Month: February 2023

9-Sulfonyl-9(H)-Purine Derivatives Inhibit HCV Replication Via their Degradation Species was written by Hu, Rong;Wang, Wan-Li;Xiao, Kun-Jie;Wang, Ning-Yu. And the article was included in Pharmaceutical Chemistry Journal in 2021.Category: chlorides-buliding-blocks This article mentions the following:

Cell-based screening of a privileged small mol. library led to the discovery of 9-sulfonyl-9(H)-purine as new scaffold for hepatitis C virus (HCV) inhibitors. Structure-activity relationship study with respect to the 2-, 6- and 9-positions in the purine core resulted in the identification of several active compounds with moderate potency against the HCV genotype 1b. Subsequent stability studies demonstrated that HCV inhibitors of this type were unstable in Dulbecco’s modified eagle medium (DMEM) and plasma, as well as glutathione-containing water, and their instability was closely related to their HCV inhibitory activity. A preliminary study of the mechanism of action showed that the sulfonamide bond at the 9-position of purine would be the primary degradation site and the resulting sulfonylation degradation species would mediate the anti-HCV activity of 9-sulfonyl-9(H)-purines. Results of this study demonstrated that 9-sulfonyl-9(H)-purine is an unstable scaffold for HCV inhibitors and further detailed anal. of the degradation species is needed to determine the main active components and direct target for this type of mols. 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. 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. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Category: chlorides-buliding-blocks

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

Interaction between molecular aggregates placed into thin layered films was written by Pisklova, Polina V.;Ropakova, Iryna Yu.;Bespalova, Iryna I.;Yefimova, Svetlana L.;Sorokin, Alexander V.. And the article was included in Molecular Crystals and Liquid Crystals.Product Details of 101-20-2 This article mentions the following:

Interaction of J-aggregates of two carbocyanine dyes, TDBC and TCC, with similar structures has been studied in aqueous solutions and thin polymer films. It has been revealed that despite the structure similarity these J-aggregates didn鈥瞭 interact explicitly when mixed both in aqueous solutions and polycation thin films. However, by placing the J-aggregates in different layers separated by polycation film spacer, efficient energy transfer can be achieved with TDBC J-aggregates as an energy donor and TCC J-aggregates as energy acceptor. In the experiment, the researchers used many compounds, for example, 1-(4-Chlorophenyl)-3-(3,4-dichlorophenyl)urea (cas: 101-20-2Product Details of 101-20-2).

1-(4-Chlorophenyl)-3-(3,4-dichlorophenyl)urea (cas: 101-20-2) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. 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.Product Details of 101-20-2

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

NHC-Pd(II)-azole complexes catalyzed Suzuki-Miyaura cross-coupling of sterically hindered aryl chlorides with arylboronic acids was written by Zhang, Yingying;Zhang, Rong;Ni, Chang;Zhang, Xue;Li, Yanji;Lu, Qingwen;Zhao, Yuxuan;Han, Fangwai;Zeng, Yongfei;Liu, Guiyan. And the article was included in Tetrahedron Letters in 2020.Recommanded Product: 5-Bromo-2-chloro-m-xylene This article mentions the following:

In order to synthesize hindered biaryls RR¹ [R = 2-MeC₆H₄, 2,6-di-EtC₆H₃, 2-Me-4-FC₆H₃, etc.; R¹ = Ph, 2-MeC₆H₄, 2-FC₆H₄, etc.], a series of NHC-Pd(II)-azole complexes I [R² = H, Me; R³ = H, Me; X = C, N] were synthesized and characterized. The steric environment effect as well as electronic effect of azole ligands had been assessed. All these complexes I were applied in the Suzuki-Miyaura cross-coupling reaction of sterically hindered aryl chlorides with low catalysts loadings (0.1 mol %) under mild conditions in air and good to excellent isolated yields of sterically hindered biaryls were obtained. In the experiment, the researchers used many compounds, for example, 5-Bromo-2-chloro-m-xylene (cas: 206559-40-2Recommanded Product: 5-Bromo-2-chloro-m-xylene).

5-Bromo-2-chloro-m-xylene (cas: 206559-40-2) 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. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Recommanded Product: 5-Bromo-2-chloro-m-xylene

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

Discovery of hydrazone containing thiadiazoles as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors was written by Dogan, Hilal;Dogan, Sengul Dilem;Gunduz, Miyase Gozde;Krishna, Vagolu Siva;Lherbet, Christian;Sriram, Dharmarajan;Sahin, Onur;Saripinar, Emin. And the article was included in European Journal of Medicinal Chemistry in 2020.Related Products of 6590-96-1 This article mentions the following:

The rational design and synthesis of eighteen new thiadiazolylhydrazones I [R¹ = H, Me; R² = H, Cl; R³ = H, Me, NO₂, etc.] which were synthesized by intramol. oxidative N-S bond formation reaction of 2-benzylidene-N-(phenylcarbamothioyl)hydrazine-1-carboximidamide derivatives II by phenyliodine(III) bis(trifluoroacetate) (PIFA) under mild conditions were presented. Furthermore, the proposed structure of compounds I [R¹ = Me, R² = H, R³ = MeO] was resolved by single-crystal X-ray anal. The compounds I were evaluated for their in vitro antitubercular activity against M. tuberculosis H37Rv. Among them, some compounds I exhibited remarkable antimycobacterial activity, MIC = 0.78-6.25渭g/mL, with low cytotoxicity. Addnl., the most active compounds were screened for their biol. activities against M. tuberculosis in nutrient starvation model. Enzyme inhibition assays and mol. docking studies revealed enoyl acyl carrier protein reductase (InhA) as the possible target enzyme of compounds to show their antitubercular activities. In the experiment, the researchers used many compounds, for example, 2,4-Dichlorophenylisothiocyanate (cas: 6590-96-1Related Products of 6590-96-1).

2,4-Dichlorophenylisothiocyanate (cas: 6590-96-1) 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. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Related Products of 6590-96-1

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

Combination of probiotic yeast and lactic acid bacteria as starter culture to produce maize-based beverages was written by Menezes, Aline Galvao Tavares;Ramos, Cintia Lacerda;Dias, Disney Ribeiro;Schwan, Rosane Freitas. And the article was included in Food Research International in 2018.Category: chlorides-buliding-blocks This article mentions the following:

Cereal-based fermented beverages are non-dairy products which are considered possible carriers for probiotic strains and alternatives for use by vegans and lactose-intolerant consumers. In the present work, the com. probiotic, Lactobacillus paracasei LBC-81, was used singly and in co-culture with potential probiotic yeasts, Saccharomyces cerevisiae CCMA 0731, S. cerevisiae CCMA 0732, and Pichia kluyveri CCMA 0615, to ferment a maize-based substrate. All tested strains showed viability higher than 6 log CFU/mL, as recommended for food probiotic products, except for the yeast P. kluyveri which decreased during fermentation and storage time. A reduction in pH value, from approx. 7 to 4, was observed This decrease was due organic acid production, which did not affect the microbial viability. Lactic and acetic acids were the main organic acids produced during fermentation, and they decreased over 28 days of storage (<0.5 and 0.1 g/L for lactic and acetic acids, resp.). Ethanol was detected in the S. cerevisiae assays; however, the content was <5 g/L in a non-alc. beverage. Seventy volatile compounds were detected, including acids, alcs., aldehydes, esters, ketones, and other compounds Sensory anal. showed score of 5.93-4.57, resp. for appearance and taste. This is an important result, considering that the beverage had no flavoring additive and lacked a sweet taste. Therefore, probiotic beverages were successfully obtained by maize fermentation inoculated with co-culture of S. cerevisiae (CCMA 0731 or CCMA 0732) and L. paracasei LBC-81. In the experiment, the researchers used many compounds, for example, 1-Chlorooctadecane (cas: 3386-33-2Category: chlorides-buliding-blocks).

1-Chlorooctadecane (cas: 3386-33-2) 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.Category: chlorides-buliding-blocks

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

Esters of p-nitrophenol in synthesis of 1-N-monoamide and 1,7-bis-N,N’-amide derivatives of 1,4,7,10-tetraazacyclododecane was written by Skwierawska, A.. And the article was included in Polish Journal of Chemistry in 2006.Safety of 5-Chloro-2-methoxybenzoic acid This article mentions the following:

The efficient synthesis of N-monoamide and bis-N,N-amide-1,4,7,10-tetraazacyclododecanes is reported. Compounds thus prepared included 1-benzoyl-1,4,7,10-tetraazacyclododecane derivatives and 1-[(pyridinyl)carbonyl]-1,4,7,10-tetraazacyclododecane derivatives and analogs. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2Safety of 5-Chloro-2-methoxybenzoic acid).

5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) 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. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Safety of 5-Chloro-2-methoxybenzoic acid

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

The synthesis and antistaphylococcal activity of N-sulfonaminoethyloxime derivatives of dehydroabietic acid was written by Zhang, Wen-Ming;Yao, Yang;Yang, Teng;Wang, Xue-Ying;Zhu, Zhen-Yun;Xu, Wen-Tao;Lin, Hai-Xia;Gao, Zhao-Bing;Zhou, Hu;Yang, Cai-Guang;Cui, Yong-Mei. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2018.Computed Properties of C7H4ClF3O2S This article mentions the following:

A series of N-sulfonaminoethyloxime derivatives of dehydroabietic acid were synthesized and investigated for their antibacterial activity against Staphylococcus aureus Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108 and NRS-271). Most of the target compounds having chloro, bromo, trifluoromethyl Ph moiety exhibited potent in vitro antistaphylococcal activity. The meta-CF3 Ph derivative T23 showed the highest activity with MIC of 0.390.78 渭g/mL against S. aureus Newman, while several analogs showed similar potent antibacterial activity with MIC values between 0.78 and 1.56 渭g/mL against fve multidrug-resistant S. aureus. The stability of T35 in plasma of SD rat and the cellular cytotoxicity were also evaluated. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Computed Properties of C7H4ClF3O2S).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) 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. 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.Computed Properties of C7H4ClF3O2S

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

Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists was written by Xi, Qiumu;Wang, Mingjin;Jia, Wenqiang;Yang, Mingjian;Hu, Jinping;Jin, Jing;Chen, Xiaoguang;Yin, Dali;Wang, Xiaojian. And the article was included in Journal of Medicinal Chemistry in 2020.Product Details of 59237-53-5 This article mentions the following:

Stimulator of interferon genes (STING) is an endoplasmic reticulum-localized adaptor protein (STING receptor) that has been shown to be activated by binding to natural cyclic dinucleotide (CDN) ligands and plays a vital role in innate immune sensing of exogenous or endogenous DNA, which then induces type I interferons and other cytokines. In this paper, we described a series of amidobenzimidazole STING agonists with high potency for the STING receptor and presented the relevant structure-activity relationships (SARs). The relative potencies of compounds I, II, and III were measured by a STING competition binding assay. A more thorough study of the effect on the STING signaling pathway demonstrated that three compounds, I, II, and III, significantly increased the protein levels and mRNA levels of IFN-尾, CXCL10, and IL-6, and II as a representative compound effectively triggered the phosphorylation of STING, TBK1, and IRF3 in both human peripheral blood mononuclear cells (hPBMCs) and WT THP-1 cells. In addition, compound II demonstrated impressive antitumor efficacy in mice with established syngeneic colon tumors by i.v. administration. Furthermore, the pharmacokinetic profile of compound II was fully evaluated. In the experiment, the researchers used many compounds, for example, Methyl 6-chloro-5-nitronicotinate (cas: 59237-53-5Product Details of 59237-53-5).

Methyl 6-chloro-5-nitronicotinate (cas: 59237-53-5) 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. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Product Details of 59237-53-5

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

Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents was written by Gadekar, Pradip K.;Roychowdhury, Abhijit;Kharkar, Prashant S.;Khedkar, Vijay M.;Arkile, Manisha;Manek, Hardik;Sarkar, Dhiman;Sharma, Rajiv;Vijayakumar, V.;Sarveswari, S.. And the article was included in European Journal of Medicinal Chemistry in 2016.Application In Synthesis of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride This article mentions the following:

The design, synthesis and antimicrobial evaluation of a novel series of azaspiro analogs I [R = acetyl, 4-(trifluoromethyl)benzoyl, nicotinoyl, etc.] of linezolid were described. Linezolid comprises of a morpholine ring which was known for its metabolism-related liabilities. Therefore, the key modification made in the linezolid structure was the replacement of morpholine moiety with its bioisostere, 2-oxa-6-azaspiro[3.3]heptane. Furthermore, the replacement of N-acetyl terminal of linezolid with various aromatic or aliphatic functionalities was carried out. The title compounds were evaluated against a panel of Gram-pos. and Gram-neg. bacteria and Mycobacterium tuberculosis. Subsequent structure-activity relationship (SAR) studies identified several compounds with mixed antibacterial and antitubercular profiles. Compound I [R = isoxazole-5-carbonyl] (IC₅₀ 0.72, 0.51, 0.88, 0.49 渭g/mL for Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillussubtilis, resp.) exhibited similar antibacterial profile as linezolid. The N-acetyl derivative I [R = acetyl] was similar to linezolid in antitubercular profile. The use of azaspiro substructure in the medicinal chem. of antibacterial and antitubercular agents was demonstrated. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Application In Synthesis of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Application In Synthesis of 3-(Trifluoromethyl)benzene-1-sulfonyl chloride

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

Design, synthesis and biological activity of N-(amino)piperazine-containing benzothiazinones against Mycobacterium tuberculosis was written by Wang, Apeng;Xu, Shijie;Chai, Yun;Xia, Guimin;Wang, Bin;Lv, Kai;Ma, Chao;Wang, Dan;Wang, Aoyu;Qin, Xiaoyu;Liu, Mingliang;Lu, Yu. And the article was included in European Journal of Medicinal Chemistry in 2021.SDS of cas: 22227-59-4 This article mentions the following:

A series of novel benzothiazinone derivatives containing a N-(amino)piperazine moiety I (R₁ = H, Me, iso-Bu, etc.; R₂ = cyclohexyl, 4-(methoxyimino)cyclohexyl, 4-F₃CC₆H₄, etc.), II (R = cyclohexylmethyl, 4-trifluoromethoxybenzyl, cyclohexanecarbonyl, pyridin-4-ylmethyl) based on the structure of WAP-1902 discovered, were designed and synthesized as new anti-TB agents. Many of the compounds exhibited excellent in vitro activity against both drug-sensitive MTB strain H37Rv and multidrug-resistant clin. isolates (MIC: < 0.016渭g/mL), and good safety index (CC₅₀: >64渭g/mL). Especially compound I (R₁ = Me; R₂ = 4-(methoxyimino)cyclohexyl) displayed low hERG cardiac toxicity and acceptable oral pharmacokinetic profiles, indicating its promising potential to be a lead compound for future antitubercular drug discovery. In the experiment, the researchers used many compounds, for example, 2-Chloro-3-nitro-5-(trifluoromethyl)benzoic acid (cas: 22227-59-4SDS of cas: 22227-59-4).

2-Chloro-3-nitro-5-(trifluoromethyl)benzoic acid (cas: 22227-59-4) 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. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.SDS of cas: 22227-59-4

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