301847-57-4Relevant academic research and scientific papers
Inhibitors of 15-Prostaglandin Dehydrogenase To Potentiate Tissue Repair
Antczak, Monika I.,Zhang, Yongyou,Wang, Changguang,Doran, Jennifer,Naidoo, Jacinth,Voruganti, Sukesh,Williams, Noelle S.,Markowitz, Sanford D.,Ready, Joseph M.
, p. 3979 - 4001 (2017)
The enzyme 15-prostaglandin dehydrogenase (15-PGDH) catalyzes the first step in the degradation of prostaglandins including PGE2. It is a negative regulator of tissue repair and regeneration in multiple organs. Accordingly, inhibitors of 15-PGDH are anticipated to elevate in vivo levels of PGE2 and to promote healing and tissue regeneration. The small molecule SW033291 (1) inhibits 15-PGDH with Ki = 0.1 nM in vitro, doubles PGE2 levels in vivo, and shows efficacy in mouse models of recovery from bone marrow transplantation, ulcerative colitis, and partial hepatectomy. Here we describe optimized variants of 1 with improved solubility, druglike properties, and in vivo activity.
COMPOSITIONS AND METHODS OF MODULATING 15-PGDH ACTIVITY
-
, (2013/11/05)
Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.
Synthesis and reactions of some new heterocyclic compounds containing the thienylthieno[2,3-b]pyridine moiety
Bakhite, Etify A.,Abdel-Rahman, Abdu E.,Mohamed, Omima S.,Thabet, Eman A.
, p. 1983 - 2006 (2007/10/03)
(4-Aryl-3-cyano-6-(2-thienyl)pyridin-2-ylthio)acethydrazides (5a-c), 3-amino-4-aryl-6-(2-thienyl)thieno[2,3-b]pyridine-2-carbohydrazides (6a-c) and 3-amino-4-phenyl-6-(2-thienyl)thieno[2,3-b]pyridine-2-carboxylic acid (30) were prepared and employed as key intermediates in the synthesis of the title compounds.
