Author: Jessica.F

Synthesis and antimalarial activity of chain substituted pivaloyloxymethyl ester analogues of Fosmidomycin and FR900098 was written by Kurz, Thomas;Schlueter, Katrin;Kaula, Uwe;Bergmann, Baerbel;Walter, Rolf D.;Geffken, Detlef. And the article was included in Bioorganic & Medicinal Chemistry in 2006.Safety of 2-(Bromomethyl)-1,3-dimethylbenzene This article mentions the following:

Fosmidomycin is a promising antimalarial drug candidate with a unique chem. structure and a novel mode of action. Chain substituted pivaloyloxymethyl ester derivatives of Fosmidomycin and its acetyl analog FR900098 have been synthesized and their in vitro antimalarial activity vs. the Chloroquine sensitive strain 3D7 of Plasmodium falciparum has been determined In the experiment, the researchers used many compounds, for example, 2-(Bromomethyl)-1,3-dimethylbenzene (cas: 83902-02-7Safety of 2-(Bromomethyl)-1,3-dimethylbenzene).

2-(Bromomethyl)-1,3-dimethylbenzene (cas: 83902-02-7) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Safety of 2-(Bromomethyl)-1,3-dimethylbenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Optimization of Phenyl-Substituted Benzimidazole Carboxamide Poly(ADP-Ribose) Polymerase Inhibitors: Identification of (S)-2-(2-Fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a Highly Potent and Efficacious Inhibitor was written by Penning, Thomas D.;Zhu, Gui-Dong;Gong, Jianchun;Thomas, Sheela;Gandhi, Viraj B.;Liu, Xuesong;Shi, Yan;Klinghofer, Vered;Johnson, Eric F.;Park, Chang H.;Fry, Elizabeth H.;Donawho, Cherrie K.;Frost, David J.;Buchanan, Fritz G.;Bukofzer, Gail T.;Rodriguez, Luis E.;Bontcheva-Diaz, Velitchka;Bouska, Jennifer J.;Osterling, Donald J.;Olson, Amanda M.;Marsh, Kennan C.;Luo, Yan;Giranda, Vincent L.. And the article was included in Journal of Medicinal Chemistry in 2010.Product Details of 179232-29-2 This article mentions the following:

We have developed a series of phenylpyrrolidine- and phenylpiperidine-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase (PARP) inhibitors with excellent PARP enzyme potency as well as single-digit nanomolar cellular potency. These efforts led to the identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (22b, A-966492) (I). Compound 22b displayed excellent potency against the PARP-1 enzyme with a K_i of 1 nM and an EC₅₀ of 1 nM in a whole cell assay. In addition, 22b is orally bioavailable across multiple species, crosses the blood-brain barrier, and appears to distribute into tumor tissue. It also demonstrated good in vivo efficacy in a B16F10 s.c. murine melanoma model in combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in combination with carboplatin. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2Product Details of 179232-29-2).

Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Product Details of 179232-29-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Chemo-proteomics exploration of HDAC degradability by small molecule degraders was written by Xiong, Yuan;Donovan, Katherine A.;Eleuteri, Nicholas A.;Kirmani, Nadia;Yue, Hong;Razov, Anthony;Krupnick, Noah M.;Nowak, Radoslaw P.;Fischer, Eric S.. And the article was included in Cell Chemical Biology in 2021.Quality Control of N-(5-Bromopentyl)phthalimide This article mentions the following:

Targeted protein degradation refers to the use of small mols. that recruit a ubiquitin ligase to a target protein for ubiquitination and subsequent proteasome-dependent degradation While degraders have been developed for many targets, key questions regarding degrader development and the consequences of acute pharmacol. degradation remain, specifically for targets that exist in obligate multi-protein complexes. Here, we synthesize a pan-histone deacetylase (HDAC) degrader library for the chemo-proteomic exploration of acute degradation of a key class of chromatin-modifying enzymes. Using chemo-proteomics, we not only map the degradability of the zinc-dependent HDAC family identifying leads for targeting HDACs 1-8 and 10 but also explore important aspects of degrading epigenetic enzymes. We discover cell line-driven target specificity and that HDAC degradation often results in collateral loss of HDAC-containing repressive complexes. These findings potentially offer a new mechanism toward controlling chromatin structure, and our resource will facilitate accelerated degrader design and development for HDACs. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Quality Control of N-(5-Bromopentyl)phthalimide).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Quality Control of N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Orally active C-6 heteroaryl- and heterocyclyl-substituted imidazo[1,2-a]pyridine acid pump antagonists (APAs) was written by Bailey, Nick;Bamford, Mark J.;Brissy, Delphine;Brookfield, Joanna;Demont, Emmanuel;Elliott, Richard;Garton, Neil;Farre-Gutierrez, Irene;Hayhow, Thomas;Hutley, Gail;Naylor, Antoinette;Panchal, Terry A.;Seow, Hui-Xian;Spalding, David;Takle, Andrew K.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2009.Category: bromides-buliding-blocks This article mentions the following:

Acid pump antagonists (APAs) such as the imidazo[1,2-a]pyridine AZD-0865 I have proven efficacious at low oral doses in acid related gastric disorders. Herein some of the broader SAR in this class of mol. are described and detail the discovery of an imidazo[1,2-a]pyridine II which has excellent efficacy in animal models of gastric acid secretion following oral administration, as well as a good overall developability profile. The discovery strategy focuses on use of heteroaryl and heterocyclic substituents at the C-6 position and optimization of developability characteristics through modulation of global physico-chem. properties. In the experiment, the researchers used many compounds, for example, 2-(Bromomethyl)-1,3-dimethylbenzene (cas: 83902-02-7Category: bromides-buliding-blocks).

2-(Bromomethyl)-1,3-dimethylbenzene (cas: 83902-02-7) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

An Intermolecular Hydroarylation of Highly Deactivated Styrenes Catalyzed by Re₂O₇/HReO₄ in Hexafluoroisopropanol was written by Hu, Liqun;Liu, Yibing;Fang, Xiong;zheng, Yuzhu;Liao, Rong-zhen;Li, Man;Xie, Youwei. And the article was included in ACS Catalysis in 2022.Application In Synthesis of 2-Bromo-4-(trifluoromethyl)benzaldehyde This article mentions the following:

Here, authors describe an activation mode for unactivated alkenes on the basis of a synergy between Re₂O₇/HReO₄ and hexafluoroisopropanol (HFIP). Highly electron-deficient styrenes have been activated to effect a challenging intermol. hydroarylation with different arenes to give a variety of diarylalkanes in high efficiency. This method is characterized by mild reaction condition, broad substrate scope, high chem. yields, and minimal waste generation. The potential synthetic application of this methodol. was exemplified by the efficient synthesis of a retinoic acid receptor (RAR) agonist. DFT calculations and deuterium-labeling experiments were conducted to elucidate the reaction mechanism, and both confirmed the critical role of HFIP, which significantly reduced the energetical barriers for several key steps of this transformation via a network of hydrogen bonding to perrhenate anion with two equivalent of HFIP. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7Application In Synthesis of 2-Bromo-4-(trifluoromethyl)benzaldehyde).

2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Application In Synthesis of 2-Bromo-4-(trifluoromethyl)benzaldehyde

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis and biological evaluation of sulforaphane derivatives as potential antitumor agents was written by Hu, Kun;Qi, Yan-jie;Zhao, Juan;Jiang, He-fei;Chen, Xin;Ren, Jie. And the article was included in European Journal of Medicinal Chemistry in 2013.Safety of N-(5-Bromopentyl)phthalimide This article mentions the following:

A series of sulforaphane derivatives, S:C:NCH₂(CH₂)_nCH₂X(O)R [I, R = PhCH₂, Et, 2-furanylmethyl, cyclopentyl, etc., X = S(O), n = 1-4; R = PhCH₂, X = S, n = 2; R = PhCH₂, X = SO₂, n = 2], were synthesized and evaluated in vitro for their cytotoxicity against five cancer cell lines (HepG2, A549, MCF-7, HCT-116 and SH-SY5Y). The pharmacol. results showed that many of the derivatives displayed more potent cytotoxicity than sulforaphane (SFN). Furthermore, SFN and derivative I [R = PhCH₂, X = S(O), n = 2] (II) could induce cell cycle arrest at S or G2/M phase and cell apoptosis. SFN and II exhibited time- and dose-dependent activation on Nrf2 transcription factor, and II acted as a more potent Nrf2 inducer than SFN. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Safety of N-(5-Bromopentyl)phthalimide).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon鑱砨romine bond is electrophilic in nature. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Safety of N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents was written by Ding, Shi;Dai, Rui-Yang;Wang, Wen-Ke;Cao, Qiao;Lan, Le-Fu;Zhou, Xian-Li;Yang, Yu-She. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2018.Name: Methyl 4-bromo-2-fluorobenzoate This article mentions the following:

LpxC inhibitors are new-type antibacterial agents developed in the last twenty years, mainly against Gram-neg. bacteria infections. To develop novel LpxC inhibitors with good antibacterial activities and biol. metabolism, the authors summarized the basic skeleton of reported LpxC inhibitors, designed and synthesized several series of compounds and tested their antibacterial activities against Escherichia coli and Pseudomonas aeruginosa in vitro. Structure-activity relations are discussed. The metabolism stability of YDL-2, YDL-5, YDL-8, YDL-14, YDL-20-YDL-23 were evaluated in liver microsomes, which indicated that the 2-amino iso-Pr group may be a preferred structure than the 2-hydroxy Et group in the design of LpxC inhibitors. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2Name: Methyl 4-bromo-2-fluorobenzoate).

Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Name: Methyl 4-bromo-2-fluorobenzoate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On-Surface Debromination of 2,3-Bis(dibromomethyl)- and 2,3-Bis(bromomethyl)naphthalene: Dimerization or Polymerization? was written by Tang, Yanning;Ejlli, Barbara;Niu, Kaifeng;Li, Xuechao;Hao, Zhengming;Xu, Chaojie;Zhang, Haiming;Rominger, Frank;Freudenberg, Jan;Bunz, Uwe H. F.;Muellen, Klaus;Chi, Lifeng. And the article was included in Angewandte Chemie, International Edition in 2022.Electric Literature of C4H4BrNO2 This article mentions the following:

We describe the on-surface dehalogenative homocoupling of benzylic bromides, namely bis-bromomethyl- and bis-gem-(dibromomethyl) naphthalene as a potential route to either hydrocarbon dimers or conjugated polymers on Au(111). While bis-gem-(dibromomethyl) naphthalene affords different dimers with naphthocyclobutadiene as the key intermediate, bis-bromomethyl naphthalene furnishes a poly(o-naphthylene vinylidene) as a non-conjugated polymer which undergoes dehydrogenation toward its conjugated derivative poly(o-naphthylene vinylene) upon mild annealing. A combination of scanning tunneling microscopy, non-contact at. force microscopy and d. functional theory calculations provides deep insights into the prevailing mechanisms. In the experiment, the researchers used many compounds, for example, 1-Bromopyrrolidine-2,5-dione (cas: 128-08-5Electric Literature of C4H4BrNO2).

1-Bromopyrrolidine-2,5-dione (cas: 128-08-5) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon閳ユ彽romine bond is electrophilic, i.e. alkyl bromides are alkylating agents. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Electric Literature of C4H4BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Domino recombinant 绾?isomerization and reverse Wacker oxidation of 绾?vinyl-绾?butyrolactone: Synthesis of (+)-trans-, (-)- and (+)-disparlures was written by Bethi, Venkati;Kattanguru, Pullaiah;Fernandes, Rodney A.. And the article was included in European Journal of Organic Chemistry in 2014.Recommanded Product: Isopentyltriphenylphosphonium bromide This article mentions the following:

A domino Pd-catalyzed recombinant 绾?isomerization and reverse Wacker oxidation of 绾?vinyl-绾?butyrolactone was explored. The strategy was used in the stereoselective synthesis of (+)-trans-, (-)- and (+)-disparlure. The synthesis was achieved in 7-8 steps from D-glucono-鏈?lactone with overall yields of 19.3, 20.7, and 22.6%, resp. In the experiment, the researchers used many compounds, for example, Isopentyltriphenylphosphonium bromide (cas: 28322-40-9Recommanded Product: Isopentyltriphenylphosphonium bromide).

Isopentyltriphenylphosphonium bromide (cas: 28322-40-9) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Recommanded Product: Isopentyltriphenylphosphonium bromide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Systematic Investigation of Halogen Bonding in Protein-Ligand Interactions was written by Hardegger, Leo A.;Kuhn, Bernd;Spinnler, Beat;Anselm, Lilli;Ecabert, Robert;Stihle, Martine;Gsell, Bernard;Thoma, Ralf;Diez, Joachim;Benz, Joerg;Plancher, Jean-Marc;Hartmann, Guido;Banner, David W.;Haap, Wolfgang;Diederich, Francois. And the article was included in Angewandte Chemie, International Edition in 2011.Name: 1-(4-Bromo-2-fluorophenyl)cyclopropanecarboxylic acid This article mentions the following:

Halogen bonding triggers activity. Increasing binding affinity was observed for a series of covalent human Cathepsin L inhibitors by exchanging an aryl ring H atom with Cl, Br, and I, which undergo halogen bonding with the C=O group of Gly61 in the S3 pocket of the enzyme. Fluorine, in contrast, strongly avoids halogen bonding. The strong distance and angle dependence of halogen bonding was confirmed for biol. systems. In the experiment, the researchers used many compounds, for example, 1-(4-Bromo-2-fluorophenyl)cyclopropanecarboxylic acid (cas: 872422-15-6Name: 1-(4-Bromo-2-fluorophenyl)cyclopropanecarboxylic acid).

1-(4-Bromo-2-fluorophenyl)cyclopropanecarboxylic acid (cas: 872422-15-6) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Name: 1-(4-Bromo-2-fluorophenyl)cyclopropanecarboxylic acid

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary