50386-54-4Relevant academic research and scientific papers
Guanidine compound for preventing and treating chronic pain medication (by machine translation)
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Paragraph 0308-0309; 0315-0316, (2020/08/27)
The invention relates to a guanidine compound as shown in general formula (I) as a guanidine compound for preventing and treating chronic pain disease. A pharmaceutically acceptable salt thereof, a prodrug thereof, a solvate thereof, a deuterated substanc
Structure-activity relationship of human glutaminyl cyclase inhibitors having an N-(5-methyl-1H-imidazol-1-yl)propyl thiourea template
Lee, Jeewoo,Tran, Phuong-Thao,Hoang, Van-Hai,Thorat, Shivaji A.,Kim, Sung Eun,Ann, Jihyae,Chang, Yu Jin,Nam, Dong Woo,Song, Hyundong,Mook-Jung, Inhee,Lee, Jiyoun
, p. 3821 - 3830 (2013/07/19)
In an effort to design inhibitors of human glutaminyl cyclase (QC), we have synthesized a library of N-aryl N-(5-methyl-1H-imidazol-1-yl)propyl thioureas and investigated the contribution of the aryl region of these compounds to their structure-activity relationships as cyclase inhibitors. Our design was guided by the proposed binding mode of the preferred substrate for the cyclase. In this series, compound 52 was identified as the most potent QC inhibitor with an IC50 value of 58 nM, which was two-fold more potent than the previously reported lead 2. Compound 52 is a most promising candidate for future evaluation to monitor its ability to reduce the formation of pGlu-Aβ and Aβ plaques in cells and transgenic animals.
Tricyclic [1,2,4]triazine 1,4-dioxides as hypoxia selective cytotoxins
Hay, Michael P.,Hicks, Kevin O.,Pchalek, Karin,Lee, Ho H.,Blaser, Adrian,Pruijn, Frederik B.,Anderson, Robert F.,Shinde, Sujata S.,Wilson, William R.,Denny, William A.
supporting information; experimental part, p. 6853 - 6865 (2009/12/03)
A series of novel tricyclic triazine-di-N-oxides (TTOs) related to tirapazamine have been designed and prepared. A wide range of structural arrangements with cycloalkyl, oxygen-, and nitrogen-containing saturated rings fused to the triazine core, coupled with various side chains linked to either hemisphere, resulted in TTO analogues that displayed hypoxia-selective cytotoxicity in vitro. Optimal rates of hypoxic metabolism and tissue diffusion coefficients were achieved with fused cycloalkyl rings in combination with both the 3-aminoalkyl or 3-alkyl substituents linked to weakly basic soluble amines. The selection was further refined using pharmacokinetic/pharmacodynamic model predictions of the in vivo hypoxic potency (AUCreq) and selectivity (HCD) with 12 TTO analogues predicted to be active in vivo, subject to the achievement of adequate plasma pharmacokinetics.
TRICYCLIC 1,2,4-TRIAZINE OXIDES AND COMPOSITIONS THEREFROM FOR THERAPEUTIC USE IN CANCER TREATMENTS
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, (2008/06/13)
The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula: (I); and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
6-(4-Benzylpiperazin-1-yl)benzodioxanes as selective ligands at cloned primate dopamine D4 receptors
Hodgetts,Kieltyka,Brodbeck,Tran,Wasley,Thurkauf
, p. 3207 - 3213 (2007/10/03)
A series of novel 6-(4-benzylpiperazin-1-yl)benzodioxanes were prepared and screened at selected dopamine receptor subtypes. 6-(4-[4-Chlorobenzyl]piperazin-1-yl)benzodioxane (2d) had high affinity and selectivity for the D4 dopamine receptor su
6-(4-arylalkylpiperazin-1-yl) benzodioxane and 6-(4-arylalkylpiperazin-1-yl) chromane derivatives: dopamine receptor subtype specific ligands
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, (2008/06/13)
Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein: R1, R2, R3, R4and R5are the same or different and represent hydrogen, halogen, C1/
SYNTHESIS OF AMINO-SUBSTITUTED 2-METHYLCOUMARINS, CHROMANS, AND BENZOXEPANES AND THEIR N-(ALKYLAMINOACYL) DERIVATIVES
Daukshas, V. K.,Pyatrauskas, O. Yu.,Purvanyatskas, G. N.
, p. 266 - 270 (2007/10/02)
The isomeric compositions of the products of nitration of 2-methylcoumaran and chroman with acetyl nitrate were determined.More convenient methods for the synhtesis of 7-amino-2-methylcoumaran and 8-aminochroman were developed, and 9-amino-1-benzoxepane was obtained for the first time.Alkylaminoacylaminosubstituted 2-methylcoumarans, chromans, and 1-benzoxepanes were synthesized.A method for the synthesis of 2-bromocaproyl chloride from caproic acid was developed.
