104941-65-3Relevant academic research and scientific papers
Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent
Brachet, Etienne,Dumond, Aurore,Liu, Wang-Qing,Fabre, Marie,Selkti, Mohamed,Raynaud, Fran?oise,Hermine, Olivier,Benhida, Rachid,Belmont, Philippe,Garbay, Christiane,Lepelletier, Yves,Ronco, Cyril,Pagès, Gilles,Demange, Luc
, (2019)
We report herein the synthesis of a newly described anti-cancer agent, NRPa-308. This compound antagonizes Neuropilin-1, a multi-partners transmembrane receptor overexpressed in numerous tumors, and thereby validated as promising target in oncology. The p
Discovery and in Vitro Optimization of 3-Sulfamoylbenzamides as ROMK Inhibitors
Sammons, Matthew F.,Kharade, Sujay V.,Filipski, Kevin J.,Boehm, Markus,Smith, Aaron C.,Shavnya, Andre,Fernando, Dilinie P.,Dowling, Matthew S.,Carpino, Philip A.,Castle, Neil A.,Zellmer, Shannon G.,Antonio, Brett M.,Gosset, James R.,Carlo, Anthony,Denton, Jerod S.
supporting information, p. 125 - 130 (2018/02/19)
Inhibitors of the renal outer medullary potassium channel (ROMK) show promise as novel mechanism diuretics, with potentially lower risk of diuretic-induced hypokalemia relative to current thiazide and loop diuretics. Here, we report the identification of a novel series of 3-sulfamoylbenzamide ROMK inhibitors. Starting from HTS hit 4, this series was optimized to provide ROMK inhibitors with good in vitro potencies and well-balanced ADME profiles. In contrast to previously reported small-molecule ROMK inhibitors, members of this series were demonstrated to be highly selective for inhibition of human over rat ROMK and to be insensitive to the N171D pore mutation that abolishes inhibitory activity of previously reported ROMK inhibitors.
Inhibitors of Neuropilin and use thereof for the treatment of Neuropilin-related diseases
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, (2015/02/02)
The present invention relates to a compound of general formula (I), and salts or solvate thereof, for treating a Neuropilin-related disease, disorder or condition; and to a composition, a pharmaceutical composition and a medicament comprising the compound of general formula (I).
INHIBITOR OF NEUROPILIN AND USE THEREOF FOR THE TREATMENT OF NEUROPILIN-RELATED DISEASES
-
, (2015/02/02)
The present invention relates to a compound of general formula (I), and salts or solvate thereof, for treating a Neuropilin-related disease, disorder or condition; and to a composition, a pharmaceutical composition and a medicament comprising the compound of general formula (I).
Synthesis, characterization and antimicrobial activity of bifunctional sulfonamide-amide derivatives
Abbavaram, Babul Reddy A.,Reddyvari, Hymavathi R.V.
, p. 731 - 737 (2014/02/14)
A convenient synthesis of bifunctional sulfonamide-amide derivatives was reported. Amide coupling of 4-methyl benzoic acid 1 followed by reaction with chlorosulfonic acid produce ethyl-4-(3-(chlorosulfonyl)-4-methylbenzoyl) piperazine-1-carboxylate 4. The
