22339-62-4Relevant academic research and scientific papers
FUNCTIONALIZED LONG-CHAIN HYDROCARBON MONO- AND DI-CARBOXYLIC ACIDS AND THEIR USE FOR THE PREVENTION OR TREATMENT OF DISEASE
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Paragraph 0549-0551, (2021/01/29)
This invention provides compounds of Formulae (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH), (IJ), (IK), (IL), (II), (III), (IIIA), and (IIIB); pharmaceutically acceptable salts and solvates thereof; and compositions thereof. This invention further provides methods for treating a disease, including but not limited to, liver disease or an abnormal liver condition; cancer (such as hepatocellular carcinoma or cholangiocarcinoma); a malignant or benign tumor of the lung, liver, gall bladder, bile duct or digestive tract; an intra- or extra-hepatic bile duct disease; a disorder of lipoprotein; a lipid-and-metabolic disorder; cirrhosis; fibrosis; a disorder of glucose metabolism; a cardiovascular or related vascular disorder; a disease resulting from steatosis, fibrosis, or cirrhosis; a disease associated with increased inflammation (such as hepatic inflammation or pulmonary inflammation); hepatocyte ballooning; a peroxisome proliferator activated receptor-associated disorder; an ATP citrate lyase disorder; an acetyl-coenzyme A carboxylase disorder; obesity; pancreatitis; or renal disease.
Mono- and bis-thiazolium salts have potent antimalarial activity
Hamzé, Abdallah,Rubi, Eric,Arnal, Pascal,Boisbrun, Michel,Carcel, Carole,Salom-Roig, Xavier,Maynadier, Marjorie,Wein, Sharon,Vial, Henri,Calas, Michèle
, p. 3639 - 3643 (2007/10/03)
Three new series comprising 24 novel cationic choline analogues and consisting of mono- or bis (N or C-5-duplicated) thiazolium salts have been synthesized. Bis-thiazolium salts showed potent antimalarial activity (much superior to monothiazoliums). Among them, bis-thiazolium salts 12 and 13 exhibited IC50 values of 2.25 nM and 0.65 nM, respectively, against P. falciparum in vitro. These compounds also demonstrated good in vivo activity (ED50 ≤ 0.22 mg/kg), and low toxicity in mice infected by Plasmodium vinckei.
Synthesis and characterization of derivatized capped porhyrins
Tang, Hang,Wijesekera, Tilak P.,Dolphin, David
, p. 1366 - 1374 (2007/10/02)
The syntheses of porphyrins carrying either a fully hydrophobic cavity with a benzene moiety (32a,b) or a polar cavity with an amidobenzene (32c-d) are described.Terephthaldehyde (1) was converted to benzene-bisalkanoic acids (8, 10) and nitrobenzene-bisalkanoic acids (13 and 16) by using standard methods.The corresponding diacid chlorides 17a-d were used to acylate two equivalents of a β-unsubstituted pyrrole, and the ketonic groups were reduced by diborane.Following the transformation of the nitro function to the acetamide, appropriate modifications of the ethyl ester functions afforded the key bisformylpyrroles 25a-d.The cyanoacrylate-protected formyl pyrrole derivatives were monochlorinated at the α-methyl groups and condensed with two equivalents of an α-unsubstituted pyrrole to give the dipyrromethane dimers.Strong aqueous alkali caused saponification of the two ester groups and deprotection of the formyl functions to produce the dipyrromethane dimer 30, which, after thermal decarboxylation, was cyclized intramolecularly in acidic medium to give the porphyrins 32 (n = 4 or 5, X = H or NHCOCH3).
Both-faces Hindered Porphyrins. Part 1. Synthesis and Characterization of Basket-handle Porphyrins and Their Iron Complexes
Momenteau, Michel,Mispelter, Joel,Loock, Bernard,Bisagni, Emile
, p. 189 - 196 (2007/10/02)
The synthesis of the 'both-faces' hindered porphyrins using two different methods is reported.These so-called 'basket-handle' porphyrins (BHP) are derived from 5,10,15,20-tetraphenylporphyrin in which two opposite phenyl groups are bridged by alkylene or arylene-p-bisalkylene chains.In addition to the desired compounds , two other isomers were obtained .These were separated by t.l.c. on silica gel and then individually characterized.The structural assignment of the three isomers in the five series studied was based on the 1H n.m.r. spectra of the free bases and of their iron(II) complexes.
