33621-61-3Relevant articles and documents
In Silico Study and In Vitro Evaluation of Novel Synthesized Quinolone Derivatives Having Five-Membered Heterocyclic Moieties
Naser, Noor H.,Raauf, Ayad M. R.,Sheehan, Mustafa R.
, p. 215 - 225 (2022/02/14)
Infectious diseases are caused by pathogens, such as viruses, bacteria, fungi, and parasites. Quinolones work by inhibition of bacterial topoisomerase IV and/or gyrase, a group of oxadiazole derivatives were incorporated into C7 piperazine ring of Gatiflo
Synthesis, in vitro α-glucosidase inhibitory potential and molecular docking studies of 2-amino-1,3,4-oxadiazole derivatives
Ullah, Hayat,Rahim, Fazal,Taha, Muhammad,Hussain, Raffaqat,Wadood, Abdul,Nawaz, Mohsan,Wahab, Zainul,Kanwal,Khan, Khalid M.
, p. 724 - 734 (2020/08/19)
Background: In the recent past, we have synthesized and reported different derivatives of oxadiazoles as potential α-glucosidase inhibitors, keeping in mind, the pharmacological aspects of oxadiazole moiety and in continuation of our ongoing research on the chemistry and bioactivity of new heterocyclic compounds. Methods: 1,3,4-Oxadiazole derivatives (1-14) have been synthesized and characterized by different spectroscopic techniques such as1 H-,13 C-NMR and HREI-MS. Results: The synthetic derivatives were screened for α-glucosidase inhibitory potential. All compounds exhibited good inhibitory activity with IC50 values ranging between 0.80 ± 0.1 to 45.1 ± 1.7 μM in comparison with the standard acarbose having IC50 value 38.45 ± 0.80 μM. Conclusion: Thirteen compounds 1-6 and 8-14 showed potential inhibitory activity as compared to the standard acarbose having IC50 value 38.45 ± 0.80 μM, however, only one compound 7 (IC50 = 45.1 ± 1.7 μM) was found to be less active. Compound 14 (IC50 = 0.80 ± 0.1 μM) showed promising inhibitory activity among all synthetic derivatives. Molecular docking studies were also conducted for the active compounds to understand the ligand-enzyme binding interactions.
Synthesis of indole-tethered [1,3,4]thiadiazolo and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids as anti-pancreatic cancer agents
Gummidi, Lalitha,Kerru, Nagaraju,Awolade, Paul,Raza, Asif,Sharma, Arun K.,Singh, Parvesh
, (2020/09/18)
New indole-tethered [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one (8a-j) and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids (9a-e) were synthesized using [4+2] cycloaddition reactions of functionalized 1,3-diazabuta-1,3-dienes with indole-ketenes. All molecul