41339-61-1Relevant academic research and scientific papers
AZEPINO-INDOLES AND OTHER HETEROCYCLES FOR TREATING BRAIN DISORDERS
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Paragraph 0205, (2020/09/12)
The present invention provides azepino-indoles and other heterocycles and methods of using the compounds for treating brain disorders.
Development of the Vinylogous Pictet–Spengler Cyclization and Total Synthesis of (±)-Lundurine A
Nash, Aaron,Qi, Xiangbing,Maity, Pradip,Owens, Kyle,Tambar, Uttam K.
supporting information, p. 6888 - 6891 (2018/05/08)
A novel vinylogous Pictet–Spengler cyclization has been developed for the generation of indole-annulated medium-sized rings. The method enables the synthesis of tetrahydroazocinoindoles with a fully substituted carbon center, a prevalent structural motif in many biologically active alkaloids. The strategy has been applied to the total synthesis of (±)-lundurine A.
Bicyclic derivatives of the potent dual aromatase-steroid sulfatase inhibitor 2-bromo-4-{[(4-cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl} phenylsulfamate: Synthesis, SAR, crystal structure, and in vitro and in vivo activities
Wood, Paul M.,Woo, L. W. Lawrence,Labrosse, Jean-Robert,Thomas, Mark P.,Mahon, Mary F.,Chander, Surinder K.,Purohit, Atul,Reed, Michael J.,Potter, Barry V. L.
experimental part, p. 1577 - 1593 (2011/12/01)
The design and synthesis of a series of bicyclic ring containing dual aromatase-sulfatase inhibitors (DASIs) based on the aromatase inhibitor (AI) 4-[(4-bromobenzyl)(4H-1,2,4-triazol-4-yl)amino] benzonitrile are reported. Biological evaluation with JEG-3 cells revealed structure-activity relationships. The X-ray crystal structure of sulfamate 23 was determined, and selected compounds were docked into the aromatase and steroid sulfatase (STS) crystal structures. In the sulfamate-containing series, compounds containing a naphthalene ring are both the most potent AI (39, IC50AROM=0.25 nm) and the best STS inhibitor (31, IC50STS=26 nm). The most promising DASI is 39 (IC50AROM= 0.25 nm, IC50STS=205 nm), and this was evaluated orally in vivo at 10 mgkg-1, showing potent inhibition of aromatase (93%) and STS (93%) after 3 h. Potent aromatase and STS inhibition can thus be achieved with a DASI containing a bicyclic ring system; development of such a DASI could provide an attractive new option for the treatment of hormone-dependent breast cancer.
A novel series of thromboxane A2 synthetase inhibitors with free radical scavenging and anti-peroxidative activities
Kamiya,Shirahase,Nakamura,Kanda,Matsui,Yoshimi,Kasai,Takahashi,Kurahashi
, p. 563 - 571 (2007/10/03)
A novel series of indoline derivatives with imidazole and carboxyl moieties were synthesized and evaluated for their thromboxane A2 (TXA2) synthetase inhibiting, radical scavenging and anti-peroxidative activities. Among the compounds synthesized, 3.{5-substituted-3-[2-(imidazol-1-yl)ethyl]indolin-1-yl}propionic acids showed free radical scavenging activity and inhibitory effects on lipid-peroxidation of rat brain homogenate and on arachidonate-induced TXA2-dependent aggregation of rabbit platelets. The anti-platelet and anti-peroxidative activities were related to the lipophilicity of the 5-substituent. The 5-hexyloxy derivative (13) showed about 35-fold higher inhibitory activity on TXA2 synthesis than that of ozagrel and about 100-fold higher activity on lipid peroxidation than that of α-tocopherol. Compound 13 showed in vivo anti-thrombotic effect in mice and ex vivo anti-peroxidative activity in rats.
NEW IMIDAZOLE DERIVATIVES, PRODUCTION THEREOF, AND USES THEREOF AS MEDICINES
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, (2008/06/13)
Imidazole derivatives of general formula (I) and pharmacologically acceptable salts thereof, wherein m and n are each an integer of 1 to 3, R1 is hydrogen or ester residue, and the indoline skeleton may be substituted by at least one member selected from a C1 to C10 alkyl group and a C1 to C15 alkoxy group. These compounds have excellent pharmacological actions such as inhibition of lipid peroxide formation, inhibition of platelet agglutination caused by thromboxane A2 synthetase inhibition, and vasodilation. Thus they are effectively used in preventing or treating asthma, thrombosis, embolism, arteriosclerosis, hypertension, hyperlipemia, cerebral apoplexy, cardiac infarction, dementia, diabetes, etc.
STEREOSELECTIVE TOTAL SYNTHESES OF (+/-)-18,19-DIHYDROHUNTERBURNINE, (+/-)-10-O-METHYL-18,19-DIHYDROHUNTERBURNINE, (+/-)-10-HYDROXYCORYNANTHEIDOL AND (+/-)-10-METHOXYCORYNANTHEIDOL
Lounasmaa, Mauri,Jokela, Reija,Tiainen, Lasse-Pekka
, p. 7873 - 7884 (2007/10/02)
Short, stereoselective total synthesis for (+/-)-18,19-dihydrohunterburnine, (+/-)-10-O-methyl-18,19-dihydrohunterburnine, (+/-)-10-hydroxycorynantheidol and (+/-)-10-methoxycorynantheidol are described.
Process for preparation of tryptophols
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, (2008/06/13)
A process for preparing tryptophol derivatives comprises reducing a 3-indolylglyoxylic acid ester or acid halide using an alkali metal borohydride in the presence of an alcohol or ether solvent. The tryptophol derivatives prepared are useful as intermediates to pharmacologically active compounds.
