2195-44-0Relevant academic research and scientific papers
Synthesis, anticancer, and computational studies of 1, 3, 4-oxadiazole-purine derivatives
Faisal, Shahla,Kamal, Shagufta,Parveen, Bushra,Rasool, Nasir,Rasul, Azhar,Raza, Zohaib,Shahzadi, Irum,Zahid, Faisal M.,Zahoor, Ameer F.,Zia-ur-Rehman, Muhammad
, p. 2782 - 2794 (2020)
Theophylline-7-acetic acid (acefylline) (3) and its derivatives are pharmacologically active compounds and generally recognized as bronchodilators for the treatment of respiratory diseases like acute asthma for over 70 years. In this article, synthesis of
Design, synthesis, in vitro antiproliferative evaluation and in silico studies of new VEGFR-2 inhibitors based on 4-piperazinylquinolin-2(1H)-one scaffold
Abdelhamid, Dalia,Abourehab, Mohammed A. S.,Abuo‐Rahma, Gamal El‐Din A.,Badr, Mohamed,Hassan, Abdelfattah,Hassan, Heba A.
, (2022/01/31)
Angiogenesis is essential in the growth of solid tumors which need oxygen and nutrients supply to grow in size. The VEGF/VEGFR-2 signaling pathway plays an important role in tumor angiogenesis. Sorafenib is an FDA approved cancer therapeutic with activity
Synthesis and Anti-Inflammatory Properties of Substituted 5-(Tetrahydro-4-phenyl-2H-pyran-4-yl)-4H-1,2,4-triazole-3-thiols
Arustamyan, Zh. S.,Margaryan,Aghekyan,Panosyan,Muradyan,Tumajyan
, p. 195 - 202 (2021/04/02)
Abstract: 5-(Tetrahydro-4-phenyl-2H-pyran-4-yl)-4H-1,2,4-triazole-3-thiol was synthesized by the reaction of 4-phenyltetrahydropyran-4-carbonyl chloride with thiosemicarbazide and subsequent cyclization of the resulting amide in the presence of KOH. The c
Nitrogen-containing ring derivative inhibitor as well as preparation method and application thereof
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Paragraph 0714-0720, (2021/05/12)
The invention relates to a nitrogen-containing ring derivative inhibitor as well as a preparation method and an application thereof. In particular, the present invention relates to a compound represented by general formula (I), a preparation method thereof, a pharmaceutical composition containing the compound, and uses of the compound as a P2X3 inhibitor in treatment of P2X3 receptor dysfunction diseases, especially in treatment of neurogenic diseases.
Pyrazoline tethered 1,2,3-triazoles: Synthesis, antimicrobial evaluation and in silico studies
Kumar, Anil,Kumar, Ashwani,Kumar, Lokesh,Lal, Kashmiri,Paul, Avijit Kumar
, (2021/08/03)
A new series of pyrazoline-amide linked 1,2,3-triazole hybrids was wisely designed and synthesized using 1,3-dipolar cycloaddition between pyrazoline linked alkynes and 2-bromo-N-arylacetamide. All the newly synthesized compounds were evaluated in vitro against different microbial strains viz. Escherichia coli, Bacillius subtilis, Staphylococcus aureus, Aspergillus niger, and Candida albicans. Pyrazoline linked terminal alkynes (4a–c) showed MIC = 0.062–0.078 μmol/mL against different bacterial and fungal strain. However, pyrazoline-amide linked 1,2,3-triazole hybrids (6a-6t) showed MIC = 0.0229–0.050 μmol/mL. Compound 6e exhibited better efficacy against E. coli and both the fungal strains compared to standard drugs used. Docking studies of the most potent compounds were carried out against bacterial DNA Gyr A and fungal 14α-steroldemethylase were also performed. The binding potential of 4a and 6e with both the target using molecular dynamics simulations was also investigated.
Synthesis and Cytotoxic Evaluation of Some New 1,2,3-Triazole Linked 2-Imino-4-(Trifuoromethyl)-Thiazolidin-4-ol Derivatives
Appalanaidu, K.,Dadmal, Tulshiram L.,Kumbhare, Ravindra M.,Pamanji, R.,Rao, J. Venkateswara,Reddy, Prathyusha J.,Velatooru, L. R.
, p. 81 - 89 (2021/08/12)
A new series of 1,2,3-triazole tagged 2-imino-4-(trifluoromethyl)thiazolidinol derivatives was synthesized through click chemistry under Sharpless conditions and evaluated for anticancer activity against human monocytic leukemia (U937), human breast adeno
Structure–activity relationship and biological evaluation of 12 N-substituted aloperine derivatives as PD-L1 down-regulatory agents through proteasome pathway
Zeng, Qing–Xuan,Wang, Kun,Zhang, Xin,Shi, Yu-Long,Dou, Yue–Ying,Guo, Zhi–Hao,Zhang, Xin–Tong,Zhang, Na,Deng, Hong–Bin,Li, Ying–Hong,Song, Dan–Qing
, (2021/10/22)
Twenty-nine 12 N-substituted aloperine derivatives were synthesized and screened for suppression on PD-L1 expression in H460 cells, as a continuation of our work. Systematic structural modifications led to the identification of compound 6b as the most act
Selective carbonic anhydrase inhibitor, synthesis method and application thereof
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Paragraph 0060; 0062, (2020/03/06)
The invention discloses a selective carbonic anhydrase inhibitor. The compound adopts acetazolamide as a lead compound, and is designed and synthesized by introducing a side chain for structural modification. The structure comprises a monosubstituted compound and a disubstituted compound; the selective inhibition effect of the compound on carbonic anhydrase is evaluated by esterase method; the neuroprotective effect of the compound is evaluated through a sodium nitroprusside oxidative stress model; and the toxicity of the compound is tested through cytotoxicity experiment. Research results show that in terms of the inhibition effect of the compound on carbonic anhydrase, monosubstitution is superior to disubstitution; the selectivity to carbonic anhydrase II is superior to that of carbonicanhydrase IX; the monosubstituted compound presents certain protective effect on sodium nitroprusside damaged PC12 cells; the IC50 of the optimal compound to carbonic anhydrase II is 16.7nM, the IC50to carbonic anhydrase IX is 4757nM, the selectivity is 285 times, which is remarkably superior to that of acetazolamide; the neuroprotective effect on PC12 is close to that of acetazolamide, and thetoxicity is lower than that of acetazolamide. The compound has the characteristics of good selectivity, effectiveness and safety, and is expected to be applied to drugs for preventing and treating neurological diseases.
5-[2-(N-(Substituted phenyl)acetamide)]amino-1,3,4-thiadiazole-2-sulfonamides as Selective Carbonic Anhydrase II Inhibitors with Neuroprotective Effects
Jiang, Caibao,Lao, Yaoqiang,Liao, Liping,Liu, Jiayong,Shi, Jinguo,Wang, Yang,Zhang, Jingxia,Zhang, Liantao
, (2020/03/24)
In this study, 22 novel compounds were designed and synthesized by acetamide bridge chains, among which 5 a–5 k were monosubstituted compounds, and 6 a–6 k were disubstituted. A series of biological evaluations was then carried out to determine the carbonic anhydrase inhibitory activity, neuroprotective effects and cytotoxicity of 5 a–5 k and 6 a–6 k. The results showed that some compounds could protect PC12 cells from sodium nitroprusside (SNP)-induced damage. In terms of the neuroprotection and inhibitory activity against carbonic anhydrase II, monosubstituted compounds were better than disubstituted. Compound 5 c exhibited better protective effect in PC12 cells than that of edaravone, and 5 c also showed less cytotoxicity. In addition, compound 5 c was found to be the most effective selective carbonic anhydrase II inhibitor (IC50=16.7 nM, CAI/CAII=54.3), which was similar to the inhibitory effect of acetazolamide. Moreover, the selectivity of compound 5 c was better than that of acetazolamide (IC50=12.0 nM, CAI/CAII=20.8). Molecular docking presented that the binding effect of compound 5 c with carbonic anhydrase II was superior to that of 5 c with carbonic anhydrase I and IX, which was consistent with the inhibitory results. Based on above findings, compound 5 c may be a potential candidate for selective carbonic anhydrase II inhibitor, and it had obviously neuroprotective effect and great advantages in drug safety.
Design, synthesis, antimicrobial evaluation and docking studies of urea-triazole-amide hybrids
Kumar, Anil,Kumar, Ashwani,Lal, Kashmiri,Poonia, Nisha,Rani, Poonam
, (2020/04/23)
A series of urea-1,2,3-triazole-amide hybrids was designed and synthesized via click reaction of urea derivatives containing a propargyl unit with 2-bromo-N-phenylacetamide derivatives and characterized by FTIR, NMR and HRMS data. The antimicrobial evalua
