425634-97-5Relevant articles and documents
Synthesis, anticancer evaluation and molecular docking studies of new benzimidazole- 1,3,4-oxadiazole derivatives as human topoisomerase types I poison
Acar ?evik, Ulviye,Atl? Eklio?lu, ?zlem,Atl?d, ?zlem,Kaplanc?kl?, Zafer As?m,Karaduman, Abdullah Burak,Kaya ?avu?o?lu, Betül,Levent, Serkan,Osmaniye, Derya,Sa?l?k, Begüm Nurpelin
, p. 1657 - 1673 (2020/08/21)
In this study, some benzimidazole-oxadiazole derivatives were synthesised and tested for their in vitro anticancer activities on five cancer cell lines, including HeLa, MCF7, A549, HepG2 and C6. Their structures were elucidated by IR, 1H-NMR,
Betulinic acid derivatives: a new class of α-glucosidase inhibitors and LPS-stimulated nitric oxide production inhibition on mouse macrophage RAW 264.7 cells
Gundoju, Narayanarao,Bokam, Ramesh,Yalavarthi, Nageswara Rao,Azad, Rajaram,Ponnapalli, Mangala Gowri
, p. 2618 - 2622 (2018/04/30)
Chemical manipulation studies were conducted on betulinic acid (1), twenty-one new rationally designed analogues of 1 with modifications at C-28 were synthesized for their evaluation of inhibitory effects on α-glucosidase and LPS-stimulated nitric oxide production in mouse macrophage RAW 264.7 cells. Compound 2 (IC50 = 5.4 μM) exhibited an almost 1.4-fold increase in α-glucosidase inhibitory activity on yeast α-glucosidase while analogues 5 (IC50 16.4 μM) and 11 (IC50 16.6 μM) exhibited a 2-fold enhanced inhibitory activity on NO-production than betulinic acid.
Design, synthesis and biological profiling of aryl piperazine based scaffolds for the management of androgen sensitive prostatic disorders
Gupta, Sonal,Pandey, Deepti,Mandalapu, Dhanaraju,Bala, Veenu,Sharma, Vikas,Shukla, Mahendra,Yadav, Santosh K.,Singh, Nidhi,Jaiswal, Swati,Maikhuri, Jagdamba P.,Lal, Jawahar,Siddiqi, Mohammad I.,Gupta, Gopal,Sharma, Vishnu L.
supporting information, p. 2111 - 2121 (2016/11/18)
In the quest for novel scaffolds for the management of androgen sensitive prostatic disorders like prostate cancer and benign prostatic hyperplasia, a series of twenty-six aryl/heteroaryl piperazine derivatives have been described. Three compounds, 8a, 8c
3-Nitrotriazole-based piperazides as potent antitrypanosomal agents
Papadopoulou, Maria V.,Bloomer, William D.,Rosenzweig, Howard S.,O'Shea, Ivan P.,Wilkinson, Shane R.,Kaiser, Marcel
supporting information, p. 325 - 334 (2015/09/22)
Novel linear 3-nitro-1H-1,2,4-triazole-based piperazides were synthesized and evaluated as antitrypanosomal agents. In addition, some bisarylpiperazine-ethanones which were formed as by-products were also screened for antiparasitic activity. Most 3-nitrotriazole-based derivatives were potent and selective against Trypanosoma cruzi parasites, but only one displayed these desired properties against Trypanosoma brucei rhodesiense. Moreover, two 3-nitrotriazole-based chlorophenylpiperazides were moderately and selectively active against Leishmania donovani. Although the bisarylpiperazineethanones were active or moderately active against T. cruzi, none of them demonstrated an acceptable selectivity. In general, 3-nitrotriazole-based piperazides were less toxic to host L6 cells than the previously evaluated 3-nitrotriazole-based piperazines and seven of 13 were 1.54-to 31.2-fold more potent antichagasic agents than the reference drug benznidazole. Selected compounds showed good ADMET characteristics. One potent in vitro antichagasic compound (3) was tested in an acute murine model and demonstrated antichagasic activity after a 10-day treatment of 15 mg/kg/day. However, neither compound 3 nor benznidazole showed a statistically significant P value compared to control due to high variability in parasite burden among the untreated animals. Working as prodrugs, 3-nitrotriazole-based piperazides were excellent substrates of trypanosomal type I nitroreductases and constitute a novel class of potentially effective and more affordable antitrypanosomal agents.
Synthesis of new piroxicam derivatives and their influence on lipid bilayers
Szczesniak-siga, Berenika,Maniewska, Jadwiga,Pola, Andrzej,rodapomianek, Kamila,Malinka, Wieslaw,Michalak, Krystyna
, p. 1045 - 1050 (2015/02/02)
A novel series of potentially biologically active 1,2-benzothiazine 1,1-dioxides analogs of piroxicam (a recognized non-steroidal anti-inflammatory drug) were synthesized from commercially available saccharin. All of the synthesized compounds were subjected to preliminary evaluation for their ability to interact with lipid bilayers. The influence of the new derivatives of piroxicam on liposomes made of EYPC was investigated by fluorescence spectroscopy with two fluorescent probes Laurdan and Prodan. All the studied compounds showed an interaction with model membranes.
Synthesis and evaluation of thiouracil derivatives as dipeptidyl peptidase iv inhibitors
Sharma, Mani,Singh, Divya,Gupta, Monica
, p. 257 - 264 (2013/03/14)
A series of thiouracil derivatives were designed, synthesized and screened for in vitro inhibition of dipeptidyl peptidase IV. The SAR study indicated the influence of substituted chemical modifications on thiouracil scaffold. Compounds 8 (IC50
Synthesis, evaluation and molecular docking of prolyl-fluoropyrrolidine derivatives as dipeptidyl peptidase IV inhibitors
Sharma, Mani,Gupta, Monica,Singh, Divya,Kumar, Manoj,Kaur, Punit
, p. 156 - 166 (2013/08/23)
A series of prolyl-fluoropyrrolidine derivatives were designed, synthesized and screened for in vitro inhibition of dipeptidyl peptidase IV. The SAR study revealed the influence of substituted chemical modifications on dipeptidyl peptidase IV inhibitory activity. Among all the compounds screened, compound 9 (IC50 = 0.83 μm) and 10 (IC50 = 0.43 μm) possessing aryl substituted piperazine with acetamide linker resulted as most potent dipeptidyl peptidase IV inhibitors. Both the compounds 9 and 10 resulted significant reduction in glucose excursion during oral glucose tolerance test in streptozotocin-induced diabetic rat model at single dose of 10 mg/kg. Molecular docking studies were performed to illustrate the probable binding mode and interactions of prolyl-fluoropyrrolidine nucleus and its derivatives at binding site of receptor. The fluoropyrrolidine moiety of prolyl-fluoropyrrolidine derivatives occupied S1 pocket as observed in the crystal structure (PDB id: 2FJP). The compounds 9 and 10 were observed to occupy S2 binding pocket and were observed to have interaction with Arg125, Tyr547 and Ser630 acquired through hydrogen bond. The aryl moiety at piperazine ring was found to extend into the cavity and interacted with Arg358. The observed interactions signalled that occupancy of the highly hydrophobic S2 pocket is very crucial for dipeptidyl peptidase IV inhibitory activity. A series of prolyl-fluoropyrrolidine derivatives were synthesized and evaluated for inhibition of dipeptidyl peptidase IV (DPP IV) for treatment of Type 2 diabetes. The binding position of docked compounds (stick rendering) in the binding pocket of DPP IV.
Synthesis, Evaluation and Molecular Docking of Thiazolopyrimidine Derivatives as Dipeptidyl Peptidase IV Inhibitors
Sharma, Mani,Gupta, Monica,Singh, Divya,Kumar, Manoj,Kaur, Punit
, p. 918 - 928,11 (2012/12/12)
A series of thiazolopyrimidine derivatives was designed, synthesized and screened for in-vitro inhibition of Dipeptidyl Peptidase IV (DPP IV). The SAR study indicated the influence of substituted chemical modifications on thiazolopyrimidine scaffold. Comp
Synthesis, Evaluation and Molecular Docking of Thiazolopyrimidine Derivatives as Dipeptidyl Peptidase IV Inhibitors
Sharma, Mani,Gupta, Monica,Singh, Divya,Kumar, Manoj,Kaur, Punit
, p. 918 - 928 (2013/01/15)
A series of thiazolopyrimidine derivatives was designed, synthesized and screened for in-vitro inhibition of Dipeptidyl Peptidase IV (DPP IV). The SAR study indicated the influence of substituted chemical modifications on thiazolopyrimidine scaffold. Comp
FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
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Page/Page column 84, (2012/12/13)
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given
