Tag: 100-200

Development, synthesis, and biological evaluation of sulfonyl-α-L-amino acids as potential anti-Helicobacter pylori and IMPDH inhibitors was written by Galal, Alaaeldin M. F.;Mohamed, Hanaa S.;Abdel-Aziz, Marwa M.;Hanna, Atef G.. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2021.Application In Synthesis of 5-Chloro-2-methoxybenzoic acid This article mentions the following:

IMP dehydrogenase (IMPDH) catalyzes a crucial step in the biosynthesis of DNA and RNA, and it has been exploited as a promising target for antimicrobial therapy. The present study discusses the development and synthesis of a series of sulfonyl-α-L-amino acids coupled with the anisamide scaffold and evaluates their activities as anti-Helicobacter pylori and IMPDH inhibitors. Twenty derivatives were synthesized and their structures were established by high-resolution mass spectrometry and ¹H and ¹³C NMR measurements. Four compounds (I) (R¹ = L-Val, L-Leu, L-Ile, L-Trp) were found to be the most potent and selective mols. in the series with min. inhibitory concentration (MIC) values <17μM, which were selected to test their inhibitory activities against HpIMPDH and human (h)IMPDH2 enzymes. In all tests, amoxicillin and clarithromycin were used as reference drugs. Compounds I (R¹ = L-Val, L-Leu) were found to have a promising activity against the HpIMPDH enzyme, with IC₅₀ = 2.42 and 2.56μM, resp. Moreover, the four compounds were found to be less active and safer against hIMPDH2 than the reference drugs, with IC₅₀ > 17.17μM, which makes sure that their selectivity is toward HpIMPDH and reverse to that of amoxicillin and clarithromycin. Also, the synergistic antibacterial activity of compounds I (R¹ = L-Val, L-Leu) amoxicillin, and clarithromycin was investigated in vitro. The combination of amoxicillin/compound I (R¹ = L-Val) (2:1 by weight) exhibited a significant antibacterial activity against H. pylori, with MIC = 0.12μg/mL. The mol. docking study and ADMET anal. of the most active compounds were used to elucidate the mode-of-action mechanism. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2Application In Synthesis of 5-Chloro-2-methoxybenzoic acid).

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.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 5-Chloro-2-methoxybenzoic acid

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

Solid-Phase Synthesis of Chlorofusin Analogues was written by Woon, Esther C. Y.;Arcieri, Mariangela;Wilderspin, Andrew F.;Malkinson, John P.;Searcey, Mark. And the article was included in Journal of Organic Chemistry in 2007.Name: 5-Chloro-2-methoxybenzoic acid This article mentions the following:

The authors have efficiently synthesized two series of chlorofusin analogs, one bearing varying chromophores and the other with various amino acid substitutions in the cyclic peptide. These peptides were prepared via solid-phase methods using a strategy involving side-chain immobilization, on-resin cyclization, and postcyclization modification. The success of these syntheses demonstrates the broad utility of the method. Both series of analogs were evaluated for their inhibitory activity against the p53/MDM2 interaction but were shown to be inactive in the concentration range tested. This suggests that the full chromophore structure may be required for activity. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2Name: 5-Chloro-2-methoxybenzoic acid).

5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) 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. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Name: 5-Chloro-2-methoxybenzoic acid

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

Pd-catalyzed amidation of 1,3-diketones with CO and azides via a nitrene intermediate was written by Gu, Zheng-Yang;Chen, Jie;Xia, Ji-Bao. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2020.Reference of 3438-16-2 This article mentions the following:

An efficient Pd-catalyzed amidation of 1,3-diketones has been developed using carbon monoxide and organic azides. This reaction provides a step-economic approach to produce β-ketoamides from readily available compounds under mild ligand-, oxidant-, and base-free conditions. The mechanistic studies showed that the reaction occurred through an in situ generated isocyanate intermediate. 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. 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 readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Reference of 3438-16-2

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

Mannich reaction. N-[2-Hydroxy-3 (or 5 or 6)-substituted] benzyl glycines was written by Kumar, Kishan;Pandey, N. D.;Mehrotra, J. K.. And the article was included in Journal of the Indian Chemical Society in 1974.Recommanded Product: 3438-16-2 This article mentions the following:

Mannich reaction of glycine and HCHO with substituted phenols gave 35-65% I (R1 = H; R2, R3, R4 = H, Me, Cl, CO2H), which were methylated with Me2SO to give 50-96% of the corresponding I (R1 = Me). Thus, glycine, HCHO, and PhOH in NaOAc and HOAc gave 38.67% I (R1-R4 = H), which was methylated with Me2SO4 in NaOH at 80° to give 60.97% Me2SO4 (R1 = Me, R2-R4 =H). 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. 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.Recommanded Product: 3438-16-2

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

Kinetics of hydrolysis for esters with a variable alcoholic part. III. Alkaline hydrolysis of esters of p-nitrobenzoic acid in water was written by Babaeva, L. G.;Bogatkov, S. V.;Kruglikova, R. I.;Unkovskii, B. V.;Unkovskii, B. V.. And the article was included in Reaktsionnaya Sposobnost Organicheskikh Soedinenii in 1974.Related Products of 5335-05-7 This article mentions the following:

The saponification kinetics of p-O2NC6H4CO2R (R = PhCH2CH2, PhCH2, MeOCH2CH2, Me, ClCH2CH2, Ph, ClCH2) were determined at 25° in H2O. Correlation parameters for the dependence of the rate constants on the inductive and steric substituent constants of the alc. part of the mol. were determined The correlation parameters were independent of the acidic part of the esters. In the experiment, the researchers used many compounds, for example, Chloromethyl benzoate (cas: 5335-05-7Related Products of 5335-05-7).

Chloromethyl benzoate (cas: 5335-05-7) 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.Related Products of 5335-05-7

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

Nickel-catalyzed ortho-halogenation of unactivated (hetero)aryl C-H bonds with lithium halides using a removable auxiliary was written by Zhan, Bei-Bei;Liu, Yan-Hua;Hu, Fang;Shi, Bing-Feng. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2016.HPLC of Formula: 36157-41-2 This article mentions the following:

The first example of Ni-catalyzed halogenation of (hetero)aryl C-H bonds with lithium halides (LiX, X = Br, I, Cl) using PIP as a removable directing group was reported. This protocol provided an efficient access to ortho-halogenated (hetero)arenes with operational simplicity, good functional group tolerance and large-scale synthesis. In the experiment, the researchers used many compounds, for example, 2,5-Dichlorothiophene-3-carboxylic acid (cas: 36157-41-2HPLC of Formula: 36157-41-2).

2,5-Dichlorothiophene-3-carboxylic acid (cas: 36157-41-2) 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. 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.HPLC of Formula: 36157-41-2

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

Discovery, synthesis and anti-atherosclerotic activities of a novel selective sphingomyelin synthase 2 inhibitor was written by Li, Yali;Huang, Taomin;Lou, Bin;Ye, Deyong;Qi, Xiangyu;Li, Xiaoxia;Hu, Shuang;Ding, Tingbo;Chen, Yan;Cao, Yang;Mo, Mingguang;Dong, Jibin;Wei, Min;Chu, Yong;Li, Huiti;Jiang, Xian-Cheng;Cheng, Nengneng;Zhou, Lu. And the article was included in European Journal of Medicinal Chemistry in 2019.Reference of 3438-16-2 This article mentions the following:

The sphingomyelin synthase 2 (SMS2) is a potential target for pharmacol. intervention in atherosclerosis. However, so far, few selective SMS2 inhibitors and their pharmacol. activities were reported. In this study, a class of 2-benzyloxybenzamides were discovered as novel SMS2 inhibitors through scaffold hopping and structural optimization. Among them, Ly93 as one of the most potent inhibitors exhibited IC₅₀ values of 91 nM and 133.9 μM against purified SMS2 and SMS1 resp. The selectivity ratio of Ly93 was more than 1400-fold for purified SMS2 over SMS1. The in vitro studies indicated that Ly93 not only dose-dependently diminished apoB secretion from Huh7 cells, but also significantly reduced the SMS activity and increased cholesterol efflux from macrophages. Meanwhile, Ly93 inhibited the secretion of LPS-mediated pro-inflammatory cytokine and chemokine in macrophages. The pharmacokinetic profiles of Ly93 performed on C57BL/6J mice demonstrated that Ly93 was orally efficacious. As a potent selective SMS2 inhibitor, Ly93 significantly decreased the plasma SM levels of C57BL/6J mice. Furthermore, Ly93 was capable of dose-dependently attenuating the atherosclerotic lesions in the root and the entire aorta as well as macrophage content in lesions, in apolipoprotein E gene knockout mice treated with Ly93. In conclusion, we discovered a novel selective SMS2 inhibitor Ly93 and demonstrated its anti-atherosclerotic activities in vivo. The preliminary mol. mechanism-of-action studies revealed its function in lipid homeostasis and inflammation process, which indicated that the selective inhibition of SMS2 would be a promising treatment for atherosclerosis. 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. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Reference of 3438-16-2

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

Synthesis and Anti-Inflammatory Activities of Some New Substituted Benzocarboxamide Pyrimidine Derivatives Using N-(4-acetylphenyl)-5-chloro-2-methoxybenzamide as Starting Material was written by Hussain, Azza A.;Abdulla, Mohamed M.;Amr, Abd El-Galil;Al-Omar, Mohamed A.;Shalaby, Ahmed F. A.. And the article was included in Asian Journal of Chemistry in 2014.COA of Formula: C8H7ClO3 This article mentions the following:

A series of substituted pyrimidine derivatives I (X = NH, O, S; Y = H, 2-Cl, 4-Cl, 4-Br, 2-NO₂, 4-NO₂, 4-OCH₃) and II (Y = H, 2-Cl, 4-Cl, 4-Br, 2-NO₂, 4-NO₂, 4-OCH₃) were prepared from corresponding chalcones III (Y = H, 2-Cl, 4-Cl, 4-Br, 2-NO₂, 4-NO₂, 4-OCH₃), which were prepared from N-(4-acetylphenyl)-5-chloro-2-methoxybenzamide as starting material. The pharmacol. screening showed that many of these compounds have less toxicity and good anti-inflammatory activities. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2COA of Formula: C8H7ClO3).

5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) 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.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.COA of Formula: C8H7ClO3

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

Bi oxyiodogallate was written by Wierzchowski, J.. And the article was included in Pharmaceutical Journal in 1944.HPLC of Formula: 3438-16-2 This article mentions the following:

3,4-Dimethylgallic acid (I) and 3-methylgallic acid (II) are treated with BiOI. I does not react and II gives a new compound resembling Bi oxyiodogallate, which is thought to have the following formula: Its properties are reported. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2HPLC of Formula: 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.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.HPLC of Formula: 3438-16-2

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

Pd-catalyzed microwave irradiated regioselective aroylation reaction of crotyl- and allyltrifluoroborates was written by Al-Masum, Mohammad;Legan, Sarah;Liu, Kwei-Yu. And the article was included in International Journal of Organic Chemistry in 2016.SDS of cas: 1711-11-1 This article mentions the following:

An interesting regioselectivity is observed when the mixture of potassium crotyltrifluoroborate and aroyl chlorides RC(O)Cl (R = 3,4,6-trifluorophenyl, naphth-2-yl, 4-bromophenyl, etc.) having electron-deficient and electron-rich groups is microwaved in the presence of palladium-catalyst. In the case of electron withdrawing group with Ph ring of aroyl chlorides, isomerized α,β-unsaturated compound RC(O)CH(CH₃)=CHCH₃ is a product, whereas the electron donating group with Ph ring of aroyl chlorides furnishes α-adduct RC(O)CH(CH₃)CH=CH₂. Similar aroylation reaction is also established for potassium allyltrifluoroborate. In this case, regioselectivity is unaffected with changing electron-rich or electron-deficient groups in Ph ring of the aroyl chlorides. Reactions proceed with, essentially in same rate, to afford the corresponding aryl propenyl ketones (crotonophenones) RC(O)CH=CHCH₃ in good to high yields. In the experiment, the researchers used many compounds, for example, 3-Cyanobenzoyl chloride (cas: 1711-11-1SDS of cas: 1711-11-1).

3-Cyanobenzoyl chloride (cas: 1711-11-1) 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. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.SDS of cas: 1711-11-1

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