Month: February 2023

Enhancement of Antibiotic Activity by 1,8-Naphthyridine Derivatives against Multi-Resistant Bacterial Strains was written by Araujo-Neto, Jose B. de;Silva, Maria M. C. da;Oliveira-Tintino, Cicera D. de M.;Begnini, Ieda M.;Rebelo, Ricardo A.;Silva, Luiz E. da;Mireski, Sandro L.;Nasato, Michele C.;Krautler, Maria I. L.;Ribeiro-Filho, Jaime;Siyadatpanah, Abolghasem;Wilairatana, Polrat;Coutinho, Henrique D. M.;Tintino, Saulo R.. And the article was included in Molecules in 2021.Category: chlorides-buliding-blocks This article mentions the following:

The purpose of this study was to evaluate the antibacterial and antibiotic-modulating activities of 1,8-naphthyridine derivatives against multi-resistant bacterial strains. The broth microdilution method was used to determine the min. inhibitory concentration (MIC) of the following compounds: 7-acetamido-1,8-naphthyridin-4(1H)-one and 3-trifluoromethyl-N-(5-chloro-1,8-naphthyridin-2-yl)-benzenesulfonamide. The antibiotic-modulating activity was analyzed using subinhibitory concentrations (MIC/8) of these compounds in combination with norfloxacin, ofloxacin, and lomefloxacin. Multi-resistant strains of Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus were used in both tests. Although the compounds had no direct antibacterial activity (MIC 鈮?1.024渭g/mL), they decreased the MIC of these fluoroquinolones, indicating synergism was obtained from the association of the compounds These results suggested the existence of a structure-activity relationship in this group of compounds with regard to the modulation of antibiotic activity. Therefore, concluded that 1,8-naphthyridine derivatives potentiate the activity of fluoroquinolone antibiotics against multi-resistant bacterial strains, and thereby interesting candidates for the development of drugs against bacterial infections caused by multidrug resistant strains. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Category: chlorides-buliding-blocks).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Category: chlorides-buliding-blocks

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Tuning Side Arm Electronics in Unsymmetrical Cyclotriazadisulfonamide (CADA) Endoplasmic Reticulum (ER) Translocation Inhibitors to Improve their Human Cluster of Differentiation 4 (CD4) Receptor Down-Modulating Potencies was written by Chawla, Reena;Van Puyenbroeck, Victor;Pflug, Nicholas C.;Sama, Alekhya;Ali, Rameez;Schols, Dominique;Vermeire, Kurt;Bell, Thomas W.. And the article was included in Journal of Medicinal Chemistry in 2016.Application In Synthesis of 4-Butoxybenzene-1-sulfonyl chloride This article mentions the following:

Cyclotriazadisulfonamide prevents HIV entry into cells by down-modulating surface CD4 receptor expression through binding to the CD4 signal peptide. According to a two-site binding model, 28 new unsym. analogs bearing a benzyl tail group and nine bearing a cyclohexylmethyl tail have been designed and synthesized. The most potent new CD4 down-modulator (40 (CK147); IC₅₀ 63 nM) has a 4-dimethylaminobenzenesulfonyl side arm. One of the two side arms was varied with substituents in different positions. This gave a range of CD4 down-modulation potencies that correlated well with anti-HIV-1 activities. The side arms of 21 of the new benzyl-tailed analogs were modeled by means of quantum mech. calculations For CADA analogs with arenesulfonamide side arms, the pIC₅₀ values for CD4 down-modulation correlated with the component of the elec. dipole moment in the aromatic ring, suggesting that an attractive electronic interaction is a major factor determining the stability of the complex between the mol. and its target. In the experiment, the researchers used many compounds, for example, 4-Butoxybenzene-1-sulfonyl chloride (cas: 1138-56-3Application In Synthesis of 4-Butoxybenzene-1-sulfonyl chloride).

4-Butoxybenzene-1-sulfonyl chloride (cas: 1138-56-3) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Application In Synthesis of 4-Butoxybenzene-1-sulfonyl chloride

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Development of high-affinity 5-HT₃ receptor antagonists. 1. Initial structure-activity relationship of novel benzamides was written by Youssefyeh, R. D.;Campbell, H. F.;Klein, S.;Airey, J. E.;Darkes, P.;Powers, M.;Schnapper, M.;Neuenschwander, K.;Fitzpatrick, L. R.. And the article was included in Journal of Medicinal Chemistry in 1992.Recommanded Product: 3438-16-2 This article mentions the following:

Novel benzamides, e.g. I (X = H, Cl, Br, n = 1; X = Cl, n = 2), II (R = Me, Me₂CHCH₂, CH₂:CHCHMe, MeCOCHMe), and S–III which are orally active, highly potent, specific antagonists of serotonin 5-HT₃ receptors were prepared and the structure-activity relationships that led to these novel structures with improved potency in selectivity are described. (S)-III was identified and selected for further evaluation as a 5-HT₃ receptor antagonist. Compared with 5-HT₃ antagonists such as GR 38032F, BRL 43694, and metoclopramide, (S)-III was most active in (a) inhibiting binding to 5-HT₃ receptor binding sites in rat entorhinal cortex with a K_i value of 0.19 nM and (b) blocking cisplatin-induced emesis in the ferret with an ED₅₀ value determined to be 9 mg/kg, i.d. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2Recommanded Product: 3438-16-2).

5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Recommanded Product: 3438-16-2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

An improved method for the synthesis of phenylacetic acid derivatives via carbonylation was written by Li, He;Zhang, Yijun;Liu, Dinghua;Liu, Xiaoqin. And the article was included in Journal of Chemical Research in 2019.Computed Properties of C8H9Cl This article mentions the following:

A series of phenylacetic acid derivatives RCH₂CO₂H [R = 2-ClC₆H₄, 4-MeC₆H₄, 2,4-Cl₂C₆H₃, etc.] was synthesized via bistriphenylphosphine palladium dichloride catalyzed carbonylation reaction of benzyl chloride derivatives in presence of tetraethylammonium chloride and sodium hydroxide as reagents and xylene as solvent at 80掳C under a CO atm. 2,4-Dichlorophenylacetic acid was obtained in a maximum yield of 95% from 2,4-dichlorobenzyl chloride using the same reaction system. In the experiment, the researchers used many compounds, for example, 1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9Computed Properties of C8H9Cl).

1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Computed Properties of C8H9Cl

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

N-Arylsulfonyl Indolines as Retinoic Acid Receptor-Related Orphan Receptor 纬 (ROR纬) Agonists was written by Doebelin, Christelle;Patouret, Remi;Garcia-Ordonez, Ruben D.;Chang, Mi Ra;Dharmarajan, Venkatasubramanian;Kuruvilla, Dana S.;Novick, Scott J.;Lin, Li;Cameron, Michael D.;Griffin, Patrick R.;Kamenecka, Theodore M.. And the article was included in ChemMedChem in 2016.Related Products of 777-44-6 This article mentions the following:

The nuclear retinoic acid receptor-related orphan receptor 纬 (ROR纬; NR1F3) is a key regulator of inflammatory gene programs involved in T helper 17 (T_H17) cell proliferation. As such, synthetic small-mol. repressors (inverse agonists) targeting ROR纬 have been extensively studied for their potential as therapeutic agents for various autoimmune diseases. Alternatively, enhancing T_H17 cell proliferation through activation (agonism) of ROR纬 may boost an immune response, thereby offering a potentially new approach in cancer immunotherapy. Herein the authors describe the development of N-arylsulfonyl indolines as ROR纬 agonists. Structure-activity studies reveal a critical linker region in these mols. as the major determinant for agonism. Hydrogen/deuterium exchange coupled to mass spectrometry (HDX-MS) anal. of ROR纬-ligand complexes help rationalize the observed results. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Related Products of 777-44-6).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Related Products of 777-44-6

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Design and Synthesis of Fsp³-Rich, Bis-Spirocyclic-Based Compound Libraries for Biological Screening was written by Stotani, Silvia;Lorenz, Christoph;Winkler, Matthias;Medda, Federico;Picazo, Edwige;Ortega Martinez, Raquel;Karawajczyk, Anna;Sanchez-Quesada, Jorge;Giordanetto, Fabrizio. And the article was included in ACS Combinatorial Science in 2016.Electric Literature of C8H9ClO4S This article mentions the following:

The exploration of innovative chem. space is a critical step in the early phases of drug discovery. Bis-spirocyclic frameworks occur in natural products and other biol. relevant metabolites and show attractive features, such as mol. compactness, structural complexity, and three-dimensional character. A concise approach to the synthesis of bis-spirocyclic-based compound libraries starting from readily available com. reagents and robust chem. transformations has been developed. A number of novel bis-spirocyclic scaffold examples, as implemented in the European Lead Factory project, is presented. In the experiment, the researchers used many compounds, for example, 2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2Electric Literature of C8H9ClO4S).

2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Electric Literature of C8H9ClO4S

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

An integrated screening strategy for novel AhR agonist candidate identification and toxicity confirmation in sediments was written by Xie, Ruili;Xu, Yiping;Ma, Mei;Wang, Zijian. And the article was included in Science of the Total Environment in 2022.Recommanded Product: 101-20-2 This article mentions the following:

Organic contaminants showing aryl hydrocarbon receptor (AhR) agonist activity are commonly detected in areas disturbed by intense human activities and they can initiate a variety of biochem., physiol., and toxicol. effects. A new integrated screening strategy for AhR agonist candidate identification and toxicity confirmation was developed to characterize the AhR-active pollutants in sediments of the contaminated Daqing River basin (DRB) in North China. The specific objectives were to (i) determine the concentrations of known AhR agonists, (ii) identify the novel AhR agonist candidates from nontarget screening (NTS) with structure alerts, computational toxicol. (CompTox) Dashboard bioassays, and in silico predictions, and (iii) evaluate contributions of AhR agonists to the overall potencies and characterize the distribution and source of these pollutants. Significant AhR-mediated potencies were observed in all sediment extracts by in vitro bioassays. Concentrations of polar target chems. in sediment extracts were much lower than nonpolar target chems. A total of 19 known AhR agonists explained 11.3 % to 49.1 % of bioassay-derived AhR-mediated potencies and polychlorinated biphenyls (PCB) 126 and PCB169 were found to contribute significantly to the total effects. 21 compounds screened from NTS by AhR-related structure alerts and further confirmed toxicity by high-throughput bioassays and in silico predictions were selected as AhR agonist candidates. Most of them were substituted PAHs, biphenyls, quinones, substituted phenols and heterocyclic compounds, and they primarily originated from nearby manufacturing industries. Of these compounds, 1-methy-pyrene exhibited significant AhR-mediated potency. Follow up studies should focus on toxicol. mechanism, source, and fate of these novel AhR agonists in water environment. In the experiment, the researchers used many compounds, for example, 1-(4-Chlorophenyl)-3-(3,4-dichlorophenyl)urea (cas: 101-20-2Recommanded Product: 101-20-2).

1-(4-Chlorophenyl)-3-(3,4-dichlorophenyl)urea (cas: 101-20-2) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Recommanded Product: 101-20-2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Synthesis, characterization and thermal decomposition mechanism of rare earth complexes with 5-chloro-2-methoxybenzoic acid and 1,10-phenanthroline was written by Zhang, Jie;Wang, Juan-Fen;Zhang, Jian-Jun. And the article was included in Wuli Huaxue Xuebao in 2012.Reference of 3438-16-2 This article mentions the following:

Three rare earth complexes of [Ln(5-Cl-2MOBA)₃phen]₂ (Ln = Nd(1), Eu(2), Ho(3); 5-Cl-2MOBA: 5-chloro-2-methoxybenzoate; phen: 1,10-phenanthroline) were synthesized and characterized by elemental anal., TG-differential TG-DSC (TG-DTG-DSC), IR spectra, UV spectra, and molar conductance techniques. The fluorescence spectra showed that complex 2 emitted a characteristic fluorescence of the Eu³⁺ ions. The thermal properties are discussed by TG – DSC / FTIR (TG-DSC/FTIR) techniques. And the three-dimensional IR accumulation spectra for the three complexes were also analyzed. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2Reference of 3438-16-2).

5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Reference of 3438-16-2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors: Optimization of Whole-Cell Anticryptococcal Activity and Insights into the Structural Origins of Cryptococcal Selectivity was written by Marcyk, Paul T.;LeBlanc, Emmanuelle V.;Kuntz, Douglas A.;Xue, Alice;Ortiz, Francisco;Trilles, Richard;Bengtson, Stephen;Kenney, Tristan M. G.;Huang, David S.;Robbins, Nicole;Williams, Noelle S.;Krysan, Damian J.;Prive, Gilbert G.;Whitesell, Luke;Cowen, Leah E.;Brown, Lauren E.. And the article was included in Journal of Medicinal Chemistry in 2021.Synthetic Route of C8H6ClFO2 This article mentions the following:

The essential eukaryotic chaperone Hsp90 regulates the form and function of diverse client proteins, many of which govern thermotolerance, virulence, and drug resistance in fungal species. However, use of Hsp90 inhibitors as antifungal therapeutics has been precluded by human host toxicities and suppression of immune responses. We recently described resorcylate aminopyrazoles (RAPs) as the first class of Hsp90 inhibitors capable of discriminating between fungal (Cryptococcus neoformans, Candida albicans) and human isoforms of Hsp90 in biochem. assays. Here, we report an iterative structure-property optimization toward RAPs capable of inhibiting C. neoformans growth in culture. In addition, we report the first X-ray crystal structures of C. neoformans Hsp90 nucleotide binding domain (NBD), as the apoprotein and in complexes with the non-species-selective Hsp90 inhibitor NVP-AUY922 and three RAPs revealing unique ligand-induced conformational rearrangements, which reaffirm the hypothesis that intrinsic differences in protein flexibility can confer selective inhibition of fungal vs. human Hsp90 isoforms. In the experiment, the researchers used many compounds, for example, Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3Synthetic Route of C8H6ClFO2).

Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.Synthetic Route of C8H6ClFO2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Direct synthesis of thiophosphates by reaction of diphenylphosphine oxide with sulfonyl chlorides was written by He, Wei;Wang, Zhiming;Li, Xinjin;Yu, Qing;Wang, Zhongwei. And the article was included in Tetrahedron in 2016.Electric Literature of C8H9ClO4S This article mentions the following:

A new method for the synthesis of thiophosphates by reductive coupling reaction of diphenylphosphine oxide and sulfonyl chlorides has been developed. The reaction is metal-free and needs no additives, affording various aryl and alkyl substituted thiophosphates in good to excellent yields under mild conditions. In the experiment, the researchers used many compounds, for example, 2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2Electric Literature of C8H9ClO4S).

2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Electric Literature of C8H9ClO4S

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics