18085-76-2Relevant academic research and scientific papers
Method and using tracer charged ion channel
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Paragraph 0449; 0451; 0452-0454, (2018/08/20)
The invention provides compounds, compositions, methods, and kits for the treatment of pain, itch, and neurogenic inflammation.
Easily assembled, modular N,O-chelating ligands for Ta(V) complexation: A comparative study of ligand effects in hydroaminoalkylation with N-methylaniline and 4-methoxy-N-methylaniline
Garcia, Pierre,Payne, Philippa R.,Chong, Eugene,Webster, Ruth L.,Barron, Benedict J.,Behrle, Andrew C.,Schmidt, Joseph A.R.,Schafer, Laurel L.
, p. 5737 - 5743 (2013/07/11)
The influence of structurally related N,O-chelating ligands with additional heteroatoms (N, O, P, S) on the reactivity of in situ generated tantalum complexes for the hydroaminoalkylation of amines has been explored. Reactivity was probed by evaluating the catalytic ability of these N,O-chelating systems with N-methylaniline and 4-methoxy-N-methylaniline substrates. Enhanced reactivity is observed with amide proligands bearing an ortho-methoxyphenyl group on the nitrogen. 4-Methoxy-N-methylaniline is found to be more prone to undergo C-H functionalization via hydroaminoalkylation than N-methylaniline. The use of the related substrate 2-methoxy-N-methylaniline is not tolerated, and instead C(sp3)-O bond cleavage was observed.
Synthesis and antispasmodic activity of lidocaine derivatives endowed with reduced local anesthetic action
Costa, Jorge C.S.,Neves, Josiane S.,de Souza, Marcus V.N.,Siqueira, Rodrigo A.,Romeiro, Nelilma C.,Boechat, Nubia,Silva, Patricia M.R.e,Martins, Marco A.
, p. 1162 - 1166 (2008/09/20)
The present structure-activity relationship (SAR) study focused on chemical modifications of the structure of the local anesthetic lidocaine, and indicated analogues having reduced anesthetic potency, but with superior potency relative to the prototype in preventing anaphylactic or histamine-evoked ileum contraction. From the SAR analysis, 2-(diethylamino)-N-(trifluoromethyl-phenyl) and 2-(diethylamino)-N-(dimethyl-phenyl) acetamides were selected as the most promising compounds. New insights into the applicability of non-anesthetic lidocaine derivatives as templates in drug discovery for allergic syndromes are provided.
Synthesis and anticonvulsant activity of some ω-(1H-imidazol-1-yl)-N- phenylacetamide and propionamide derivatives
Soyer, Zeynep,Kilic, Fatma Sultan,Erol, Kevser,Pabuccuoglu, Varol
, p. 595 - 600 (2007/10/03)
In this study, eight new ω-(1H-imidazol-1-yl)-N-phenylacetamide and propionamide derivatives having 2,6-dimethyl, 2,6-dichloro, 2-chloro-6-methyl and 2-isopropyl substitutions on N-phenyl ring were synthesized to evaluate anticonvulsant activity against maximal electroshock test. The most active compounds in the series were the derivatives bearing 2-isopropyl and 2,6-dimethyl substituents on N-phenyl ring.
The synthesis and anticonvulsant activity of some omega-phthalimido-N-phenylacetamide and propionamide derivatives.
Soyer, Zeynep,Kilic, Fatma Sultan,Erol, Kevser,Pabuccuoglu, Varol
, p. 105 - 111 (2007/10/03)
In this study, by combining anilide and N', N'-phthaloylglycinamide pharmacophores which are known to produce potent anticonvulsant compounds, sixteen omega-phthalimido-N-phenylacetamide and propionamide derivatives bearing substituents at positions 2 or 2, 6 on N-phenyl ring have been synthesized. The structural confirmation of the title compounds was achieved by interpretation of spectral and analytical data. The anticonvulsant activity of the title compounds was determined against maximal electroshock seizure at 100 mg/kg dose level in mice. The preliminary screening results indicated that omega-phthalimido-N-phenylacetamide and propionamide nuclei have pronounced anticonvulsant activity against maximal electroshock seizure.
(Aminoiminomethyl) amino) alkane-carboxamides and their applications in therapy
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, (2008/06/13)
The invention to a pharmaceutical composition comprising as active principle a compound of general formula (I), in which R1, R2, R3, and A are as defined in claim 1. These compositions can be used in the treatment of patho
