1581726-07-9Relevant academic research and scientific papers
Synthesis of novel hetero ring fused pyridine derivatives; Their anticancer activity, CoMFA and CoMSIA studies
Santhosh Kumar,Poornachandra,Kumar Gunda, Shravan,Ratnakar Reddy,Mohmed, Jaheer,Shaik, Kamal,Ganesh Kumar,Narsaiah
, p. 2328 - 2337 (2018)
A series of novel furo[2,3-b]pyridine-2-carboxamide 4a–h/pyrido[3′,2′:4,5]furo[3,2-d] pyrimidin-4(3H)-one derivatives 5a–p were prepared from pyridin 2(1H) one 1 via selective O-alkylation with α-bromoethylester followed by cyclization, then reaction with
Novel 1,2,3-triazole-functionalized pyrido[3',2':4,5]furo[3,2-d]pyrimidin-4(3h)-one derivatives: Synthesis, anticancer activity, comfa and comsia studies
Vadla, Balakishan,Betala, Sailu
, p. 969 - 978 (2020/12/23)
A series of novel triazole functionalized pyrido [3',2':4,5] furo[3,2-d] pyrimidin-4 (3H)-one derivatives 7a-p were prepared from ethyl furo[2,3-b]pyridine-2-carboxylate 3 on reaction with am-monia to afford furo[2,3-b]pyridine-2-carboxamide 4. This compo
Synthesis of Novel Trifluoromethyl Group Containing Pyrido Furo/Thieno Pyrimidinone Derivatives and Their Anticancer Activity
Racha, Hanumandlu,Vadla, Balakishan,Peddolla, Kavitha,Betala, Sailu
, p. 1844 - 1849 (2019/05/21)
A series of novel trifluoromethyl group containing pyridofuro/thieno pyrimidinone derivatives 5a–p were prepared starting from 2-oxo/thioxo-6-phenyl/thien-2-yl-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile 1 compound on reaction with bromoethylac
Synthesis of Novel Alkyl Amide Functionalized Trifluoromethyl Substituted Furo/thieno Pyridine Derivatives: Their Anticancer Activity and CoMFA and CoMSIA Studies
Bhoomandla, Srinu,Gunda, Shravan Kumar,Kotoori, Srawanthi,Kanuparthy, Phani Raja
, (2019/06/27)
A series of novel alkyl amide functionalized trifluoromethyl substituted furo/thieno pyridine derivatives 4a–h, 5a–d, and 6a–h were prepared starting from 2-oxo/thioxo-6-phenyl/thien-2-yl-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile 1 on reactio
Synthesis of novel triazolothione, thiadiazole, triazole-functionalized furo/thieno[2,3-b]pyridine derivatives and their antimicrobial activity
Kumar, G. Santhosh,Poornachandra,Reddy, K. Ratnakar,Kumar, C. Ganesh,Narsaiah
, p. 1864 - 1873 (2017/10/06)
A series of novel triazolothione, thiadiazole, triazole-functionalized furo/thieno[2,3-b]pyridine derivatives 9a–l, respectively, were prepared starting from 2 (1H) pyridone 3 through selective O/S-alkylation followed by Thorpe–Ziegler cyclization to form furo/thieno[2,3-b]pyridine derivatives 6. Compounds 6 on reaction with hydrazine hydrate resulted carbohydrazide derivatives 7 and further reacted with diverse substituted phenyl isothiocyanates to form phenyl hydrazine carbothiamide derivatives 8. Each compound 8 is independently reacted in presence of NaOH, H2SO4, and N2H4.H2O to form triazolothione, thiadiazole, triazole-functionalized furo/thieno[2,3-b]pyridine derivatives 9a–l, respectively. All the products 9a–l were screened against Gram +ve, Gram –ve bacteria and fungal strains. Compounds 9c–h showed high activity against Bacillus subtilis microbial-type culture collection (MTCC) 121 at 8.0 micromolar concentration. Promising compounds further screened for minimum bactericidal concentration against B. subtilis MTCC 121 using ciprofloxacin as standard and found to show very good activity. These compounds also screened for biofilm inhibition activity against B. subtilis MTCC 121 using erythromycin as standard and confirmed the high activity.
Discovery and structure-activity relationships study of novel thieno[2,3-b]pyridine analogues as hepatitis C virus inhibitors
Wang, Ning-Yu,Zuo, Wei-Qiong,Xu, Ying,Gao, Chao,Zeng, Xiu-Xiu,Zhang, Li-Dan,You, Xin-Yu,Peng, Cui-Ting,Shen, Yang,Yang, Sheng-Yong,Wei, Yu-Quan,Yu, Luo-Ting
, p. 1581 - 1588 (2014/03/21)
Current treatment for hepatitis C is barely satisfactory, there is an urgent need to develop novel agents for combating hepatitis C virus infection. This study discovered a new class of thieno[2,3-b]pyridine derivatives as HCV inhibitors. First, a hit compound characterized by a thienopyridine core was identified in a cell-based screening of our privileged small molecule library. And then, structure activity relationship study of the hit compound led to the discovery of several potent compounds without obvious cytotoxicity in vitro (12c, EC50 = 3.3 μM, SI >30.3, 12b, EC50 = 3.5 μM, SI >28.6, 10l, EC50 = 3.9 μM, SI >25.6, 12o, EC 50 = 4.5 μM, SI >22.2, respectively). Although the mechanism of them had not been clearly elucidated, our preliminary optimization of this class of compounds had provided us a start point to develop new anti-HCV agents.
