- Drug-protein conjugates: Haptenation of 1-methyl-10α- methoxydihydrolysergol and 5-bromonicotinic acid to albumin for the production of epitope-specific monoclonal antibodies against nicergoline
-
Two types of monoclonal antibodies were used for the determination of nicergoline in biological matrices. The antibodies were prepared with the hydrolysis products 5-bromonicotinic acid and 1-methyl-10α- methoxydihydrolysergol after hemisuccinoylation to haptens. The current amide bond-generating methods (mixed anhydride-, carbodiimide-, carbodiimide/sulfo- N-hydroxysuccinimide-, and dicyclohexylcarbodiimide/N-hydroxysuccinimide methods) were used in bovine serum albumin (BSA)-coupling techniques and yielded conjugates that were haptenated to varying extents. The conjugates exhibiting 23 mol of 1-methyl-10α-methoxydihydrolysergol (MMD) or 41 mol of 5-bromonicotinic acid (BNA) per mole of BSA were used for both immunization of mice and for coating the wells of the microtiter plates to select hybridomas and investigate specificity of the obtained antibodies. The results of hapten-inhibition ELISA using antigen-coated wells indicate that the supernatant of MMD-specific hybridoma exhibited 50% inhibition of antibody binding at 17 ± 2 μg of MMD and at 24.5 ± 2 μg of nicergoline, and the BNA-specific hybridoma exhibited similar inhibition at 147 ± 6 μg of BNA and 500 ± 30 μg of nicergoline. A main requirement for analytical purposes is that two different types of monoclonal antibodies recognize two different epitopes on nicergoline and its main metabolite, as shown by hapten-inhibition ELISA.
- Gabor,Hamilton,Pittner
-
-
Read Online
- INHIBITORS OF MYOCARDIN-RELATED TRANSCRIPTION FACTOR AND SERUM RESPONSE FACTOR (MRTF/SRF)-MEDIATED GENE TRANSCRIPTION AND METHODS FOR USE OF THE SAME
-
Disclosed herein are inhibitors of gene transcription mediated by myocardin-related transcription factor and serum response factor, or both myocardin-related transcription factor and serum response factor ("MRTF/SRF"), and methods for their use in treating or preventing cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts thereof: wherein the substituents are as described.
- -
-
Paragraph 00198
(2016/06/01)
-
- Amyl nitrite-mediated conversion of aromatic and heteroaromatic primary amides to carboxylic acids
-
A series of aromatic and heteroaromatic primary amides were converted directly to carboxylic acids by heating with amyl nitrite in acetic acid. Most conversions proceeded to give reasonable to excellent yields on a range of substrates containing various functional groups. This reagent system is thus applicable for the direct hydrolysis of a range of different primary carboxamides. The reaction with a phenolic aromatic substrate afforded two alternative nitration products as major outcomes, evidencing alternative reaction pathways resulting from the free phenolic OH.
- Potter, Garrett T.,Jayson, Gordon C.,Miller, Gavin J.,Gardiner, John M.
-
supporting information
p. 5153 - 5156
(2015/08/19)
-
- AZOLECARBOXAMIDE HERBICIDES
-
Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation, wherein J is (J-1), (J-2,(J-3), (J-4), (J-5), (J-6), (J-7), (J-8) and R1a, R1b, R1c, R2a, R2b, R3, R4, R05, T, U, W, Y and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula (I). Also disclosed are mixtures and compositions comprising a herbicidally effective amount of a compound of Formula (Iz) wherein J, R1a, R1b, R1c, R2a, R2b, R3, R4, R05, T, U, W, Y and Z are as defined in the disclosure; and an effective amount of another herbicide or herbicide safener. Also disclosed is a method for selectively controlling undesired vegetation in a crop that involves contacting the locus of a crop with an effective amount of a compound of Formula (Iz) and a effective amount of a safener.
- -
-
-
- Synthesis of formylphenylpyridinecarboxylic acids using Suzuki-Miyaura coupling reactions
-
Formylphenylboronic acids were coupled with bromopyridylcarboxylic acids in the presence of a palladium catalyst. The yields of the different biaryls are strongly dependant on the substitution pattern of the two coupling partners. The electronic and steric effects of these are discussed.
- Meier, Peter,Legraverant, Stephanie,Mueller, Sascha,Schaub, Josette
-
p. 551 - 554
(2007/10/03)
-
- Chiral organometallic NADH mimics: Highly stereoselective reductions of ethyl benzoylformate with a 1,4-dihydronicotinoyl fragment attached to the homochiral auxiliary 5-C5H5)Fe(CO)(PPh3)> and possessing a homochiral β-hydroxy-carboxamide at C-5.
-
A series of homochiral organometallic NADH mimics incorporating the chiral auxiliary 5-C5H5)Fe(CO)(PPh3)> at the C-3 carbonyl and a chiral carboxamide at C-5 of a 1,4-dihydronicotinoyl fragment have been prepared.These complexes were shown to stereoselectively reduce ethyl benzoylformate to either (R)- or (S)-ethyl mandelate by a combination of steric and chelation control.For example, complex (R,R)-12 bearing a carboxamide derived from (R)-(+)-methylbenzylamine afforded (R)-ethyl mandelate in 89percent enantiomeric excess.Utilisation of complexes (R,S)-19a and (R,R,S)-22a bearing chiral β-hydroxy-carboxamides derived from valinol and norephedrine respectively gave the (R)-ethyl mandelate in greater than 97percent enantiomeric excess.
- Burgess, Vicky A.,Davies, Stephen G.,Skerlj, Renato T.,Whittaker, Mark
-
p. 871 - 901
(2007/10/02)
-
- Process for preparing lysergol derivatives
-
A novel process is disclosed for the preparation of derivatives of lysergol having the general formula: STR1 According to this process lysergol is directly used as the starting compound and, after the methylation at the 1 position of the corresponding 10 alpha-methoxy-lumilysergol, the methylated compound is directly esterified with a carboxylic acid R--COOH, the acid being selected in the group comprising aliphatic, cycloaliphatic, aromatic, and heterocyclic carboxylic acids, containing up to 10 carbon atoms.
- -
-
-
