5304-15-4Relevant articles and documents
COMPOUNDS AND COMPOSITIONS FOR USE IN AUGMENTATION OF GLUCOSE UPTAKE AND INSULIN SECRETION
-
Page/Page column 28, (2013/03/26)
The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of -S-, -S-S-, -S-(CH2)n-, -NH-, -NH-(CH2)n-, -0-, -S02-, arylene, heteroarylene; Rl is selected from the group consisting of straight or branched C4- C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5- C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or het- eroaromatic ring, each optionally substituted with at least one group selected from -COOH, -NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 car- boxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, N02, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2 - C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, halogen; and compositions for use in the treatment of diabetes and related dis? orders.
Topically Active Carbonic Anhydrase Inhibitors. 1. O-Acyl Derivatives of 6-Hydroxybenzothiazole-2-sulfonamide
Woltersdorf, O. W.,Schwam, H.,Bicking, J. B.,Brown, S. L.,deSolms, S. J.,et al.
, p. 2486 - 2492 (2007/10/02)
A series of O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide (4, L-643,799) was prepared and the potential utility of each series member as a topically active inhibitor of ocular carbonic anhydrase was determined.In vitro studies showed these esters to be substrates for ocular esterases which liberate 4 during corneal translocation.The most interesting series member, 2-sulfamoyl-6-benzothiazolyl 2,2-dimethylpropionate (22, L-645,151), acting as a prodrug form of 4, was found to enhance delivery through the isolated albino rabbit cornea by 40-fold when compared to the parent phenol 4.Studies in rabbits revealed that 22 is a potent topically active ocular hypotensive carbonic anhydrase inhibitor.