103860-25-9Relevant academic research and scientific papers
Synthesis of 5, 6-dichloroindan-1-acids and their tetrazolyl derivatives as analgesic and anti-inflammatory agents
Pal, Rajib Kumar,Yasmin, Hasina,Nahar, Lutfun,Datta, Bidyut Kanti,Kundu, Joydeb Kumar,Bachar, Sitesh Chandra,Chowdhury, Abul Kalam Azad,Sarker, Satyajit Dey
, p. 874 - 882,9 (2020/08/31)
Indan derivatives, namely, 5-(5′,6′-dichloroindan-1′-yl)- tetrazole (12a) and 5-(5′,6′-dichloroindan-1′-yl)- methyltetrazole (12b), were synthesized conveniently from 5,6-dichloroindan-1- carboxylic acid (9a) and 5,6- dichloroindan-1-acetic acid (9b), respectively, as potential analgesic and anti-inflammatory agents. The analgesic and anti-inflammatory properties of 9a, 9b, 12a and 12b were evaluated by the acetic acid induced writhing in Swiss albino mice and the carrageenan-induced rat paw edema models, respectively. Compounds 9a and 12a exhibited significant analgesic activity with the doses of 50 and 100 mg/kg body weight, comparable to that of the positive controls, phenylbutazone, indomethacin and aminopyrine. The anti-inflammatory potencies of 9a and 12a were also comparable to that of the positive control, phenylbutazone. Compounds 9b and 12b showed analgesic and anti-inflammatory activities, but were weaker than that of compounds 9a and 12a.
4-benzimidazolyl-3-phenylbutanoic acids as novel pif-pocket-targeting allosteric inhibitors of protein kinase PKCΧ
Fr?hner, Wolfgang,Lopez-Garcia, Laura A.,Neimanis, Sonja,Weber, Nadja,Navratil, Jeanette,Maurer, Frauke,Stroba, Adriana,Zhang, Hua,Biondi, Ricardo M.,Engel, Matthias
, p. 6714 - 6723 (2011/12/02)
Protein kinase inhibitors with an allosteric mode of action are expected to reach, in many cases, higher selectivity for the target enzyme than ATP-competitive compounds. Therefore, basic research is aiming at identifying and establishing novel sites on the catalytic domain of protein kinases which might be targeted by allosteric inhibitors. We previously published the first structure-activity relationships (SARs) for allosteric activators of protein kinase PDK1. Here, we present the design, synthesis, and SAR data on a series of novel compounds, 4-benzimidazolyl-3-phenylbutanoic acids, that inhibit the atypical protein kinace C (PKC) Χ via binding to the PIF-pocket. Key positions were identified in the compounds that can be modified to increase potency and selectivity. Some congeners showed a high selectivity toward PKCΧ, lacking inhibition of the most closely related isoform, PKC1, and of further AGC kinases. Furthermore, evidence is provided that these compounds are also active toward cellular PKCΧ without loss of potency compared to the cell-free assay.
Enzymatic desymmetrization of 3-arylglutaric acid anhydrides
Fryszkowska, Anna,Komar, Marta,Koszelewski, Dominik,Ostaszewski, Ryszard
, p. 2475 - 2485 (2007/10/03)
Optically active (R)- and (S)-3-arylglutaric acid monoesters 3 were synthesized in quantitative yields and good stereoselectivities by lipase-catalyzed desymmetrization of the corresponding 3-arylglutaric anhydrides 2 with alcohols. It was observed that the stereochemical outcome of the reaction was influenced by the substituents present on the aromatic ring. The influence of the enzyme, alcohol, and solvent was systematically examined. Absolute configurations of the monoesters 3 were assigned by chemical correlation to corresponding lactones 4.
Piperidine derivatives as neurokinin antagonists
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, (2008/06/13)
The invention relates to compounds of the formula STR1 wherein X, i, j, n, n', A, A', R2, R3, and U are as described herein. The compounds of the invention are NK1 or NK2 or NK3 receptor antagonists and as such are useful in the treatment of diseases such as asthma.
