2487-40-3Relevant articles and documents
2-Alkyloxyalkylthiohypoxanthines as new potent inhibitors of xanthine oxidase.
Biagi,Giorgi,Pacchini,Livi,Scartoni
, p. 809 - 813 (2001)
The title compounds were prepared and tested as xanthine oxidase (XO) inhibitors. Results evidenced that potency was related to the position of the oxygen atom in the 2-linear chain and that it grew with distance from the sulfur atom until it became equipotent to 2-n-hexylthiohypoxanthine. Enzymatic oxidation on C(2) occurred in the 8-alkylthiohypoxanthines. On the contrary, oxidation on C(8) did not occur in the 2-alkythioderivatives, demonstrating that the chain forced these molecules to form a complex with molybdenum(VI) involving only the N(3) and N(9) nitrogen atoms.
Discovery and evaluation of new compounds targeting ribosomal protein S1 in antibiotic-resistant Mycobacterium Tuberculosis
Dai, Yazhuang,Guo, Chenyun,Lin, Donghai,Lin, Kejiang,Xu, Yinqiu,Xue, Xiaowen
, (2020/04/20)
The emergence of antibiotic-resistant Mycobacterium Tuberculosis (Mtb) infections compels new treatment strategies, of which targeting trans-translation is promising. During the trans-translation process, the ribosomal protein S1 (RpsA) plays a key role, and the Ala438 mutant is related to pyrazinamide (PZA) resistance, which shows its effects after being hydrolysed to pyrazinoic acid (POA). In this study, based on the structure of the RpsA C-terminal domain (RpsA-CTD) and POA complex, new compounds were designed. After being synthesized, the compounds were tested in vitro with saturation transfer difference (STD), fluorescence quenching titration (FQT) and chemical shift perturbation (CSP) experiments. Finally, six of the 17 new compounds have high affinity for both RpsA-CTD and its Ala438 deletion mutant. The active compounds provide new choices for targeting trans-translation in Mtb, and the analysis of the structure-activity relationships will be helpful for further structural modifications based on derivatives of 2-((hypoxanthine-2-yl)thio)acetic acid and 2-((5-hydroxylflavone-7-yl)oxy)acetamide.
POTASSIUM CHANNEL MODULATORS
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Paragraph 0371-0372, (2018/01/14)
Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with potassium channels. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with potassium channels.
Substituted 6-(Benzylamino) Purine Riboside Derivatives, Use Thereof and Compositions Containing These Derivatives
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Page/Page column 12, (2012/04/04)
The invention relates to 2-substituted-6-(substituted benzylamino)purine riboside derivatives of the general formula I. These compounds possess antiapoptotic, anti-inflammatory and differentiating activities. The invention relates also to the compositions, which contain these derivatives as active ingredients.
SUBSTITUTED 6-(BENZYLAMINO) PURINE RIBOSIDE DERIVATIVES, USE THEREOF AND COMPOSITIONS CONTAINING THESE DERIVATIVES
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Page/Page column 30-31, (2010/12/17)
The invention relates to 2-substituted-6-(substituted benzylamino)purine riboside derivatives of the general formula I. These compounds possess antiapoptotic, anti-inflammatory and differentiating activities. The invention relates also to the compositions, which contain these derivatives as active ingredients. ˙
SUBSTITUTED 6-ANILINOPURINE DERIVATIVES AS INHIBITORS OF CYTOKININ OXIDASE/DEHYDROGENASE AND PREPARATIONS CONTAINING THESE DERIVATIVES
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Page/Page column 8, (2010/08/07)
The invention relates to substituted 6-anilinopurine derivatives of the general formula I, wherein R denotes one to five substituents independently selected from the group consisting of hydrogen, halogen, hydroxyl, amino, alkyloxy and alkyl group, and R2 denotes amino, halogen, nitro, thio, alkylthio or alkyl group for use as inhibitors of cytokinin oxidase/dehydrogenase. The invention also relates to the compositions containing these derivatives.
NEW SYNTHETIC APPROACH FOR AZOLOPURINES AND ANALOGS
Tisler, Miha,Stanovnik, Branko,Zrimsek, Zdenka
, p. 405 - 411 (2007/10/02)
A new synthetic approach has been developed for the synthesis of some azolopurines, i.e. derivatives of 1,2,4-triazolo(3,4-b)purine (3) and pyrrolo(2,1-b)purine (8), and for some pyrazolo(3,4-d)pyrimidines (12,14).
