38922-77-9Relevant articles and documents
DNA binding ligands targeting drug-resistant bacteria: Structure, activity, and pharmacology
Kaizerman, Jacob A.,Gross, Matthew I.,Ge, Yigong,White, Sarah,Hu, Wenhao,Duan, Jian-Xin,Baird, Eldon E.,Johnson, Kirk W.,Tanaka, Richard D.,Moser, Heinz E.,Bürli, Roland W.
, p. 3914 - 3929 (2003)
We describe the lead optimization and structure-activity relationship of DNA minor-groove binding ligands, a novel class of antibacterial molecules. These compounds have been shown to target A/T-rich sites within the bacterial genome and, as a result, inhibit DNA replication and RNA transcription. The optimization was focused on N-terminal aromatic heterocycles and C-terminal amines and resulted in compounds with improved in vivo tolerability and excellent in vitro antibacterial potency (MIC ≥ 0.031 μg/mL) against a broad range of Gram-positive pathogens, including drug-resistant strains such as methicillin-resistant Stapylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), and vancomycin-resistant Enterococcus faecalis (VRE). In a first proof-of-concept study, a selected compound (35) showed in vivo efficacy in a mouse peritonitis model against methicillin-sensitive S. aureus infection with an ED50 value of 30 mg/kg.
Synthesis and biological evaluation of novel imidazo[1,2-a]pyridine-oxadiazole hybrids as anti-proliferative agents: Study of microtubule polymerization inhibition and DNA binding
Babu, Bathini Nagendra,Jadhav, Govinda Shivaji,Kadagathur, Manasa,Kiranmai, Gaddam,Nagesh, Narayana,Parimala Devi, G.,Sana, Sravani,Shankaraiah, Nagula,Sigalapalli, Dilep Kumar,Tangellamudi, Neelima D.,Tokala, Ramya,Tripura, Chaturvedula
, (2021/06/30)
Efforts towards the development of potential anticancer agents, a new series of imidazo[1,2-a]pyridine-oxadiazole hybrids were synthesized and evaluated for their in vitro anticancer activity against lung cancer (A549) and prostate cancer (PC-3, DU-145) cell lines. Amongst the compounds tested, 6d showed the highest potency on A549 cells with an IC50 value of 2.8 ± 0.02 μM. Flow cytometric analysis of compound 6d treated A549 cells showed apoptosis induction by annexin-v/PI dual staining assay and the effect of 6d on different phases of cell cycle was also analyzed. Target based studies demonstrated the inhibition of tubulin polymerization by 6d at an IC50 value of 3.45 ± 0.51 μM and its effective binding with CT-DNA. Further, the molecular modelling studies revealed that 6d has a prominent binding affinity towards α/β-tubulin receptor with admirable physico-chemical properties.
Design, synthesis, in vitro evaluation and molecular docking study of N'-Arylidene imidazo [1,2-a] pyridine -2-carbohydrazide derivatives as novel Tyrosinase inhibitors
Damghani, Tahereh,Edraki, Najmeh,Hadaegh, Saba,Khoshneviszadeh, Mehdi,Pirhadi, Somayeh,Sabet, Razieh,khoshneviszadeh, Mahsima
, (2020/07/21)
A novel series of imidazo[1,2-a]pyridine 2-carbohudrazide derivatives bearing different arylidene pendantrs were designed, synthesized and evaluated for their inhibitory activity against mushroom Tyrosinase. It was found that compounds bearing 3-nitro (6j) and 4?hydroxy (6g) moieties on the arylidene pendant exhibited the best Tyrosinase inhibitory activity with IC50 values of 7.19 and 8.11 μM, respectively. These results were comparable to that of kojic acid as the reference drug (IC50 = 9.64±0.5 μM). Additionally, molecular docking analysis was performed to study the interactions and binding modes of compounds 6j, 6h and 6g which are showing the potential of two critical pi-pi interactions with His263 and Phe264 in the active site of Tyrosinase. The results indicated that 6j and 6g could be introduced as potent Tyrosinase inhibitors that might serve as promising candidates in medicine, cosmetics or food industry.