117571-33-2Relevant academic research and scientific papers
N-(PYRIDIN-2-YLSULFONYL)CYCLOPROPANECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF A CFTR MEDIATED DISEASE
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Page/Page column 236, (2020/07/14)
The invention relates to heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.
Solid-phase synthesis of new saphenamycin analogues with antimicrobial activity
Laursen, Jane B.,De Visser, Peter C.,Nielsen, Henrik K.,Jensen, Knud J.,Nielsen, John
, p. 171 - 175 (2007/10/03)
An array of 12 new saphenamycin analogues modified at the benzoate moiety was synthesized on solid support. Synthesis commenced with a chemoselective anchoring of saphenic acid through the carboxyl group to a 2-chlorotrityl functionalized polystyrene resin. The secondary alcohol was acylated in parallel with a series of differently substituted benzoic acid derivatives. Treatment with TFA-CH2Cl2 (5:995) released the expected saphenamycin analogues into solution. These new analogues were purified, characterized and screened for antimicrobial activity against Bacillus subtilis and Proteus mirabilis. Eight analogues exhibited MIC values against B. subtilis ranging from 0.07 to 3.93 μg/mL, comparable to the activities of previously reported saphenamycin analogues.
Aromatic amino ethers as pain relieving agents
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, (2008/06/13)
The present invention relates to compounds of formula (I), STR1 wherein A is an optionally substituted phenyl naphthyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidyl, thienyl, thiazolyl, oxazolyl, thiadiazolyl having at least two adjacent ring carbon atoms or a bicyclic ring system, provided that the --CH(R3)N(R2)B--R1 and --OCH(R4 --)--D linking groups arm positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the --OCHR4 -- linking group (and therefore in the 3-position relative to the --CHR3 NR2 -- linking group) is not substituted; B is an optionally substituted ring system; D is an optionally substituted ring system; R1 is a variety of group as defined in the description; R2 is hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, phenylC1-3 alkyl or 5- or 6-membered heteroarylC1-3 alkyl; R3 is hydrogen or C1-4 alkyl; R4 is hydrogen or C1-4 alkyl; and N-oxides of NR2 where chemically possible; and S-oxides of sulphur containing rings were chemically possible; and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof. Process for their preparation, intermediates in theirpreparation, their use as therapeutic agents and pharmaceutical compositions containing them.
Compounds having antitumor and antibacterial properties
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, (2008/06/13)
The novel class of xanthenone-4-acetic acids represented by the general formula (I) STR1 where R1 represents up to two of the groups lower alkyl, halogen, CF3, CN, NO2, NH2, CH2 COOH, OR2,
Potential Antitumor Agents. 58. Synthesis and Structure-Activity Relationships of Substituted Xanthenone-4-acetic Acids Active against the Colon 38 Tumor in Vivo
Rewcastle, Gordon W.,Atwell, Graham J.,Baguley, Bruce C.,Calveley, Stephen B.,Denny, William A.
, p. 793 - 799 (2007/10/02)
In a search for compounds related to flavoneacetic acid with activity against solid tumors, a series of methyl- methoxy-, chloro, nitro-, and hydroxy-substituted xanthenone-4-acetic acids have been synthesized and evaluated against subcutaneously implanted colon adenocarcinoma 38 in vivo, using a short-term histology assay as a primary screening system.A major goal of this work was to identify compounds with similar profiles of activity to that of flavoneacetic acid but of higher potency.The level of activity of the compounds appeared to depend more on the nature of the substituent than its positioning, in the order Cl > Me, OMe > NO2, OH.However, the potency of the compounds was related much more to the position rather than the nature of the substitution, with 5-substituted compounds being clearly the most dose potent. 5-Methylxanthenone-4-acetic acid has a similar level of activity to that of flavoneacetic acid in the test systems employed but is more than 7-fold as does potent.
