72737-95-2Relevant academic research and scientific papers
Novel 1,3,4-oxadiazole linked benzopyrimidinones conjugates: Synthesis, DFT study and antimicrobial evaluation
Al-Ghamdi, Youssef O.,Almalki, Sami G.,Alqurashi, Yaser E.,Ben Jannet, Hichem,Chortani, Sarra,Edziri, Hayet,Manachou, Marwa,Romdhane, Anis
, (2020/05/13)
This work describes the synthesis, characterization and antimicrobial evaluation of a series of new 1,3,4-oxadiazole linked benzopyrimidinones. Their structures were confirmed on the basis of 1H, 13C NMR and ES-HRMS analysis. Their molecular geometry are also studied theoretically by the Density Functional Theory (DFT) method with B3LYP/6–31++G (d,p). All the calculations were done in DMSO, using conductor like polarizable continuum (CPCM). The target compounds were screened for their antimicrobial activity against four types of pathogenic bacteria and three fungal strains. Biological results revealed that some of these compounds demonstrated excellent to moderate antimicrobial activities with minimum inhibitory concentration (MIC) values ranging from 10.8 to 140.7 μM. Notably, compounds 5g and 5h showed the highest inhibitory activity against all bacterial strains with MIC values ranging from 111.3 to 10.8 μM against S. aureus, E. coli and P. aeruginosa, and displayed a good antifungal activity against C. albicans with MIC values of 10.8 and 27,8 μM, respectively. The structure-activity relationship (SAR) was discussed.
Synthesis, biological evaluation and molecular docking analysis of novel benzopyrimidinone derivatives as potential anti-tyrosinase agents
Chortani, Sarra,Nimbarte, Vijaykumar D.,Horchani, Mabrouk,Ben Jannet, Hichem,Romdhane, Anis
, (2019/09/19)
2-substitued-benzopyrimidinones 2 were synthesized in high to excellent yields in a single step via condensation of 2-aminobenzamide 1 with some aryl-aldehydes in the presence of iodine. Cyclocondensation reaction of hydrazides 3 which were obtained in two steps from benzopyrimidinones 2, with some electrophilic species such as 2,4-pentandione, 2,5-hexandione, 1-phenylbutan-1,3-dione and cyclic anyhdrides provided the new compounds 4a–c, 5a–c, 6a–c, 7a–c, 8a–c and 9a–c. The synthesized compounds were characterized by spectroscopic means. They were also evaluated for their anti-tyrosinase potential. The structure-activity relationship (SAR) was discussed on the basis of the molecular docking analysis.
Heterocyclic synthesis: A convenient route to some 2-mercepto 1,3,4-oxadiazole and green chemistry microwave-induced one-pot synthesis of 2-aryl 1,3,4-oxadiazole in quinazolone and their antibacterial and antifungal activity
Desai,Desai
, p. 995 - 999 (2007/10/03)
Several 6-substituted-3-[(5-mercepto-1,3,4-oxadiazol-2-yl)methyl]-2- substituted quinazolin-4(3H)-one or 6-substituted-3-[4-(5-mercepto-1,3,4- oxadiazol-2-yl)phenyl]-2-substituedquinazolin-4(3H)-one 2(a-l) and 6-substituted-3-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl]-2-substitutedquinazolin- 4(3H)-one or 6-substituted-3-[4-(5-phenyl-1,3,4-oxadiazol-2-yl) phenyl]-2-substitutedquinazolin-4(3H)-one 3(a-l) were synthesized using conventional and microwave techniques respectively and were screened for antibacterial and antifungal activity.
Synthesis and antimicrobial activity of some pyrazoline derivatives of 4(3H)-quinazolinones
Panda,Srinivas,Rao, M.E. Bhanoji,Panda
, p. 770 - 771 (2007/10/03)
The present communication describes the synthesis and antimicrobial activity of some new 6,8-disubstituted-2-(phenyl/methyl)-3-|4-(3-methyl-5-pyrazolinon-1-yl)carbonyl) phenyl/benzyl/methyl|-4(3H)-qainazolinones.
