1123-92-8

Upstream product

• 95-83-0 4-Chloro-1,2-phenylenediamine 
• 95-54-5 1,2-diamino-benzene 
• 7446-08-4 selenium(IV) oxide 
• 1635-61-6 5-chloro-2-nitroaniline 
• 89-63-4 4-Chloro-2-nitroaniline 

Downstream Products

• 20718-46-1 5-chloro-4-nitro-2,1,3-benzoselenadiazole 
• 92588-88-0 5-chloro-2,1,3-benzoselenadiazole * 7,7,8,8-tetracyano-p-quinodimethane 
• 77597-85-4 3-chloro-5-(1,2-benzoselenazol-3-yl)pentadienonitrile 
• 77597-80-9 2-(4-chloro-2-pyridyl)phenyl selenocyanate 
• 77597-83-2 cis-4-chloro-5-(1,2-benzoselenazol-3-yl)pentadienonitrile 
• 77597-92-3 2-(5-chloro-2-pyridyl)phenyl diselenide 
• 147021-82-7 4-nitro-2,1,3-benzoselenadiazol-5-ol 
• 862179-93-9 5-chloro-2-phenylsulfanyl-1H-benzoimidazol-4-ylamine 
• 862179-91-7 5-chloro-4-nitro-2-phenylsulfanyl-1H-benzoimidazole 
• 862179-95-1 N-(1-acetyl-5-chloro-2-phenylsulfanyl-1H-benzoimidazol-4-yl)-acetamide 
• 1422955-36-9 C₁₃H₉ClFN₅O₂ 
• 1422955-34-7 C₁₃H₈ClFN₄O₂ 
• 32046-86-9 5-chloro-4-nitro-1⁽³⁾H-benzoimidazole 
• 144729-44-2 4-chloro-3-nitro-1,2-phenylenediamine 

Relevant academic research and scientific papers

Design and Synthesis of 11H-Xantheno[2,1-c][1,2,5]Selenadiazol-11-One Derivatives as Potent Antimicrobial and Antitubercular Agents

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)

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

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

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.

SPIROLACTAM TRICYCLIC CGRP RECEPTOR ANTAGONISTS

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

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

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

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.

Phototransformations of 6-X-5-nitroquinoxalines

Photophysical properties and photochemical activity of 6-X-5- nitroquinoxalines with electron-donor substituents (X = H, CH3, Cl, OC2H5, NH2) ortho to the nitro group were studied. The quantum yield of the formation of 5-hydroxyquinoxaline from the corresponding nitro derivative depends on the nature of the substituent and irradiation conditions. Phototransformations can go through nitro-nitrite rearrangement with the participation of two alternative T(nπ*) levels, depending on the size and electronic effects of the substituent. The latter factor is largely determined by the population on excitation of different charge-transfer states involving the nitro group.

Regiospecific Oxidative Nitration of 3,4-Dihydro-6,7-disubstituted Quinoxalin-2(1H)-ones Gives 1,4-Dihydro-5-nitro-6,7-disubstituted Quinoxaline-2,3-diones, Potent Antagonists at the NMDA/Glycine Site

The regiospecific oxidative nitration of 3,4-dihydro-6,7-disubstituted quinoxalin-2(1H)-ones (15a-h, 20) utilizing fuming nitric acid in TFA gave 1,4-dihydro-5-nitro-6,7-disubstituted quinoxaline-2,3-diones (6a-i), respectively, in good yields.Compounds 15a-h were prepared from commercially available 1-halo-3,4-disubstituted benzenes 12a-h in three steps.These were nitration, nucleophilic substitution of the halogen ortho to the nitro group with sodium glycinate, and finally, reduction of the nitro group and concomitant cyclization.Compound 20 was prepared from 16 by a different route involving alkylation of substituted o-nitroaniline 18.The final oxidative nitration yields a single, predictable nitro isomer and is a significant improvement over the direct nitration of 6,7-disubstituted quinoxaline-2,3-diones.