19651-44-6Relevant articles and documents
KCNT1 INHIBITORS AND METHODS OF USE
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Paragraph 000628, (2020/11/23)
The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
Screening of ligands for the Ullmann synthesis of electron-rich diaryl ethers
Otto, Nicola,Opatz, Till
supporting information; experimental part, p. 1105 - 1111 (2012/09/07)
In the search for new ligands for the Ullmann diaryl ether synthesis, permitting the coupling of electron-rich aryl bromides at relatively low temperatures, 56 structurally diverse multidentate ligands were screened in a model system that uses copper iodide in acetonitrile with potassium phosphate as the base. The ligands differed largely in their performance, but no privileged structural class could be identified.
Palatability of aquaculture feed
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, (2008/06/13)
A method for enhancing the palatability of aquaculture food, the method comprising treating the food with a compound of Formula I: wherein R1, R2, R3, and n are as defined herein, are disclosed.
N-Salicylideneamino acidato complexes of oxovanadium(IV). the cysteine and penicillamine complexes
Pessoa, Joao Costa,Calhorda, Maria J.,Cavaco, Isabel,Costa, Paulo J.,Correia, Isabel,Costa, Dina,Vilas-Boas, Luis F.,Felix, Vitor,Gillard, Robert D.,Henriques, Rui T.,Wiggins, Robert
, p. 2855 - 2866 (2007/10/03)
Oxovanadium(iv) complexes with ligands derived from the reaction of salicylaldehyde with L-cysteine and with D- and D,L-penicillamine are prepared. The compounds are characterised by elemental analysis, spectroscopy (UV-VIS, CD, EPR), TG, DSC and magnetic susceptibility measurements (9-295 K). We discuss several aspects related to the structure of these complexes in the solid state and in solution; in particular, the possibility of forming thiazolidine complexes, and their comparison with the characterised complexes is studied by molecular mechanics and density functional theory calculations. The solution structures depend on pH and solvent, and while with L-Cys the spectroscopic results show trends similar to those of the L-Ala and L-Ser systems up to ca. pH 8-9, where thiolate coordination starts being detected, the penicillamine system is quite distinct, namely thiolate coordination occurs for pH > 6.5. In the presence of salicylaldehyde and VIVO the desulfydration of cysteine proceeds rapidly, but no similar reaction occurs with penicillamine, although its decomposition is also activated. The DFT calculations do not indicate any energetic basis for this distinct reactivity, which possibly results from different complexes present in the Cys and Pen systems. In the cysteine system, the N-salicylidene dehydroalanine-VIVO complex V is believed to form in an intermediate stage of the desulfydration. Further, addition of several nucleophiles to the cysteine reaction mixtures produce amino acid derivatives by a Michael-type base-catalysed addition, a result compatible with the formation of V. The products of these reactions were analysed by TLC and HPLC, and in some cases isolated.
Amino Acids, 12. - Syntheses of DL-Cysteines from Acrylic Acid Derivatives
Effenberger, Franz,Beisswenger, Thomas,Dannenhauer, Fritz
, p. 2209 - 2224 (2007/10/02)
The addition of sulfenyl chlorides 1 to 2-alkenoic acid esters 2 gives mixtures of 2(3)-chloro-3(2)-thioalkenoic acid esters 3/4, whereas the addition of thiols 7 to methyl 2-chloro-2-propenoate (6) results in the formation of methyl 2-chloro-3-thiopropanoates 3 only.The dependence of the isomerization of 3 to 4 on the reaction conditions was investigated; at higher temperatures the formation of 4 is especially favored.At temperatures below 55 deg C the 2-azido compounds 8 are obtained without isomerization from 3 by reaction with sodium azide in the presence of a PT catalyst.Cysteine derivatives 9 or 10, resp., are obtained by hydrogenation of 8 with H2S/pyridine/H2O or with H2/Re2S; the overall yields of 9 or 10, resp., starting from 6 are as high as 70percent.DL-Cysteine is obtained in good overall yields as hydrochloride hydrate 16 by HCl-catalyzed hydrolysis of the 2-thiazolines 15a*HCl and 15e, which are prepared by HCl-catalyzed addition of thioacetamide (11a) to α-chloroacrylic acid (12) or the amide 13 and consecutive ring closure.
S-substituted 2-azido-3-mercapto-propionic acid ester and process for its production and use
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, (2008/06/13)
The subject matter of the invention are S-substituted 2-azido-3-mercapto-propionic acid esters of the general formula STR1 in which R1 is a methyl or ethyl group and R2 is an unsubstituted or substituted alkyl group, a cycloalkyl group, an unsubstituted or substituted aromatic or heteroaromatic group or a benzyl group, and a process for their production by reaction of a methyl or ethyl ester of 2-chloroacrylic acid with a corresponding thiol to form an S-substituted 2-chloro-3-mercapto-propionic acid ester and subsequently exchanging the chlorine atom with an azido group as well as use of the compounds of formula (I) as intermediate products in the production of D,L-cysteine or derivatives of D,L-cysteine.
Sulfur containing trialkoxybenzoylamino carboxylic acids
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, (2008/06/13)
Compounds are prepared of the formula: STR1 wherein A is a straight or branched chain alkylene or alkylidene radical having 2 to 5 carbon atoms and which is substituted by an alkylthio group having 1 to 4 carbon atoms, a carboxymethyl thio group, a carboxyethyl thio group, an alkylsulfonyl group having 1 to 4 carbon atoms, a mercapto group, or the substituent on A together with --COR4 forms a 4 to 7 membered thiolactone ring, or A is substituted by an acylmercapto group wherein the acyl is benzoyl, a benzoyl radical substituted with one, two or three alkoxy groups with 1 to 6 carbon atoms, an alkanoyl radical of 1 to 6 carbon atoms, an alkenoyl radical of 3 to 6 carbon atoms, R1, R2 and R3 are the same or different and are alkyl groups of 1 to 5 carbon atoms and one of R1, R2 and R3 also can be hydrogen or the acyl radical of an alkanoic acid of 2 to 4 carbon atoms and R4 is a hydroxy group or an alkoxy group with 1 to 5 carbon atoms and their pharmacologically acceptable salts. The compounds are pharmacodynamically active and are suited for prophylaxis and treatment of heart illnesses such as cardiac ischemia, cardiac infarct, heart rhythm and circulatory disturbances.
Pyrimidinylpropenamides as antitumor agents. Analogues of the antibiotic sparsomycin
Lin,Dubois
, p. 337 - 341 (2007/10/06)
A series of pyrimidinylpropenamides 9 and their oxidation products 10 was prepared, as analogues of sparsomycin (1), for antitumor evaluation. Syntheses involved condensation of the appropriate amino alcohol 5 with acid 8. The resulting sulfides 9 were then oxidized with NaIO4 or H2O2 to sulfoxides 10. Activity was studied in lymphocytic leukemia P-388 and KB cell culture. With the exception of the n-decyl analogue, all of the deoxygenated compounds 9 were inactive regardless of the sterochemical form. In the sulfoxide series 10, those compounds prepared with an L configuration at the asymmetric carbon were also inactive. The completely racemic sulfoxides, on the other hand, displayed substantial antitumor activity (ILS=37-61% in P-388; ED50=1.2-2.4μg/ml in KB) suggesting that both the presence of a sulfoxide moiety and a D configuration at the chiral carbon atom were structural requirements for a positive antitumor response. There appeared to be a large tolerance for the group substituted at the sulfoxide moiety, however.
