Tag: 200-300

On March 31, 2020, Hamdani, Syeda Shamila; Khan, Bilal Ahmad; Hameed, Shahid; Batool, Farwa; Saleem, Hafiza Nosheen; Ullah Mughal, Ehsan; Saeed, Muhammad published an article.HPLC of Formula: 574-98-1 The title of the article was Synthesis and evaluation of novel S-benzyl- and S-alkylphthalimide- oxadiazole -benzenesulfonamide hybrids as inhibitors of dengue virus protease. And the article contained the following:

Direct acting antiviral drugs (DAADs) are becoming therapeutics of choice for the treatment of viral infections. Successful development of anti HIV and HCV drugs by targeting the viral proteases has provided impetus for discovering newer DAADs. Dengue virus (DENV) protease, which is composed of two nonstructural proteins, NS2B and NS3pro, can be likewise exploited for discovering new anti-dengue therapeutics. In this study, we have linked together two pharmaceutically interesting motifs, namely 1,3,4-oxadiazole and benzenesulfonamide in two alternative series to develop novel S-benzylated and S-alkylphthalimidated hybrids. For the first series of hybrids, 4-aminobenzoic acid (1) was reacted with substituted benzenesulfonyl chlorides via its amino group, whereas the carboxylic acid side was elaborated to sulfonamido-1,3,4-oxadiazole-2-thiols (6a/b) in three steps. At this stage, the intermediates 6a/b were bifurcated to either S-alkylphthalimidated (8a-j) or S-benzylated (9a-c) hybrids by reacting with corresponding halides. For the alternative series of hybrids, the carboxylic acid group of probenecid (10) was similarly elaborated to sulfonamido-1,3,4-oxadiazole-2-thiols (13), and diverged to S-alkylphthalimidated (14a-f) and S-benzylated hybrids (15a-e). Bioactivity assays demonstrated that 8g and 8h are the most potent inhibitors among the synthesized analogs, exhibiting the IC50 values of 13.9 μM and 15.1 μM, resp. Computational assessment predicted the binding of the inhibitors at an allosteric site developed in the open conformation of DENV2 NS2B/NS3pro. Taken together these findings point out that the synthesized hybrid inhibitors possess a great potential for further antiviral drug development. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).HPLC of Formula: 574-98-1

The Article related to dengue virus protease antiviral drug binding benzenesulfonamide oxadiazole hybrids, Placeholder for records without volume info and other aspects.HPLC of Formula: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Auti, Prashant S.; Nandi, Arijit; Kumari, Vijeta; Paul, Atish T. published an article in 2022, the title of the article was Design, synthesis, biological evaluation and molecular modelling studies of oxoacetamide warhead containing indole-quinazolinone based novel hybrid analogues as potential pancreatic lipase inhibitors.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione And the article contains the following content:

A novel series of indolyl oxoacetamide-quinazolinone hybrid analogs (9aa-9df) were designed, synthesized, and evaluated for their in vitro pancreatic lipase (PL) inhibitory potential which may lead to efficient anti-obesity agents. All the synthesized hybrid analogs exhibited moderate to potent PL inhibitory activity (IC50 = 32.51 to 4.86 μM). Among all the analogs, 9ak, 9af, 9aj, and 9ah were found to have the most potent PL inhibitory activity (IC50 = 4.86, 5.73, 5.83, and 5.94 μM resp.), as compared to orlistat (IC50 = 0.86 μM). The most potent analogs 9af and 9ak were found to inhibit PL competitively with an inhibition constant (Ki) of 2.136, 1.648 μM. Furthermore, the docking study confirmed the binding of analogs 9ak and 9af (MolDock score of -161.25, -133.67 kcal mol-1) that exhibited docking interactions with important active site amino acids, namely Phe 77, Tyr 114, Ser 152, Arg 256, His 263, etc. Also, the anal. of analog 9ak and 9af in SeeSAR revealed the covalent inhibition of PL. In mol. dynamics simulations of 100 ns, the complex between each analog (9ak & 9af) and PL was found to be stable (RMSD < 1.5 Å). The present work highlights the importance of a hybrid drug design approach for the development of indole and quinazolinone containing hybrids as potential PL inhibitors. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to obesity indole quinazolinone mol modeling pancreatic lipase inhibitor antiobesity, Placeholder for records without volume info and other aspects.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 15, 2021, Falkowski, Michal; Kucinska, Malgorzata; Piskorz, Jaroslaw; Wieczorek-Szweda, Ewelina; Popenda, Lukasz; Jurga, Stefan; Sikora, Adam; Mlynarczyk, Dariusz T.; Murias, Marek; Marszall, Michal P.; Goslinski, Tomasz published an article.Related Products of 574-98-1 The title of the article was Synthesis of sulfanyl porphyrazines with bulky peripheral substituents – Evaluation of their photochemical properties and biological activity. And the article contained the following:

Alkylation reaction of dimercaptomaleonitrile disodium salt with N-(2-bromoethyl)phthalimide in N,N-dimethylformamide, and potassium carbonate led to novel maleonitrile derivative This compound was used in the Linstead tetramerization reaction in n-butanol in the presence of magnesium n-butoxide towards magnesium(II) sulfanyl porphyrazine with phthalimide peripheral substituents. Its demetallation and subsequent zinc(II) ion insertion led to zinc(II) sulfanyl porphyrazine derivative All obtained compounds were thoroughly characterized using UV-vis, MS, and 1H and 13C NMR spectroscopy. The purity of macrocycles was assessed using HPLC. Novel sym. porphyrazines were found to generate singlet oxygen in N,N-dimethylformamide and DMSO in low yields. The highest, over 4% yield of singlet oxygen generation, was noted for zinc(II) porphyrazine derivative in DMSO. In the biol. study, the cytotoxicities and photocytotoxicities of sym. sulfanyl porphyrazines with phthalimide peripheral substituents were compared with lately obtained unsym. sulfanyl tribenzoporphyrazine, 22,23-bis[3,5-bis(3,5-dimethoxybenzyloxy)benzylsulfanyl]tribenzo[b,g,l]porphyrazinato magnesium(II). The in vitro study was performed on androgen-sensitive human prostate adenocarcinoma (LNCaP) and human prostate cancer (PC3) cell lines using MTT assay. The data obtained for liposomal formulations containing sulfanyl porphyrazines with phthalimide substituents indicated their low and light-independent cytotoxicity against cancer cells. On the contrary, the sulfanyl tribenzoporphyrazine was studied in its free form and after incorporation in liposomes. In the free form it revealed moderate photocytotoxicity against both cancer cell lines with IC50 values of 7.71 μM and 8.82 μM for LNCaP and PC3 cells, resp. Moreover, the liposomal DOTAP : POPC formulation containing sulfanyl tribenzoporphyrazine revealed over 10-fold higher effectiveness reaching the IC50 up to 0.52 μM against LNCaP cancer cells in comparison to its free form. On the contrary, liposomal PG formulation of sulfanyl tribenzoporphyrazine was found to be inactive on the human cancer cells. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Related Products of 574-98-1

The Article related to sulfanyl porphyrazine peripheral substituent photochem property biol activity, Placeholder for records without volume info and other aspects.Related Products of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 5, 2021, Singh, Ved Prakash; Dowarah, Jayanta; Marak, Brilliant N.; Sran, Balkaran Singh; Tewari, Ashish Kumar published an article.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Study of the structure-bioactivity of fleximers: synthesis, crystal structure, Hirshfeld surface analysis, and anti-inflammatory assays. And the article contained the following:

Synthesized and natural pyridones/pyridines derivatives exhibiting diverse biol. activities. 2-Pyridone has lactam-lactim tautomerization like thymine and uracil bases. In this study, COX-2 target based series of pyridone/pyridine linked fleximers were designed, synthesized and studied. All analogs binding affinity with COX-2 active site were studied through mol. docking, and anti-inflammatory activity studied by in vivo anal. Weak interactions were studied to find binding sites among analogs through crystal packing, Hirshfeld surface anal. and in silico anal. All the analogs exhibited anti-inflammatory activity, while compound (3) is the most active analog among the series. In contrast, since compound (3) is a pyridine-phthalimide ring-containing analog, the presence of a phthalimide group probably favors anti-inflammatory activity over other types of rings. The results suggested further investigations on compounds as anti-inflammatory prodrugs. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to pyridone pyridine linked fleximer crystal packing hirshfeld surface analysis, Placeholder for records without volume info and other aspects.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 31, 2022, Heo, Jinyeong; Koh, Dahae; Woo, Minjeong; Kwon, Doyoon; de Almeida Falcao, Virginia Carla; Wood, Connor; Lee, Honggun; Kim, Kideok; Choi, Inhee; Jang, Jichan; Brodin, Priscille; Shum, David; Delorme, Vincent published an article.COA of Formula: C10H8BrNO2 The title of the article was A combination screening to identify enhancers of para-aminosalicylic acid against Mycobacterium tuberculosis. And the article contained the following:

Para-aminosalicylic acid (PAS) is an antibiotic that was largely used for the multi-therapy of tuberculosis in the twentieth century. To try to overcome the inconvenience of its low efficacy and poor tolerance, we searched for novel chem. entities able to synergize with PAS using a combination screening against growing axenic Mycobacterium tuberculosis. The screening was performed at a sub-inhibitory concentration of PAS on a library of about 100,000 small mols. Selected hit compounds were analyzed by dose-response and further probed with an intracellular macrophage assay. Scaffolds with potential additive effect with PAS are reported, opening interesting prospects for mechanism of action studies. We also report here evidence of a yet unknown bio-activation mechanism, involving activation of pyrido[1,2-a]pyrimidin-4-one (PP) derivatives through the Rv3087 protein. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).COA of Formula: C10H8BrNO2

The Article related to mycobacterium tuberculosis paraaminosalicylic acid combination screening, Placeholder for records without volume info and other aspects.COA of Formula: C10H8BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Ramachandran, Mohanraj; Syed, Asad; Marraiki, Najat; Anandan, Sambandam published an article in 2021, the title of the article was The aqueous dependent sensing of hydrazine and phosphate anions using a bis-heteroleptic Ru(II) complex with a phthalimide-anchored pyridine-triazole ligand.Synthetic Route of 574-98-1 And the article contains the following content:

Selective turn-on luminescence properties are shown by a non-luminescent metalloreceptor upon the addition of phosphate anions in CH3CN and hydrazine in CH3CN/H2O (6/4, volume/volume). The non-luminescent metalloreceptors [RuII(phen)2(TpH)]2PF6- (RtpH) and [RuII(Phen)2(TpI)]2PF6- (RtpI) {phen = 1,10-phenanthroline; TpH = 2-(2-(4-(pyridin-2-yl)-1H-1,2,3-triazol-1-yl)ethyl)isoindoline-1,3-dione; and TpI = 2-(2-(5-iodo-4-(pyridin-2-yl)-1H-1,2,3-triazol-1-yl)ethyl)isoindoline-1,3-dione} were synthesized and characterized. Both metalloreceptors have excellent sensing properties for phosphate anions (H2PO4- and H2P2O72-) over other anions in CH3CN. The limit of detection (LOD) values were calculated to be 79 nM and 48 nM for H2PO4- upon addition to RtpH and RtpI, resp. Noncovalent interactions play a key role in the sensing of phosphate anions, among which the halogen-anion interaction showed superior recognition properties over the hydrogen-anion interaction. Comparative electrochem. experiments, 1H NMR titration, 31P NMR titration, and lifetime studies also show that RtpI has better sensing properties, as evidenced by its more drastic emission response to H2PO4- anions compared with RtpH. Moreover, the metalloreceptors showed a remarkable fluorescence increase (at ~584 nm) upon the addition of hydrazine, without the interference of other amines in CH3CN/H2O (6/4, volume/volume). Interestingly, fluorescence enhancement was observed within live HeLa cells upon hydrazine addition, which is caused by the efficient photoinduced electron transfer process. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Synthetic Route of 574-98-1

The Article related to hydrazine phosphate detection luminescent indicator ruthenium complex, Placeholder for records without volume info and other aspects.Synthetic Route of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 31, 2021, Damghani, Tahereh; Moosavi, Fatemeh; Khoshneviszadeh, Mehdi; Mortazavi, Motahareh; Pirhadi, Somayeh; Kayani, Zahra; Saso, Luciano; Edraki, Najmeh; Firuzi, Omidreza published an article.Related Products of 574-98-1 The title of the article was Imidazopyridine hydrazone derivatives exert antiproliferative effect on lung and pancreatic cancer cells and potentially inhibit receptor tyrosine kinases including c-Met. And the article contained the following:

Abstract: Aberrant activation of c-Met signalling plays a prominent role in cancer development and progression. A series of 12 imidazo [1,2-α] pyridine derivatives bearing 1,2,3-triazole moiety were designed, synthesized and evaluated for c-Met inhibitory potential and anticancer effect. The inhibitory activity of all synthesized compounds against c-Met kinase was evaluated by a homogeneous time-resolved fluorescence (HTRF) assay at the concentration range of 5-25 μM. Derivatives 6d, 6e and 6f bearing Me, tert-Bu and dichloro-Ph moieties on the triazole ring, resp., were the compounds with the highest potential. They significantly inhibited c-Met by 55.3, 53.0 and 51.3%, resp., at the concentration of 25 μM. Synthetic compounds showed antiproliferative effects against lung (EBC-1) and pancreatic cancer cells (AsPc-1, Suit-2 and Mia-PaCa-2) expressing different levels of c-Met, with IC50 values as low as 3.0 μM measured by sulforhodamine B assay. Active derivatives significantly blocked c-Met phosphorylation, inhibited cell growth in three-dimensional spheroid cultures and also induced apoptosis as revealed by Annexin V/propidium iodide flow cytometric assay in AsPc-1 cells. They also inhibited PDGFRA and FLT3 at 25 μM among a panel of 16 kinases. Mol. docking and dynamics simulation studies corroborated the exptl. findings and revealed possible binding modes of the select derivatives with target receptor tyrosine kinases. The results of this study show that some imidazopyridine derivatives bearing 1,2,3-triazole moiety could be promising molecularly targeted anticancer agents against lung and pancreatic cancers. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Related Products of 574-98-1

The Article related to antiproliferative effect lung pancreatic cancer cell tyrosine kinase, Placeholder for records without volume info and other aspects.Related Products of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Rothschild, Daniel A.; Kopcha, William P.; Tran, Aaron; Zhang, Jianyuan; Lipke, Mark C. published an article in 2022, the title of the article was Gram-scale synthesis of a covalent nanocage that preserves the redox properties of encapsulated fullerenes.SDS of cas: 2567-29-5 And the article contains the following content:

Discrete nanocages provide a way to solubilize, sep., and tune the properties of fullerenes, but these 3D receptors cannot usually be synthesized easily from inexpensive starting materials, limiting their utility. Herein, we describe the first fullerene-binding nanocage (Cage4+) that can be made efficiently on a gram scale. Cage4+ was prepared in up to 57% yield by the formation of pyridinium linkages between complemantary porphyrin components that are themselves readily accessible. Cage4+ binds C60 and C70 with large association constants (>108 M-1), thereby solubilizing these fullerenes in polar solvents. Fullerene association and redox-properties were subsequently investigated across multiple charge states of the host-guest complexes. Remarkably, neutral and singly reduced fullerenes bind with similar strengths, leaving their 0/1- redox couples minimally perturbed and fully reversible, whereas other hosts substantially alter the redox properties of fullerenes. Thus, C60@Cage4+ and C70@Cage4+ may be useful as solubilized fullerene derivatives that preserve the inherent electron-accepting and electron-transfer capabilities of the fullerenes. Fulleride dianions were also found to bind strongly in Cage4+, while further reduction is centered on the host, leading to lowered association of the fulleride guest in the case of C602-. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).SDS of cas: 2567-29-5

The Article related to covalent nanocage preserve redox property encapsulated fullerene, Placeholder for records without volume info and other aspects.SDS of cas: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 15, 2021, El-Sayed, W. N.; Alkabli, J.; Althumayri, Khalid; Elshaarawy, Reda F. M.; Ismail, Lamia A. published an article.SDS of cas: 574-98-1 The title of the article was Azomethine-functionalized task-specific ionic liquid for diversion of toxic metal ions in the aqueous environment into pharmacological nominates. And the article contained the following:

By this work, a new azomethine-supported task-specific ionic liquid (ABIIL) was fabricated based on bis-(butylimidazolium hexafluorophosphate) salicylidene Schiff base. The successful formation of ABIIL was confirmed form its microanal. and spectral results. The excellent aqueous-ethanolic solubility coupled with the high chelating capacity of ABIIL enabled it to act as a multifunctional scavenger for removing of Cu(II) and Fe(III) ions from aqueous environments. Not only has that, but also transformed these toxic ions into promising pharmacol. candidates. ABIIL showed an excellent scavenging efficiency, as it can uptake up to 98.9% and 96.7% of Fe(III) and Cu(II) ions, resp., from aqueous-ethanolic effluents. Besides, it could be easily regenerated and reused for six cycles without significant loss in its efficiency. The scavenging outputs (M-ABIIL) exhibited excellent and broad-spectrum antimicrobial activity, with a slight preference toward fungi than bacteria. Fe-ABIIL is the most potent antimicrobial nominate as revealed from its MIC values (μg/mL): 16.8 (C. albicans) < 18.9 (S. aureus) < 19.5 (A. flavus) < 23.1 (E. coli). Addnl., this complex is more cytotoxic (IC50 3.40 ±0.53 μg/mL) than the clin. anticancer drug (Vinblastine, VB) (IC50 3.79 ± 1.01 μg/mL) toward colon cancer cells (HTC116), whereas it is less cytotoxic (IC50 85.66 ± 1.44 μg/mL) than VB (IC50 57.12 ± 1.95 μg/mL) to normal human cells (HeLa). Thus, ABIIL has great potential for removing toxic Cu(II) and Fe(III) ions from aqueous environments, converting them into chemotherapeutic agents. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).SDS of cas: 574-98-1

The Article related to azomethine ionic liquid toxic metal ion pharmacol nominate, Placeholder for records without volume info and other aspects.SDS of cas: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 14, 2022, Huang, Jian; Shi, Qiong; Choudhry, Namrta; Li, Hongmei; Yang, Chenglu; Kalashova, Julia; Yan, Ziqi; Li, Jinhua; Reddy, Mallu Chenna; Gopala, Sridhar Goud; Zhang, Shenqiu; Zhang, Jing; Nimishetti, Naganna; Yang, Dun published an article.HPLC of Formula: 2567-29-5 The title of the article was Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. And the article contained the following:

We used mechanism-informed phenotypic screening to identify and optimize compounds that phenocopy the genetic depletion of the mitotic aurora kinase B (AURKB) kinase. After assaying nine aryl fused seven-membered lactam compounds, we identified a hit compound 6a that was subsequently optimized to five lead compounds with low nanomolar activity, represented by the lead compound 6v (19 nM). With excellent drug-like properties, these compounds reproduced the loss of function in phenotypes of AURKB and exhibited potent cytotoxic activities in various cancer cell lines. Collectively, these data support that seven-membered lactam-based analogs might be valuable for further development as a new type of antimitotic agents for the treatment of cancer. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).HPLC of Formula: 2567-29-5

The Article related to lactam compound prepnd aurora kinase b inhibitor cancer, Placeholder for records without volume info and other aspects.HPLC of Formula: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary