20718-46-1Relevant academic research and scientific papers
Synthesis and antimicrobial studies of selenadiazolo benzimidazoles
Kuarm, B. Suresh,Madhav, J. Venu,Rajitha
, p. 1337 - 1341 (2013)
An efficient and eco-friendly method has been developed for the synthesis of selenadiazolo benzimidazoles by the condensation of N-benzylbenzo[c][1,2,5] selenadiazole-4,5-diamine with various aromatic aldehydes catalyzed by xanthan sulfuric acid. All the synthesized compounds 5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i, 5j were evaluated for in vitro antibacterial activity against Gram-positive bacterial strains (Bacillus subtilis, Staphylococcus aureus, and Streptococcus pyogenes), and Gram-negative bacterial strains (Escherichia coli, Klebsiella pneumonia, and Salmonella typhimurium) and antifungal against Aspergillus niger, Candida albicans, and Aspergillus flavus (Fungi). Compound 5i emerged as the most interesting compound in this series exhibiting excellent antimicrobial activity.
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.
INHIBITION OF HIF-2α HETERODIMERIZATION WITH HIF1β (ARNT)
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Paragraph 0103, (2014/06/11)
Provided is a method of inhibiting heterodimerization of HIF-2α to HIF1β (ARNT) comprising binding certain small molecules to the HIF-2α PAS-B domain cavity but not to HIF1α and inhibiting HIF-2α heterodimerization to HIF1β (ARNT) but not inhibiting HIF1α
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.
TRICYCLIC ANILIDE HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS
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Page/Page column 73-74, (2009/01/24)
Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y 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.
INDOLYLMALEIMIDE DERIVATIVES
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Page/Page column 42-43, (2008/06/13)
A compound of formula (I) wherein R, R1, and R2, ring A and ring B are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
SPIROLACTAM TRICYCLIC CGRP RECEPTOR ANTAGONISTS
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Page/Page column 114, (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.
SPIROHYDANTOIN TRICYCLIC CGRP RECEPTOR ANTAGONISTS
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Page/Page column 110, (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, R6, 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.
TRICYCLIC ANILIDE SPIROHYDANTOIN CGRP RECEPTOR ANTAGONISTS
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Page/Page column 54, (2008/06/13)
The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, T, U, V, W, X, Y, Z, R4, R5a?, R5b/su
TRICYCLIC ANILIDE SPIROLACTAM CGRP RECEPTOR ANTAGONISTS
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Page/Page column 77-78, (2010/10/20)
The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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.
