23776-98-9Relevant articles and documents
Design, synthesis and in vitro evaluation studies of sulfonyl-amino-acetamides as small molecule BACE-1 inhibitors
Jain, Priti,Wadhwa, Pankaj K.,Gunapati, Sinduri,Jadhav, Hemant R.
, p. 2567 - 2575 (2016/05/10)
The identification of a series of sulfonyl-amino-acetamides as BACE-1 (β-secretase) inhibitors for the treatment of Alzheimer's disease is reported. The derivatives were designed based on the docking simulation study, synthesized and assessed for BACE-1 inhibition in vitro. The designed ligands revealed desired binding interactions with the catalytic aspartate dyad and occupance of S1 and S2′ active site regions. These in silico results correlated well with in vitro activity. Out of 33 compounds synthesized, 12 compounds showed significant inhibition at 10 μM concentration. The most active compound 2.17S had IC50 of 7.90 μM against BACE-1, which was concomitant with results of in silico docking study.
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.
Novel inhibitors of rat lens aldose reductase: N-[[(substituted amino)phenyl]sulfonyl]glycines
Mayfield,DeRuiter
, p. 1595 - 1598 (2007/10/02)
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