Month: November 2022

Wang, Lin; Fang, Zhijie published an article in 2020, the title of the article was Study on the synthesis and biological activities of N-alkylated deoxynojirimycin derivatives with a terminal tertiary amine.Electric Literature of 574-98-1 And the article contains the following content:

A series of N-alkylated deoxynojirimycin (DNJ) derivatives I (n = 1, 3; R = R1 = Me; RR1 = -(CH2)4-, -(CH2)5-, -(CH2)2O(CH2)2-) connected to a terminal tertiary amine at the alkyl chains of various lengths was prepared These novel synthetic compounds I were assessed for preliminary glucosidase inhibition and anticancer activities in vitro. Potent and selective inhibition was observed among them. Compound I (n = 1; RR1 = -(CH2)2O(CH2)2-) II (IC50 = 0.052μM) showed improved and selective inhibitory activity against β-glucosidase compared to DNJ (IC50 = 0.65μM). In addition, anal. of the kinetics of enzyme inhibition by using Lineweaver-Burk plots indicated that II inhibited β-glucosidase in a competitive manner, suggesting that II was expected to bind to the active site of β-glucosidase. Compounds I [n = 3; RR1 = -(CH2)4-, -(CH2)5-] were found to be moderate and selective inhibitors of α-glucosidase. Nevertheless, none of compounds inhibited the growth of B16F10 melanoma cells. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Electric Literature of 574-98-1

The Article related to tertiary amine alkyl deoxynojirimycin preparation glucosidase inhibition antitumor activity, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.Electric Literature of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 24, 2015, Kancharla, Papireddy; Kelly, Jane Xu; Reynolds, Kevin A. published an article.Application In Synthesis of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde The title of the article was Synthesis and Structure-Activity Relationships of Tambjamines and B-Ring Functionalized Prodiginines as Potent Antimalarials. And the article contained the following:

Synthesis and antimalarial activity of 94 novel bipyrrole tambjamines (TAs) and a library of B-ring functionalized tripyrrole prodiginines (PGs) against a panel of Plasmodium falciparum strains are described. The activity and structure-activity relationships demonstrate that the ring-C of PGs can be replaced by an alkylamine, providing for TAs with retained/enhanced potency. Furthermore, ring-B of PGs/TAs can be substituted with short alkyl substitutions at either 4-position (replacement of OMe) or 3- and 4-positions without impacting potency. Eight representative TAs and two PGs have been evaluated for antimalarial activity against multidrug-resistant P. yoelii in mice in the dose range of 5-100 mg/kg × 4 days by oral administration. The KAR425 TA (I) offered greater efficacy than previously observed for any PG, providing 100% protection to malaria-infected mice until day 28 at doses of 25 and 50 mg/kg × 4 days, and was also curative in this model in a single oral dose (80 mg/kg). This study presents the first account of antimalarial activity in tambjamines. The experimental process involved the reaction of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde(cas: 89909-51-3).Application In Synthesis of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde

The Article related to antimalarial tambjamine prodiginine preparation sar, Alkaloids: Alkaloids Containing Three Or More Nitrogen Atoms and other aspects.Application In Synthesis of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 3, 2016, Kancharla, Papireddy; Kelly, Jane Xu; Reynolds, Kevin A. published a patent.HPLC of Formula: 89909-51-3 The title of the patent was Preparation of tambjamines and B-ring functionalized prodiginines as potent antimalarials. And the patent contained the following:

The invention is related to compounds I [(i) R1 is H, lower alkyl or lower alkoxy; R2 is H, lower alkyl, lower alkoxy, halo, or pyrrolyl; R3 is aryl or heteroaryl; and R4 is cycloalkyl; or (ii) R1-3 independently are lower alkyl; and R4 is alkyl or cycloalkyl] and II and their pharmaceutically acceptable salts. Specifically, the synthesis and antimalarial activity of 94 novel bipyrrole tambjamines (TAs) and a library of B-ring functionalized tripyrrole prodiginines (PGs) against a panel of Plasmodium falciparum strains are described. The activity and structure-activity relationships demonstrate that the ring-C of PGs can be replaced by an alkylamine, providing for TAs with retained/enhanced potency. Furthermore, ring-B of PGs/TAs can be substituted with short alkyl substitutions at either 4-position (replacement of OMe) or 3- and 4-positions without impacting potency. Eight representative TAs and two PGs have been evaluated for antimalarial activity against multidrug-resistant P. yoelii in mice in the dose range of 5-100 mg/kg × 4 days by oral administration. The KAR425 TA (III) offered greater efficacy than previously observed for any PG, providing 100% protection to malaria-infected mice until day 28 at doses of 25 and 50 mg/kg × 4 days, and was also curative in this model in a single oral dose (80 mg/kg). III was tested using the Ames assay at concentration of 10 uM, with and without S9 activation, against Salmonella typhimurium TA1OO and TA98, there was no increase over the background reversion rate demonstrating its non-genotoxic character. The experimental process involved the reaction of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde(cas: 89909-51-3).HPLC of Formula: 89909-51-3

The Article related to antimalarial tambjamine prodiginine preparation sar, Alkaloids: Alkaloids Containing Three Or More Nitrogen Atoms and other aspects.HPLC of Formula: 89909-51-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 9, 2021, Kaldor, Stephen W.; Tyhonas, John; Murphy, Eric A.; Kanouni, Toufike; Arnold, Lee D.; Kania, Robert; Cox, Jason M. published a patent.Safety of 5-Bromo-4-chloro-2-fluoroaniline The title of the patent was Pyrazolecarboxamides as inhibitors of fibroblast growth factor receptor kinases and their preparation. And the patent contained the following:

Provided herein are heteroaryl compounds as inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases. Compounds of formula I wherein Z is (un)substituted alkenoyl, (un)substituted alkynoyl, (un)substituted cyanoacetyl, etc.; R is H, (un)substituted C1-6 alkyl, (un)substituted C3-7 carbocyclyl, (un)substituted C3-7 heterocyclyl, etc.; R4 is (un)substituted 9- to 10-membered heteroaryl; R6 is (un)substituted alkyl (un)substituted carbocyclylalkyl and (un)substituted heterocyclylalkyl; and pharmaceutically acceptable salts and solvates thereof, are claimed. Example compound II was prepared by coupling of 3-bromo-1-[(3S,5R)-5-(methoxymethyl)-1-(prop-2-enoyl)pyrrolidin-3-yl]-5-(methylamino)pyrazole-4-carboxamide and 5-ethynyl-2-methylbenzimidazole. The invention compounds were evaluated for their FGFR2 kinase inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of ≤ 0.10μM. The experimental process involved the reaction of 5-Bromo-4-chloro-2-fluoroaniline(cas: 111010-07-2).Safety of 5-Bromo-4-chloro-2-fluoroaniline

The Article related to pyrazolecarboxamide preparation fgfr2 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Safety of 5-Bromo-4-chloro-2-fluoroaniline

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 14, 2021, Garofalo, Albert W.; De Lombaert, Stephane; Schwarz, Jacob Bradley; Andreotti, Daniele; Sabbatini, Fabio Maria; Serra, Elena; Bernardi, Silvia; Migliore, Marco; Budassi, Federica; Beato, Claudia published a patent.Related Products of 1427433-22-4 The title of the patent was Indazoles and azaindazoles as LRRK2 inhibitors in the treatment of CNS disorders and their preparation. And the patent contained the following:

The invention relates compounds of formula I, their preparation and their use as inhibitors of LRRK2 in the treatment of CNS disorders. Compound I, wherein A is halo, (un)subsititued C1-6 alkyl, (un)subsititued C2-6 alkenyl, etc.; ring B is Ph and 5- to 10-membered heteroaryl wherein said 5- to 10-membered heteroaryl comprises 1, 2 and 3 ring-forming heteroatoms independently864 selected from N, O and S; X2 is N and CR2; X3 is N and CR3; X4 is N and CR4; no more than two of X2, X3 and X4 are simultaneously N; R1 is independently H, halo, C1-6 alkyl, etc.; R2 and R4 are independently H, halo, C2-6 alkenyl, etc.; R3 is H, halo, C1-6 haloalkyl, etc.; n is 0, 1, 2, and 3; and pharmaceutically acceptable salts thereof, are claimed. Compound II was prepared by reacting 3-bromo-1H-indazol-5-amine with 3-furanylboronic acid yielding 3-(furan-3-yl)-1H-indazole-5-amine, then 5-cyano-3-fluoropyridine-2-carboxylic acid underwent amidation with 3-(furan-3-yl)-1H-indazole-5-amine to yield compound II. Compound II was evaluated for LRRK2 inhibitory activity resulting in a wild type LRRK2 and G2019S LRRK2 IC50 of ≤ 100 nM for both. Compounds of the invention were evaluated for their LRRK2 inhibitory activity (data given). The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methyl-benzoic acid(cas: 1427433-22-4).Related Products of 1427433-22-4

The Article related to indazole azaindazole preparation lrrk2 inhibitor cns disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 1427433-22-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 19, 2018, Blagg, Brian S. J.; Kent, Caitlin Nicole; Mishra, Sanket Jaiprakash; Khandelwal, Anuj published a patent.Related Products of 39503-58-7 The title of the patent was Preparation of isoindolin-2-ylmethanone compounds as Hsp90b selective inhibitors for treatment of cancer. And the patent contained the following:

Provided are compounds of formula I as well as compositions including such compounds useful for the treatment of cancers such as non-small cell lung cancer, bladder cancer, or colon cancer. I [wherein each X independently = H, halo, sulfoxide, sulfone, etc.; R1 = H, OH, C1-3 alkyl, etc.; R2 = CH2X5 or OH; X5 = OH, halo, CN, etc.; R3 = alkyl, -CH(CH3)2, CF3, etc.] or a pharmaceutically acceptable salt and/or solvate thereof, are claimed and exemplified. Example compound II was prepared from a multistep procedure (preparation given). Exemplified I was evaluated for antiproliferative activity in cancer cell lines with II demonstrating IC50 values as low as 6.74 ± 1.1 μM in NCI-H23 non-small cell lung cancer cells. The experimental process involved the reaction of Methyl 5-bromo-2-methoxy-4-methylbenzoate(cas: 39503-58-7).Related Products of 39503-58-7

The Article related to isoindolinylmethanone compound preparation hsp90b inhibitor cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 39503-58-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 21, 2022, Garofalo, Albert W.; Schwarz, Jacob Bradley; Sabbatini, Fabio Maria; Migliore, Marco; Bernardi, Silvia; Budassi, Federica published a patent.Related Products of 1427433-22-4 The title of the patent was Preparation of indazoles and azaindazoles as LRRK2 inhibitors. And the patent contained the following:

The present invention is directed to indazole and azaindazole derivatives I and II [A = (un)substituted aryl, cycloalkyl, 5-14 membered heteroaryl, etc.; L = O or NH; ring B = Ph or 6-membered heteroaryl; ring C = Ph or 6-membered heteroaryl, wherein ring C is fused to ring D; X2 = N or CR2; X3 = N or CR3; X4 = N or CR4; wherein not more than two of X2, X3, and X4 are simultaneously N; each R1 and R5 = (independently) H, halo, alkyl, etc.; R2-R4 = (independently) H, halo, alkyl, etc.; n = 0-3; m = 0-1; p = 0-3; wherein in I: when ring B = Ph, then n = 1-3 and R1 = group other than H] or pharmaceutically acceptable salts thereof which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders such as Parkinson’s disease. E.g., a multi-step synthesis of III, starting from 6-bromo-1H-indazole and 1-cyclopropyl-4-iodopyrazole, was described. Exemplified compounds I and II were tested in the LRRK2 kinase activity assay (data given). Pharmaceutical composition comprising compound I or II was disclosed. The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methyl-benzoic acid(cas: 1427433-22-4).Related Products of 1427433-22-4

The Article related to indazole azaindazole preparation lrrk2 inhibitor cns disorder parkinson disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 1427433-22-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On March 15, 1989, Hill, William E.; Islam, Mohammed Q.; Webb, Thomas R.; McAuliffe, Charles A. published an article.Recommanded Product: (6-Bromohexyl)triphenylphosphonium bromide The title of the article was Solution studies of gold(I) complexes of n-hexyldimethylphosphine, n-butyldiphenylphosphine, 1-dimethylphosphino-6-diphenylphosphinohexane, 1,6-bis(dimethylphosphino)hexane and 1,6-bis(diphenylphosphino)hexane. And the article contained the following:

The 31P{1H} NMR spectra of the monodentate phosphines (L = PMe2(C6H13) (L1) and PPh2Bu (L2)) in the presence of Et4N[AuBr2] in CDCl3 solution were studied at various L:Au ratios and temperatures At 195 K and a P:Au ratio = 1, only [BrAuL] is present. Increasing the amount of phosphine leads to [BrAuL2], [AuL3]Br and [AuL4]Br. When AuBr2-, L1 and L2 are mixed in a 1:1:1 ratio [BrAuL1], [BrAuL12], [BrAuL2], [BrAuL22] and [BrAuL1L2] are present. Addition of more L1 causes the disappearance of [BrAuL1] with formation of [BrAuL12]; however this does not occur for L2 when [BrAuL2] is still present even at a Au:L1:L2 ratio of 1:1:2. Employing the unsym. Ph2P(CH2)6PMe2 (L3) gives [BrAuL3AuBr], 3-coordinate (BrAuL32AuBr] (2 forms) and 3-coordinate AuL3Br. Similar studies for the sym. Ph2P(CH2)6PPh2 (dph) and Me2P(CH2)6PMe2 are reported. The rate constants for the exchange BrAuL1 ⇌ BrAuL12, BrAuL2 ⇌ BrAuL12 and BrAu(dph)AuBr ⇌ BrAu(dph)2AuBr were determined from the 31P〈1H〉 NMR spectra. Activation parameters were calculated by a least-squares method. The activation entropies for the exchange processes range from -1.1 to 13.9 cal(mol deg)-1 depending on the ligand type. An associative mechanism is more probable although the possibility of a dissociative process cannot be ruled out. An improved synthetic method is reported for unsym. bisphosphines with chain length > (CH2)4. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).Recommanded Product: (6-Bromohexyl)triphenylphosphonium bromide

The Article related to kinetics exchange gold bromo phosphine, phosphine substitution gold bromo complex, Inorganic Chemicals and Reactions: Reactions (Nonpreparative) and other aspects.Recommanded Product: (6-Bromohexyl)triphenylphosphonium bromide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zeng, Leli; Ma, Gongcheng; Xu, Han; Mu, Jing; Li, Fan; Gao, Xiaoting; Deng, Zhuoting; Qu, Junle; Huang, Peng; Lin, Jing published an article in 2019, the title of the article was In Vivo Chemoselective Photoacoustic Imaging of Copper(II) in Plant and Animal Subjects.Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione And the article contains the following content:

The detection of Cu2+ in living plants and animals is of great importance for environment monitoring and disease diagnosis. Here, a near-IR (NIR) turn-on photoacoustic (PA) probe (denoted as LET-2) is developed for Cu2+ detection in living subjects, such as soybean sprouts and mice. The absorbance band of LET-2 shifts from 625 to 715 nm after the interaction with Cu2+, thus producing strong PA signal output at 715 nm (PA715) as an indicator. The PA715 value is increased as a function of the concentration of Cu2+ (0 × 10-6-20 × 10-6M), with a calculated limit of detection of 10.8 × 10-9M. More importantly, both in vitro and in vivo studies in soybean sprouts and mice indicate that the as-prepared LET-2 PA probe is highly sensitive and selective for Cu2+ detection. These findings provide a solution for in vivo detection of metal ions by using chemoselective PA probes. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to photoacoustic imaging copper plant animal, animals, copper detection, in vivo, photoacoustic imaging, plants, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 15, 2021, Sturbaut, Manon; Bailly, Fabrice; Coevoet, Mathilde; Sileo, Pasquale; Pugniere, Martine; Liberelle, Maxime; Magnez, Romain; Thuru, Xavier; Chartier-Harlin, Marie-Christine; Melnyk, Patricia; Gelin, Muriel; Allemand, Frederic; Guichou, Jean-Francois; Cotelle, Philippe published an article.Category: bromides-buliding-blocks The title of the article was Discovery of a cryptic site at the interface 2 of TEAD – Towards a new family of YAP/TAZ-TEAD inhibitors. And the article contained the following:

The Hippo pathway is involved in organ size control and tissue homeostasis by regulating cell growth, proliferation and apoptosis. It controls the phosphorylation of the transcription co-activator YAP (Yes associated protein) and TAZ (Transcriptional coactivator with PDZ-binding motif) in order to control their nuclear import and their interaction with TEAD (Transcriptional Enhanced Associated Domain). YAP, TAZ and TEADs are dysregulated in several cancers making YAP/TAZ-TEAD interaction a new emerging anti-cancer target. We report the synthesis of a set of trisubstituted pyrazoles which bind to hTEAD2 at the interface 2 revealing for the first time a cryptic pocket created by the movement of the phenol ring of Y382. Compound I disrupts YAP/TAZ-TEAD interaction in HEK293T cells and inhibits TEAD target genes and cell proliferation in MDA-MB-231 cells. Compound I is therefore the first inhibitor of YAP/TAZ-TEAD targeting interface 2. This mol. could serve with other pan-TEAD inhibitors such as interface 3 ligands, for the delineation of the relative importance of VGLL vs YAP/TAZ in a given cellular model. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Category: bromides-buliding-blocks

The Article related to pyrazole preparation tead2 inhibitor structure activity relationship, binding assays, hippo pathway, interface 2, tead cryptic binding pocket, tead inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary