Synthesis and biological evaluation of some newer Indole Derivatives

2021 ◽  
pp. 6066-6072
Author(s):  
Himanshu Bhardwaj ◽  
Gyanendra Kumar Sharma ◽  
Nitin Mittal ◽  
Harsh Bhardwaj
Keyword(s):  
Inhibitory Action ◽  
Biological Evaluation ◽  
Indole Derivatives ◽  
Wide Scope ◽  
Parasitic Species ◽  
Dla Cells ◽  
Synthesis And Biological Evaluation

The indole skeleton is one of the most appealing structures with a wide scope of natural and pharmacological exercises, for example, antibacterial, antifungal, anticancer. A progression of new N-Substituted benzyidene 2- (1H-indol-2-yl)benzenamine subordinates (3a-3k) were combined by the response of 2-(o-aminophenyl)indole and fragrant aldehyde within the sight of ethanol with scarcely any drops of acidic corrosive. The response blend was observed by TLC and recrystallized from wanted dissolvable. The structures of these mixes have been affirmed by FTIR, 1HNMR, mass ghastly information, natural investigation. All the combined mixes were assessed for antibacterial, antifungal and anticancer activity.the results uncovered that 3g, 3h and 3k display progressively powerful movement against on the two microbes and parasitic species and compound 3h indicated promising inhibitory action against DLA cells which is cancer-causing.

Synthesis and biological evaluation of N-glucosyl indole derivatives as sodium-dependent glucose co-transporter 2 inhibitors

2019 ◽  
Vol 83 ◽  
pp. 520-525 ◽  
Author(s):  
Kuang-Feng Chu ◽  
Jen-Shin Song ◽  
Chiung-Tong Chen ◽  
Teng-Kuang Yeh ◽  
Tsung-Chih Hsieh ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Indole Derivatives ◽  
Sodium Dependent ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of new dihydroindolizino[8,7-b]indole derivatives as novel α-glucosidase inhibitors

2021 ◽  
Vol 1224 ◽  
pp. 129290
Author(s):  
Fariba Peytam ◽  
Mehdi Adib ◽  
Reihaneh Shourgeshty ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Mehdi Jahani ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Indole Derivatives ◽  
Glucosidase Inhibitors ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl) indole derivatives: Multi-target compounds with dual antimicrobial and anti-inflammatory activities

2020 ◽  
Author(s):  
Ahmed Shaker ◽  
Eman K. A. Abdelall ◽  
Khaled R. A. Abdellatif ◽  
Hamdy M. Abdel-Rahman
Keyword(s):  
Active Site ◽  
High Selectivity ◽  
Biological Evaluation ◽  
Indole Derivatives ◽  
E Coli ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Synthesis And Biological Evaluation

Abstract Three series of 2-(4-methylsulfonylphenyl) indole derivatives have been designed and synthesized. The synthesized compounds were evaluated for their antimicrobial, COX inhibitory and anti-inflammatory activities. Compound 7g was identified to be the most potent antibacterial candidate against strains of MRSA , E. coli, K. pneumoniae, P. aeruginosa, and A. baumannii , respectively with safe therapeutic dose. Compounds 7a-k, 8a-c and 9a-c showed good anti-inflammatory activity with high selectivity toward COX-2 in comparison with reference drugs indomethacin and celecoxib. Compounds 9a-c were found to release moderate amounts of NO to decrease the side effects associated with selective COX-2 inhibitors. A molecular modeling study for compounds 7b, 7h, and 7i into COX-2 active site correlated with results of in vitro COX-2 inhibition assays.

scholarly journals Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl) indole derivatives: Multi-target compounds with dual antimicrobial and anti-inflammatory activities

2019 ◽  
Author(s):  
Ahmed Shaker ◽  
Eman K. A. Abdelall ◽  
Khaled R. A. Abdellatif ◽  
Hamdy M. Abdel-Rahman
Keyword(s):  
Active Site ◽  
High Selectivity ◽  
Biological Evaluation ◽  
Indole Derivatives ◽  
E Coli ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Synthesis And Biological Evaluation

Abstract Three series of 2-(4-methylsulfonylphenyl) indole derivatives have been designed and synthesized. The synthesized compounds were evaluated for their antimicrobial, COX inhibitory and anti-inflammatory activities. Compound 7g was identified to be the most potent antibacterial candidate against strains of MRSA , E. coli, K. pneumoniae, P. aeruginosa, and A. baumannii , respectively with safe therapeutic dose. Compounds 7a-k, 8a-c and 9a-c showed good anti-inflammatory activity with high selectivity toward COX-2 in comparison with reference drugs indomethacin and celecoxib. Compounds 9a-c were found to release moderate amounts of NO to decrease the side effects associated with selective COX-2 inhibitors. A molecular modeling study for compounds 7b, 7h, and 7i into COX-2 active site correlated with results of in vitro COX-2 inhibition assays.

scholarly journals QSAR Model of Indeno[1,2-b]indole Derivatives and Identification of N-isopentyl-2-methyl-4,9-dioxo-4,9-Dihydronaphtho[2,3-b]furan-3-carboxamide as a Potent CK2 Inhibitor

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 97 ◽  
Author(s):  
Samer Haidar ◽  
Christelle Marminon ◽  
Dagmar Aichele ◽  
Abdelhamid Nacereddine ◽  
Wael Zeinyeh ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Qsar Model ◽  
Biological Evaluation ◽  
Indole Derivatives ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Synthesis And Biological Evaluation ◽  
Ck2 Inhibitors ◽  
Ck2 Inhibitor

Casein kinase II (CK2) is an intensively studied enzyme, involved in different diseases, cancer in particular. Different scaffolds were used to develop inhibitors of this enzyme. Here, we report on the synthesis and biological evaluation of twenty phenolic, ketonic, and para-quinonic indeno[1,2-b]indole derivatives as CK2 inhibitors. The most active compounds were 5-isopropyl-1-methyl-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione 4h and 1,3-dibromo-5-isopropyl-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione 4w with identical IC50 values of 0.11 µM. Furthermore, the development of a QSAR model based on the structure of indeno[1,2-b]indoles was performed. This model was used to predict the activity of 25 compounds with naphtho[2,3-b]furan-4,9-dione derivatives, which were previously predicted as CK2 inhibitors via a molecular modeling approach. The activities of four naphtho[2,3-b]furan-4,9-dione derivatives were determined in vitro and one of them (N-isopentyl-2-methyl-4,9-dioxo-4,9-dihydronaphtho[2,3-b]furan-3-carboxamide) turned out to inhibit CK2 with an IC50 value of 2.33 µM. All four candidates were able to reduce the cell viability by more than 60% after 24 h of incubation using 10 µM.

Synthesis and Biological evaluation of some newer Pyrazole Derivatives

2021 ◽  
pp. 6304-6308
Author(s):  
Ajay Sharma ◽  
Gyanendra Kumar Sharma ◽  
Himansu Chopra
Keyword(s):  
Biological Evaluation ◽  
Pyrazole Derivatives ◽  
Wide Scope ◽  
Phenyl Hydrazine ◽  
Carbon Particles ◽  
Ongoing Work ◽  
Definition Of ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation ◽  
Heterocyclic Moiety

Pyrazoline is a 5-membered heterocyclic moiety has two adjoining nitrogen iotas and three carbon particles inside the ring. Pyrazoline subordinate are related wide scope of pharmacological and restorative exercises, for example, antibacterial, antifungal, pain relieving, calming, hostile to parasitic, against malarial, against oxidant. The ongoing work of exploration is fundamentally engaged at the revelation and improvement of a progression of 1,3,5-trisubstituted pyrazoline. A progression of new 1-phenyl-3-(4-nitrophenyl)- 5-(subbed phenyl) pyrazoline subordinates (2a-2j) were blended by the response of subbed acetophenone and subbed benzaldehyde within the sight of fluid sodium hydroxide arrangement by Claisen Schmidt buildup system. The subbed chalcone were integrated which is additionally dense with phenyl hydrazine in ethanol and results in the definition of conclusive subordinates of pyrazoline (2a-2j). The response blend was observed by TLC and the last mixes were refined by recrystallization from wanted dissolvable. All the structures of blended mixes were affirmed by FTIR, 1H NMR, mass unearthly information and essential investigation. All the recently combined mixes (2a-2j) were assessed for antibacterial and antifungal movement. Mixes 2f, 2i and 2h showed powerful inhibitory impact against on strains of both bacterial and parasitic species.

ChemInform Abstract: A Novel Class of Inhibitors for Human Steroid 5α-Reductase: Synthesis and Biological Evaluation of Indole Derivatives. Part 2.

ChemInform ◽  
2010 ◽  
Vol 31 (33) ◽  
pp. no-no
Author(s):  
Susumu Igarashi ◽  
Hiroshi Inami ◽  
Hiromu Hara ◽  
Masahiro Fujii ◽  
Hiroshi Koutoku ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Indole Derivatives ◽  
Synthesis And Biological Evaluation
Sign in / Sign up

Export Citation Format

Share Document