50690-34-1Relevant academic research and scientific papers
NOVEL INHIBITORS
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Page/Page column 112-113, (2011/05/03)
The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
Synthesis and microbiological activity of some novel 5-benzamido- and 5- phenylacetamido- substituted 2-phenylbenzoxazole derivatives
Sener, Esin Aki,Temiz Arpaci, Oezlem,Yalcin, Ismail,Altanlar, Nurten
, p. 397 - 405 (2007/10/03)
The synthesis and microbiological activity of a new series of 5- benzamido- and 5-phenylacetamidosubstituted-2-phenylbenzoxazole derivatives (1-26) were described. The in vitro microbiological activity of the compounds was determined against Gram-positive, Gram-negative bacteria and the yeast Candida albicans in comparison with standard drugs. Microbiological results indicated that the synthesized compounds possessed a broad spectrum of activity against the tested microorganisms. The compounds 1, 21, 25 showed higher activity than tetracycline and streptomycin against Pseudomonas aeruginosa. (C) 2000 Elsevier Science S.A.
Synthesis of some new benzimidazole-5(6)-carboxylic acids
Goker,Olgen,Ertan,Akgun,Ozbey,Kendi,Topcu
, p. 1767 - 1773 (2007/10/03)
The title compounds, 1,2-dialkyl-benzimidazole-5(6)-carboxylic acids 34-45 were prepared at four steps; 1) preparation of mono amide derivatives 1-11 by the reaction of methyl 3,4-diaminobenzoate and substituted phenyl or phenoxyacetic acid chlorides; 2) preparation of the methyl benzimidazolecarboxylates 12-22, with zinc chloride and dry hydrogen chloride gas; 3) alkaline hydrolysis of the esters 23-33; and 4) substitution of the imidazole ring with benzyl or p-fluorobenzyl bromide, in alkali medium. 2-Aryl-benzimidazole-5(6)-carboxylic acids 50-53 were prepared via the oxidative condensation of 3,4-diaminobenzoic acid and aromatic aldehydes with cupric ion.
Spasmolytic Agents. 2. 1,2,3,4-Tetrahydro-2-naphthylamine Derivatives
Kanao, Munefumi,Hashizume, Takeshi,Ichikawa, Yoshifumi,Irie, Kiyoshi,Isoda, Sumiro
, p. 1358 - 1363 (2007/10/02)
N--1,2,3,4-tetrahydro-2-naphthylamine derivatives were synthesized from 1,2,3,4-tetrahydro-2-naphthylamines evaluated for their spasmolytic activity.Some of these compounds showed a nerve-selective effect on colon rather than stomach in anesthetized dogs and were found to be equal to or more active than the reference drug (mebeverine).The biological data have indicated some structure-activity relationships.Among these compounds, N-ethyl-N-hexyl>-1,2,3,4-tetrahydro-6-methoxy-2-naphthylamine hydrochloride (63) was found to be the most active spasmolytic agent.
