199682-73-0Relevant articles and documents
Design and synthesis of amino acid derivatives of substituted benzimidazoles and pyrazoles as Sirt1 inhibitors
Asthana, Shailendra,Banerjee, Sanjay K.,Kumar, Vasantha,Paramesha, Bugga,Poojary, Boja,Purushotham, Nikil,Singh, Mrityunjay,Wakode, Sharad
, p. 3809 - 3827 (2022/02/16)
Owing to its presence in several biological processes, Sirt1 acts as a potential therapeutic target for many diseases. Here, we report the structure-based designing and synthesis of two distinct series of novel Sirt1 inhibitors, benzimidazole mono-peptide
Synthesis and evaluation of antimicrobial and anticancer activities of 3-phenyl-1-phenylsulfonyl pyrazoles containing an aminoguanidine moiety
Huang, Yushan,Hu, Hongmei,Yan, Rui,Lin, Liwen,Song, Mingxia,Yao, Xiaodong
, (2020/10/15)
A series of 3-phenyl-1-phenylsulfonyl pyrazoles containing an aminoguanidine moiety was designed, synthesized, and evaluated for their antimicrobial and anticancer activities. The majority of the target compounds showed broad-spectrum antimicrobial activi
Synthesis and biological evaluation of some pyrazole derivatives, containing (Thio) semicarbazide, as dual anti-inflammatory antimicrobial agents
Liang, Zhaochang,Huang, Yuping,Wang, Shiben,Deng, Xianqing
, p. 1020 - 1030 (2019/10/28)
Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1
Synthesis and antimicrobial evaluation of (Z)-5-((3-phenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one derivatives
Wei, Zhi-Yu,Liu, Jia-Chun,Zhang, Wen,Li, Ya-Ru,Li, Chao,Zheng, Chang-Ji,Piao, Hu-Ri
, p. 751 - 759 (2016/11/29)
Background: An alarming increment in pathogenic resistance to existing anti-microbial agents is a serious problem and the treatment of these bacterial infections is becoming increasingly challenging. Therefore, there is an urgent need to develop novel ant
Synthesis and antitubercular and antibacterial activity of some active fluorine containing quinoline–pyrazole hybrid derivatives
Nayak, Nagabhushana,Ramprasad, Jurupula,Dalimba, Udayakumar
, p. 59 - 68 (2017/11/28)
In an attempt to develop newer antitubercular and antibacterial agents against the increasing bacterial resistance, we have designed new quinoline–pyrazole analogs (8a–u) following the molecular hybridization approach. The structure of one of the final compounds, 8a was unambiguously confirmed by single crystal X-ray diffraction (SC-XRD) analysis. The target compounds were evaluated for their antitubercular activity against Mycobacterium tuberculosis and antibacterial activity against three common pathogenic bacterial strains. Four derivatives (8b, 8c, 8j and 8o) displayed significant antitubercular activity. The compounds derived from 8-trifluoromethylquinoline and 6-fluoroquinoline scaffolds with halogen substitution on the pyrazole ring exhibited superior inhibition activity than corresponding 6-methoxyquinoline analogs. The cytotoxic studies revealed that the active compounds are nontoxic to normal Vero cell lines with selectivity index values ≥10, which indicate the suitability of these compounds for further drug development. The in silico molecular docking study demonstrated strong binding affinity of the compounds with the target enzymes (InhA, CYP121 and TMPK) of M. tuberculosis. Further, the in vitro antibacterial activity of compounds 8b, 8c, 8d and 8g is comparable with that of the reference drug, Ciprofloxacin.
Hantzsch reaction: Synthesis and characterization of some new 1,4-dihydropyridine derivatives as potent antimicrobial and antioxidant agents
Vijesh,Isloor, Arun M.,Peethambar,Shivananda,Arulmoli,Isloor, Nishitha A.
experimental part, p. 5591 - 5597 (2011/12/22)
In the present study two new series of Hantzsch 1,4-dihydropyridine derivatives (1,4-DHPs) containing substituted pyrazole moiety (4a-f and 5a-f) were synthesized by the reaction of 3-aryl-1H-pyrazole-4-carbaldehydes with 1,3-dicarbonylcompounds (ethylace
Structure-activity relationship study of a novel necroptosis inhibitor, necrostatin-7
Zheng, Weihong,Degterev, Alexei,Hsu, Emily,Yuan, Junying,Yuan, Chengye
scheme or table, p. 4932 - 4935 (2009/05/26)
Necroptosis is a regulated caspase-independent cell death mechanism characterized by morphological features resembling non-regulated necrosis. Necrotatin-7 (Nec-7), a novel potent small-molecule inhibitor of necroptosis, is structurally distinct from previously described necrostatins (Nec-1, Nec-3, Nec-4 and Nec-5). Here, we describe a series of structural modifications and the structure-activity relationship (SAR) of the Nec-7 series for inhibiting necroptosis.
Synthesis of 3-substituted arylpyrazole-4-carboxylic acids
Lebedev,Lebedeva,Sheludyakov,Kovaleva,Ustinova,Kozhevnikov
, p. 782 - 789 (2007/10/03)
A method was suggested for preparing previously unknown 3-aryl-substituted pyrazole-4-carboxylic acids, involving Vilsmeier formylation of semicarbazones of 26 available mono- and disubstituted acetophenones and 2-acetylthiophene followed by oxidation of
A new synthethic approach to indazole synthesis
Baraldi, Pier Giovanni,Cacciari, Barbara,Spalluto, Giampiero,Romagnoli, Romeo,Braccioli, Giovanni,Zaid, Abdel Naser,De Pineda Las Infantas, Maria J.
, p. 1140 - 1142 (2007/10/03)
Stobbe condensation of 3-alkyl- or aryl-4-formylpyrazoles 3a-f with diethyl succinate in the presence of potassium f-butoxide, followed by intramolecular ring closure (Ac2O-NaOAc), afforded the corresponding indazole derivatives 5a-f in 65-85% overall yield. These compounds are good starting materials for transformation to biologically active molecules, such as new pyrazole analogs of the left-hand segment of the potent natural antineoplastic agent CC-1065.