188005-80-3Relevant academic research and scientific papers
Sulfonylamino acid derivatives
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, (2008/06/13)
The present invention is related to: (i) matrix metalloproteinase inhibitors containing sulfonylamino acid derivatives of the formula (Ia): wherein R1is hydrogen, C1-4 alkyl; R is hydrogen, C1-8 alkyl etc.; E is —CONR3—, in which R3is hydrogen, C1-4 alkyl etc., —NR3CO—, —CO—O—, —O—CO— etc.; A is hydrogen, C1-8 alkyl, C3-7 cycloalkyl, or Ar; J is bond, C2-4 alkylene etc.; G is —(CH2)m— in which m is 2, 3 or 4, or in which R6and R7is hydrogen, C1-8 alkyl etc.; and non-toxic salts thereof, (ii) novel sulfonylamino acid derivatives of the formula (Ib): wherein all the symbols are the same meaning as (i); and non-toxic salts thereof, and (iii) process for the preparation of the compound of the formula (Ib). The compounds of the formula (Ia) are useful for prevention and/or treatment of diseases induced by overexpression and excess activity of MMP. The diseases such as above, for example, are rheumatoid, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cell, autoimmune disease (Crohn's disease, Sjogren's syndrome etc.), disease caused by vascular emigration or infiltration of leukocytes, arterialization.
A comparative study of the reactions of thiophene-2-carboxanilides and related compounds
El-Sayed, Ragab A.
, p. 796 - 801 (2007/10/03)
Thiophene-2-carboxanilide and its p-chloro and p-bromo derivatives react with chlorosulfonic acid to give the corresponding sulfonyl chlorides, which react with amino acids to give the respective derivatives. Several methyl esters of the latter were prepared. Hydrazinolysis of these methyl esters yielded the hydrazides. Coupling reactions of some sulfonylamino acids with amino acid methyl ester hydrochlorides in THF-Et3N medium using the dicyclohexylcarbodiimide method give the corresponding dipeptide methyl esters. The spectral data of the compounds are briefly discussed. 1999 Kluwer Academic/Plenum Publishers.
