3788-94-1Relevant articles and documents
Multi-targeting exploration of new 2-aminothiazolyl quinolones: Synthesis, antimicrobial evaluation, interaction with DNA, combination with topoisomerase IV and penetrability into cells
Cheng, Yu,Avula, Srinivasa Rao,Gao, Wei-Wei,Addla, Dinesh,Tangadanchu, Vijai Kumar Reddy,Zhang, Ling,Lin, Jian-Mei,Zhou, Cheng-He
, p. 935 - 945 (2016)
A series of new potentially multi-targeting antimicrobial 2-aminothiazolyl quinolones were designed, synthesized and characterized by1H NMR,13C NMR, IR, MS and HRMS spectra. Bioactive assay manifested that some of the prepared compounds showed moderate to good antibacterial and antifungal activities. Noticeably, compound 10f could effectively inhibit the growth of B. typhi and MRSA with MIC values of 1 and 8 μg/mL, respectively. Experimental results revealed that compound 10f was membrane-active and had the ability to rapidly kill the tested strains and effectively prevent the development of bacterial resistance. Moreover, this compound also exhibited low toxicity against L929 cells. Molecular docking indicated that compound 10f could bind with topoisomerase IV–DNA complexes through hydrogen bonds and hydrophobic interactions. Quantum chemical studies were also performed on 10f to understand the structural features essential for activity. The preliminary mechanism research suggested that compound 10f could intercalate into calf thymus DNA to form a steady supramolecular complex which might block DNA replication to exert the powerful bioactivities.
Synthesis and Herbicidal Activity of 1,2,4-Triazole Derivatives Containing a Pyrazole Moiety
Mu, Jin-Xia,Zhai, Zhi-Wen,Tan, Cheng-Xia,Weng, Jian-Quan,Wu, Hong-Ke,Duke, Stephen O.,Zhang, Yong-Gang,Liu, Xing-Hai
, p. 968 - 971 (2019)
A series of triazole derivatives containing a pyrazole moiety were synthesized and characterized by 1H NMR, 13C NMR, and HRMS. The herbicidal activities of these compounds were tested against lettuce and bentgrass. Most of the tested compounds were moderately herbicidal activity against lettuce and bentgrass. Among them, compounds 6f and 6g had the highest herbicidal activity (80% inhibitory) against lettuce and bentgrass.
Lanthanide complexes based on ethyl 2-hydroxymethylidene-3-oxobutanoate
Kudyakova, Yulia S.,Bazhin, Denis N.,Burgart, Yanina V.,Saloutin, Victor I.
, p. 54 - 56 (2016)
The reaction of europium(iii) or terbium(iii) chlorides with ethyl 2-hydroxymethylidene-3-oxobutanoate in the presence of 2,2'-bipyridine (2,2'-bipy) resulted in the luminescent complexes [LnL3]·2,2'-bipy (L = ethyl 2-hydroxymethylidene-3-oxobutanoate, Ln = Tbiii or Euiii), whose molecular structure has been determined by X-ray analysis.
Preparation method of azabenzoazulene derivative
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Paragraph 0109-0115, (2021/06/13)
The invention belongs to the technical field of preparation of medicinal chemistry, and particularly relates to a preparation method of an azabenzoazulene derivative, ethyl acetoacetate and triethyl orthoformate are used as raw materials, and the azabenzoazulene derivative is prepared after a series of reactions. Compared with the existing synthetic method of the azabenzoazulene derivative, the method disclosed by the invention has the advantages that the raw materials are simple and easy to obtain, the synthetic route is simple and easy to implement, the yield is high, the operation is convenient, the cost is low, and the method can be easily applied to laboratory drug modification.
Optimization of the in Vivo Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood
Quancard, Jean,Simic, Oliver,Pissot Soldermann, Carole,Aichholz, Reiner,Blatter, Markus,Renatus, Martin,Erbel, Paulus,Melkko, Samu,Endres, Ralf,Sorge, Mickael,Kieffer, Laurence,Wagner, Trixie,Beltz, Karen,McSheehy, Paul,Wartmann, Markus,Régnier, Catherine H.,Calzascia, Thomas,Radimerski, Thomas,Bigaud, Marc,Weiss, Andreas,Bornancin, Frédéric,Schlapbach, Achim
, p. 14594 - 14608 (2020/12/23)
The paracaspase MALT1 has gained increasing interest as a target for the treatment of subsets of lymphomas as well as autoimmune diseases, and there is a need for suitable compounds to explore the therapeutic potential of this target. Here, we report the optimization of the in vivo potency of pyrazolopyrimidines, a class of highly selective allosteric MALT1 inhibitors. High doses of the initial lead compound led to tumor stasis in an activated B-cell-like (ABC) diffuse large B-cell lymphoma (DLBCL) xenograft model, but this compound suffered from a short in vivo half-life and suboptimal potency in whole blood. Guided by metabolism studies, we identified compounds with reduced metabolic clearance and increased in vivo half-life. In the second optimization step, masking one of the hydrogen-bond donors of the central urea moiety through an intramolecular interaction led to improved potency in whole blood. This was associated with improved in vivo potency in a mechanistic model of B cell activation. The optimized compound led to tumor regression in a CARD11 mutant ABC-DLBCL lymphoma xenograft model.
