1123-92-8Relevant articles and documents
Design and Synthesis of 11H-Xantheno[2,1-c][1,2,5]Selenadiazol-11-One Derivatives as Potent Antimicrobial and Antitubercular Agents
Bowroju, Suresh Kuarm,Marumamula, Hanumaiah,Bavanthula, Rajitha
, p. 593 - 600 (2021/05/03)
Abstract: A series of 11H-xantheno[2,1-c][1,2,5]selenadiazol-11-one derivatives (Va–m) that incorporate a variety of substituents have been synthesized under both conventional heating and microwave irradiation procedures. All these analogs were evaluated for their antimicrobial activity against the Gram-positive bacteria Bacillus subtilis (BS), Staphylococcus aureus (SA), and Staphylococcus epidermidis (SE), against the Gram-negative bacteria Escherichia coli (EC), Pseudomonas aeruginosa (PA), and Klebsiella pneumonia (KP), and against the fungal species Candida albicans (CA), Candida rugosa (CR), Rhizopus oryzae (RO), and Aspergillus niger (AN) and antitubercular activity against MTB H37Rv. Analog, 7,9-dimethoxy-11H-xantheno[2,1-c][1,2,5]selenadiazol-11-one (Vc) was identified as a potent antibacterial agent (MIC[BS] = 2.5 μg/mL, MIC[SA] = 10 μg/mL, MIC[SE] = 2.5 μg/mL, MIC[EC] = 5 μg/mL, MIC[PA] = 10 μg/mL, MIC[KP] = 2.5?μg/mL), and a potent antifungal agent (MIC[CA] = 15 μg/mL, MIC[CR] = 15 μg/mL, MIC[RO] = 10?μg/mL). Another analog, 7,9-dimethyl-11H-xantheno[2,1-c][1,2,5]selenadiazol-11-one (Vj) was also identified as a potent antibacterial agent (MIC[BS] = 2.5 μg/mL, MIC[SA] = 15 μg/mL, MIC[SE] = 2.5 μg/mL, MIC[EC] = 10 μg/mL, MIC[PA] = 15 μg/mL, MIC[KP] = 20 μg/mL), and a potent antifungal agent (MIC[CA]?= 2.5 g/mL, MIC[CR] = 10 μg/mL MIC[RO] = 15 μg/mL and MIC[AN] = 10 μg/mL). Based on the MIC data analogs, 7,9-dimethoxy-11H-xantheno[2,1-c][1,2,5]selenadiazol-11-one (Vc) and 7,9-dimethyl-11H-xantheno[2,1-c][1,2,5]selena-diazol-11-one (Vj) were identified as the most potent antimicrobial agents in the series. All these 11H-xantheno[2,1-c][1,2,5]selenadiazol-11-one derivatives (Va–m) were also evaluated for their antitubercular activity against MTB H37Rv. Analogs, 7,9-dimethoxy-11H-xantheno[2,1-c][1,2,5]selenadiazol-11-one (Vc) and 7,9-dimethyl-11H-xantheno[2,1-c][1,2,5]selenadiazol-11-one (Vj) showed MIC of 3.12 μg/mL. These results suggest that analogs, 7,9-dimethoxy-11H-xantheno[2,1-c][1,2,5]selenadiazol-11-one (Vc) and 7,9-dimethyl-11H-xantheno[2,1-c][1,2,5]selenadiazol-11-one (Vj) may be a potential multifunctional ligands for the development of highly effective antimicrobial and antitubercular activity.
Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor
Rogers, Jamie L.,Bayeh, Liela,Scheuermann, Thomas H.,Longgood, Jamie,Key, Jason,Naidoo, Jacinth,Melito, Lisa,Shokri, Cameron,Frantz, Doug E.,Bruick, Richard K.,Gardner, Kevin H.,MacMillan, John B.,Tambar, Uttam K.
supporting information, p. 1739 - 1747 (2013/03/29)
Hypoxia inducible factors (HIFs) are heterodimeric transcription factors induced in a variety of pathophysiological settings, including cancer. We describe the first detailed structure-activity relationship study of small molecules designed to inhibit HIF-2α-ARNT heterodimerization by binding an internal cavity of the HIF-2α PAS-B domain. Through a series of biophysical characterizations of inhibitor-protein interactions (NMR and X-ray crystallography), we have established the structural requirements for artificial inhibitors of the HIF-2α-ARNT PAS-B interaction. These results may serve as a foundation for discovering therapeutic agents that function by a novel mode of action.
SPIROLACTAM TRICYCLIC CGRP RECEPTOR ANTAGONISTS
-
Page/Page column 113, (2008/06/13)
Compounds of formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, J, K, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.