- Carbonic anhydrase inhibitors - Part 29: Interaction of isozymes I, II and IV with benzolamide-like derivatives
-
Reaction of 5-amino-1,3,4-thiadiazole-2-sulfonamide and 5-imino-4- methyl-2-sulfonamido-δ2-1,3,4-thiadiazoline with sulfonyl halides/sulfonic acid anhydrides afforded benzolamide-like derivatives possessing strong inhibitory effects towards three isozymes of carbonic anhydrase (CA), CA I, II anal IV. Some of the compounds were designed in such a way to possess good leaving groups (such as nitro-; 2,4,6-triphenyl-pyridinium, etc.) for aromatic nucleophilic substitution reactions with fluoride, in order to introdUCe positron-emitting isotopes in their molecule, such as 18F. Reactions done initially with the stable isotope of fluorine were not very effective, as the yields in the desired fluoro-derivatives were low, and a complex reaction mixture was obtained. By using this type of approach, and optimizing the synthetic procedure, CA inhibitors for positron emission tomography (PET) applications might be obtained (in the case utilizing a carrier, which is the non-radioactive derivative itself, since the affinities of such derivatives for the receptor are in the nanomolar range). Further improving of such synthetic procedures might lead to better yields and the respective CompOUnds should be used as selective ligands (also in carrier- free systems) in assessing the role of membrane bound CA isozymes or for new diagnostic tools based on PET.
- Supuran, Claudiu T.,Ilies, Marc A.,Scozzafava, Andrea
-
p. 739 - 751
(2007/10/03)
-
- Treatment of chronic inflammatory joint disease with arylsulfonamides
-
A method of treating chronic inflammatory joint disease with arylsulfonamides of the formula: wherein R1 and R2 are selected from hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, loweralkylphenyl, 2 or 3 pyrrolidinyl, 2 or 3-(N-loweralkylpyrrolidinyl, or R1 and R2 taken together may form pyrrolidinyl or piperidinyl heterocyclic amino radicals and Z is an aryl group selected from substituted or unsubstituted tetrazole, 1,3,4-thiadiazole, 1,2,4-triazole, benzothiazole, benzimidazole, imidazole, pyridyl, 4,6-dimethyl pyrimidine, benzene or naphthalene is disclosed.
- -
-
-