scholarly journals Design, synthesis and SAR study of 2-aminopyridine derivatives as potent and selective JAK2 inhibitors

2022 ◽  
Author(s):  
Dandan Liu ◽  
Huan Ge ◽  
Fangling Xu ◽  
Yufang Xu ◽  
Wenjun Liu ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Sar Study ◽  
Jak2 Inhibitors

scholarly journals Novel Acetohydrazide Pyrazole Derivatives: Design, Synthesis, Characterization and Antimicrobial Activity

2019 ◽  
Vol 31 (12) ◽  
pp. 2740-2744
Author(s):  
Anil Verma ◽  
Vinod Kumar ◽  
Ramesh Kataria ◽  
Joginder Singh
Keyword(s):  
Mass Spectrometry ◽  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Pyrazole Derivatives ◽  
Reaction Conditions ◽  
Design Synthesis ◽  
Structure Activity ◽  
Electron Withdrawing Group ◽  
Sar Study

Eleven acetohydrazide linked pyrazole derivatives were designed and synthesized via condensation of acetohyadrazide with different substituted formyl pyrazole derivatives under mild reaction conditions. Synthesized compounds were characterized on the basis of IR, NMR (1H & 13C) and mass spectrometry. The antimicrobial activities of all the compounds were screened against four bacterial and two fungal strains. Among the synthesized compounds, three compounds viz. 6b, 6c and 6d were found as efficient antimicrobial agents in reference to the standard drugs viz. ciprofloxacin and amphotericin-B. Further, structure-activity relationship (SAR) study revealed that electron-withdrawing group enhances the antimicrobial potential of synthesized derivatives as compared to other groups present in the ring. Hence, among compounds 6b-c, compound 6d could be explored further against other microbes to prove its vitality.

scholarly journals Design, Synthesis and SAR Study of Novel Trisubstituted Pyrimidine Amide Derivatives as CCR4 Antagonists

Molecules ◽  
2014 ◽  
Vol 19 (3) ◽  
pp. 3539-3551 ◽  
Author(s):  
Libao Xu ◽  
Yang Zhang ◽  
Wenjie Dai ◽  
Ying Wang ◽  
Dan Jiang ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Amide Derivatives ◽  
Sar Study

Design, Synthesis and biological evaluation of diazeno-thiazole derivatives as ribonucleotide reductase inhibitors

2017 ◽  
Vol 4 (2) ◽  
pp. 20-24 ◽  
Author(s):  
Mohd Usman Mohd Siddique ◽  
Surender Singh Jadav ◽  
Geraldine Graser ◽  
Philipp Saiko ◽  
Thomas Szekeres ◽  
...  
Keyword(s):  
Dna Synthesis ◽  
Ribonucleotide Reductase ◽  
Biological Evaluation ◽  
Thiazole Derivatives ◽  
Design Synthesis ◽  
Reductase Inhibitors ◽  
Good Target ◽  
Cell Synthesis ◽  
Ribonucleotide Reductase Inhibitors ◽  
Sar Study

Ribonucleotide reductase(RNR) is a metalloenzyme that catalyses the rate limiting step in DNA synthesis and repair. It causes the reduction of ribonucleotide to 2’-deoxyribonuclotides which are used as precursors for DNA synthesis, thus offering a good target for inhibition of cell synthesis. Experimental results have been proven that RNR inhibitors can be used as antiviral, anticancer or antibacterial agents. Here we report the synthesis of a novel class of diazeno-thiazole derivatives as potent RNR inhibitors. A series of forty molecules were synthesized and evaluated for their RNR inhibitory properties. All compounds were found to be good inhibitors of the RNR. Compound 3iwas found to be most active showing an IC50 value of 0.8 µm. The established SAR study indicated the presence of a polar bridge with an adjacent flexible aromatic ringprerequisite for RNR inhibitory activity. Moreover, compounds having an additional 4-chloro phenyl ring were found to be most potent.

Design, synthesis and SAR study of hydroxychalcone inhibitors of human β-secretase (BACE1)

2011 ◽  
Vol 26 (5) ◽  
pp. 643-648 ◽  
Author(s):  
Lei Ma ◽  
Zhengyi Yang ◽  
Chenjing Li ◽  
Zhiyuan Zhu ◽  
Xu Shen ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Sar Study

Design, Synthesis and SAR Study of Novel Spiro [Pyrimido[5,4-b]Quinoline-10,5′-Pyrrolo[2,3-d]Pyrimidine] Derivatives as Promising Anticancer Agents

2018 ◽  
Vol 55 (10) ◽  
pp. 2297-2302 ◽  
Author(s):  
Asha V. Chate ◽  
Sagar P. Kamdi ◽  
Amruta N. Bhagat ◽  
Chetan K. Jadhav ◽  
Amol Nipte ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Pyrimidine Derivatives ◽  
Design Synthesis ◽  
Sar Study

scholarly journals Bi-aryl Analogues of Salicylic Acids: Design, Synthesis and SAR Study to Ameliorate Endoplasmic Reticulum Stress

2021 ◽  
Vol Volume 15 ◽  
pp. 3593-3604
Author(s):  
Ye Eun Kim ◽  
Dong Hwan Kim ◽  
Ami Choi ◽  
Seoul Jang ◽  
Kwiwan Jeong ◽  
...  
Keyword(s):  
Endoplasmic Reticulum ◽  
Endoplasmic Reticulum Stress ◽  
Design Synthesis ◽  
Sar Study ◽  
Salicylic Acids

Design, Synthesis, SAR Study, Antimicrobial and Anticancer Evaluation of Novel 2-Mercaptobenzimidazole Azomethine Derivatives

2020 ◽  
Vol 20 (15) ◽  
pp. 1559-1571 ◽  
Author(s):  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Siong Meng Lim ◽  
Kalavathy Ramasamy ◽  
Vasudevan Mani ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Benzimidazole Derivatives ◽  
Dilution Method ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range ◽  
Sar Study

Background: Various analogues of benzimidazole are found to be biologically and therapeutically potent against several ailments. Benzimidazole when attached with heterocyclic rings has shown wide range of potential activities. So, from the above provided facts, we altered benzimidazole derivatives so that more potent antagonists could be developed. In the search for a new category of antimicrobial and anticancer agents, novel azomethine of 2-mercaptobenzimidazole derived from 3-(2- (1H-benzo[d]imidazol-2-ylthio)acetamido)benzohydrazide were synthesized. Results and Discussion: The synthesized analogues were characterized by FT-IR, 1H/13C-NMR and MS studies as well C, H, N analysis. All synthesized compounds were evaluated for in vitro antibacterial activity against Gram-positive (B. subtilis), Gram-negative (E. coli, P. aeruginosa, K. pneumoniae and S. typhi) strains and in vitro antifungal activity against C. albicans and A. niger strains by serial dilution method, the minimum inhibitory concentration (MIC) described in μM/ml. The in vitro anticancer activity of synthesized compounds was determined against human colorectal carcinoma cell line (HCT- 116) using 5-fluorouracil as standard drug. Conclusion: In general, most of the synthesized derivatives exhibited significant antimicrobial and anticancer activities. Compounds 8, 10, 15, 16, 17, 20 and 22 showed significant antimicrobial activity towards tested bacterial and fungal strains and compound 26 exhibited significant anticancer activity.

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