54981-39-4Relevant academic research and scientific papers
N - aryl sulfonamide compound, its pharmaceutical composition and its use (by machine translation)
-
Paragraph 0290-0292, (2019/04/30)
The invention discloses a category represented by the following general formula I N - aryl sulfonamide compound, to the compound as the active ingredient of the pharmaceutical composition, and their preparation for treating Lp - PLA2 In the diseases related to the activity of the use. (by machine translation)
Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2
Liu, Qiufeng,Huang, Fubao,Yuan, Xiaojing,Wang, Kai,Zou, Yi,Shen, Jianhua,Xu, Yechun
supporting information, p. 10231 - 10244 (2018/01/10)
Lipoprotein-associated phospholipase A2 (Lp-PLA2) is a promising therapeutic target for atherosclerosis, Alzheimer's disease, and diabetic macular edema. Here we report the identification of novel sulfonamide scaffold Lp-PLA2 inhibitors derived from a relatively weak fragment. Similarity searching on this fragment followed by molecular docking leads to the discovery of a micromolar inhibitor with a 300-fold potency improvement. Subsequently, by the application of a structure-guided design strategy, a successful hit-to-lead optimization was achieved and a number of Lp-PLA2 inhibitors with single-digit nanomolar potency were obtained. After preliminary evaluation of the properties of drug-likeness in vitro and in vivo, compound 37 stands out from this congeneric series of inhibitors for good inhibitory activity and favorable oral bioavailability in male Sprague-Dawley rats, providing a quality candidate for further development. The present study thus clearly demonstrates the power and advantage of integrally employing fragment screening, crystal structures determination, virtual screening, and medicinal chemistry in an efficient lead discovery project, providing a good example for structure-based drug design.
DISAZO COMPOUNDS AND THEIR USE IN INK-JET PRINTING
-
Page/Page column 19, (2010/04/28)
A compound of Formula (1) or asalt thereof: wherein: X is N or C(CN); Z is optionally substituted naphthyl;and Ar is an aryl group carrying at least one nitro substituentand optionally one or more further substituents. Also compositions, inks, printing processes, printed material and ink-jet cartridges.
Sulfonamide inhibitors of aspartyl protease
-
Example 91, (2008/06/13)
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE
-
, (2010/12/01)
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE
-
, (2010/11/30)
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
Process for the preparation of N-acetylaminoarylsulfonic acids in sulfuric acid as solvent
-
, (2008/06/13)
The invention relates to salt-free N-acetylaminoarylsulfonic acids, their preparation by acetylation with acetic anhydride or acetyl chloride, sulfuric acid, which can also contain a small amount of water and/or dimethylformamide and/or N-methylpyrrolidone, serving as the solvent, and the use of the N-acetylaminoarylsulfonic acids for the preparation of their acid chlorides.
