PKC inhibition, and (3) the conformation associated with the benzamido moiety seems to have a profound effect on PKC inhibition. The requirement of a free 4-hydroxyl group in conjunction with an appropriate conformation of the benzamido moiety for optimal PKC inhibition suggests that the 4-hydroxyphenyl group may be involved in a specific inhibitor-enzyme interaction important for PKC inhibition.
- Hu, Hong,Mendoza, Jose S.,Lowden, Christopher T.,Ballas, Lawrence M.,Janzen, William P.
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p. 1873 - 1882
(2007/10/03)
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- Substituted benzene derivatives useful as neuraminidase inhibitors
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A compound of the Formula (I): STR1 or pharmaceutically-suitable salts or prodrug forms thereof, wherein: n is 0-1; m is 0; p is 0-1; R1 is --CO2 H; R2 is selected from the group consisting of H, --OH, and --NH2 ; R3 is H; R4 is --C(O)NHR8 ; R5 is --NHC(R6)NH2 R6 is selected from the group consisting of =NH, =NOH, =NCN, =O, and =S; and R8 is selected from the group consisting of C1 -C4 linear or branched alkyl substituted with 0-3 halogens on each carbon.
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- 4-(1-hydroxy-2-N-substituted sulfonamido) ethyl-5-hydroxy-2(5H)-furanones and 4-(N-substituted sulfonamido)-2-ethenyl-5-hydroxy-2(5H)-furanones as anti-inflammatory agents
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Compounds of Formula 1, and of Formula 2, STR1 in which R1 is H or alkyl of 1 to 20 carbons, CO--R1* CO--O--R1* CO--NH--R1* or PO(OR1*)2 or PO(OR
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- Substituted sulfonamidobenzamides, antiarrhythmic agents and compositions thereof
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Novel substituted sulfonamidobenzamides are described as useful antiarrhythmic agents. Their use in the treatment of cardiac arrhythmias, especially re-entrant arrhythmias, via the prolongation of the action potential of cardiac tissue is provided. Pharmaceutical formulations containing such compounds are also disclosed.
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