Tag: 100-200

Benzimidazole-based compounds kill Mycobacterium tuberculosis was written by Gong, Yaling;Somersan Karakaya, Selin;Guo, Xiaoyong;Zheng, Purong;Gold, Ben;Ma, Yao;Little, David;Roberts, Julia;Warrier, Thulasi;Jiang, Xiuju;Pingle, Maneesh;Nathan, Carl F.;Liu, Gang. And the article was included in European Journal of Medicinal Chemistry in 2014.Safety of 3-Cyanobenzoyl chloride This article mentions the following:

Tuberculosis remains one of the deadliest infectious diseases, killing 1.4 million people annually and showing a rapid increase in cases resistant to multiple drugs. New antibiotics against tuberculosis are urgently needed. Here the authors describe the design, synthesis and structure-activity relationships of a series of benzimidazole-based compounds, e.g. I [R¹ = Me, cyclobutyl, t-Bu, etc.; R² = morpholin-4-yl, thiomorpholin-4-yl; R³ = H, Me] with activity against Mycobacterium tuberculosis in a replicating state, a physiol.-induced nonreplicating state, or both. Several compounds, which shared a 5-nitrofuranyl moiety, exhibited high potency and acceptable selectivity indexes (SI). As illustrated by compound I [R¹ = isopentyl, R² = morpholin-4-yl, R³ = Me] (MIC₉₀ < 0.049 渭g/mL, SI > 512), the 5-nitrofuranyl group was compatible with minimal cytotoxicity and good intramacrophage killing, although it lacked nonreplicating activity when assessed by CFU assays. Compound I [R¹ = isopentyl, R² = morpholin-4-yl, R³ = Me] had low mutagenic potential by SOS Chromotest assay, making this class of compounds good candidates for further evaluation and target identification. In the experiment, the researchers used many compounds, for example, 3-Cyanobenzoyl chloride (cas: 1711-11-1Safety of 3-Cyanobenzoyl chloride).

3-Cyanobenzoyl chloride (cas: 1711-11-1) 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. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Safety of 3-Cyanobenzoyl chloride

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

Synthesis and some reactions of 2-acylcyclopentane-1,3-diones was written by Lakhvich, F. A.;Khlebnikova, T. S.;Akhrem, A. A.. And the article was included in Zhurnal Organicheskoi Khimii in 1989.Application In Synthesis of 2-(3-Methoxyphenyl)acetyl chloride This article mentions the following:

Acyloxycyclopentenones I [R = Me, hexyl, heptyl, PhCH₂, Ph, (CH₂)_nCO₂Et (n = 4-6)] were prepared in 88-97% yields by acylation of cyclopentanedione as its enol by RCOCl. Treating I with AlCl₃ in CH₂Cl₂ 3 h at -5 to 20掳 gave 68-96% acylcyclopentanediones II. Treating II [R = (CH₂)₄CO₂Et] with NH₂OH.HCl gave 86% oxime III which underwent Beckmann rearrangement to give 61% adipamic acid derivative IV. In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0Application In Synthesis of 2-(3-Methoxyphenyl)acetyl chloride).

2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) 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.Application In Synthesis of 2-(3-Methoxyphenyl)acetyl chloride

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

Reactivity of functionalized arylcarbenes. 2-Phenylethyl side chains and hetero analogs was written by Kirmse, Wolfgang;Konrad, Wolfgang;Ozkir, Ismail S.. And the article was included in Tetrahedron in 1997.SDS of cas: 7476-66-6 This article mentions the following:

Phenylcarbenes with -X-CH₂Ph and -CH₂X-Ph (X = CH₂, O, SiMe₂) groups in the ortho position were generated thermally and photolytically from diazo or tosylhydrazone precursors. Stereorandom insertion reactions with 尾-C-H bonds were observed, pointing to a triplet abstraction-recombination mechanism. Large kinetic and stereochem. deuterium isotope effects support this notion. The ample formation of benzocyclobutenes from 2-CH₂-X-Ph substrates is due to insertion of the carbenes into ArCH₂-X bonds. Addition to the terminal Ph groups competes with C-H and C-X insertion. The results of benzophenone sensitization and of trapping with methanol suggest that the intramol. reactions of functionalized arylcarbenes proceed, at best, competitively with spin inversion. In the experiment, the researchers used many compounds, for example, Methyl 2-chloro-2-phenylacetate (cas: 7476-66-6SDS of cas: 7476-66-6).

Methyl 2-chloro-2-phenylacetate (cas: 7476-66-6) 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.SDS of cas: 7476-66-6

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

Synthesis and Evaluation of 5-(o-Tolyl)-1H-tetrazole Derivatives as Potent Anticonvulsant Agents was written by Dong, Shiyang;Wang, Tiantian;Wang, Huayu;Qian, Kun;Zhang, Zhongli;Zuo, Yueming;Luo, Guangming;Jin, Yi;Wang, Zengtao. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2017.Quality Control of 2-(Chloromethyl)-1,3-difluorobenzene This article mentions the following:

A series of 5-(o-tolyl)-1H-tetrazole derivatives were synthesized and evaluated for their anticonvulsant activities. 1-(2-Methylbenzyl)-5-(o-tolyl)-1H-tetrazole (3h) showed important anticonvulsant activity against the MES-induced seizures, as well as lower neurotoxicity with an ED₅₀ value of 12.7 mg/kg and a TD₅₀ value of over 500 mg/kg after i.p. injection into mice, providing 3h with a high protective index (TD₅₀/ED₅₀) of over 39.4. The achieved results prove that the distinctive compounds could be valuable as a model for future development, adaptation, and investigation to construct more active analogs. In the experiment, the researchers used many compounds, for example, 2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4Quality Control of 2-(Chloromethyl)-1,3-difluorobenzene).

2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4) 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 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.Quality Control of 2-(Chloromethyl)-1,3-difluorobenzene

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

Preparation of 2,6-difluoro-n-alkylbenzenes from 1,3-difluorobenzene. Transformation of 2,6-difluorotoluene to the corresponding benzaldehyde via benzyl chloride was written by Malykhin, Evghenii V.;Shteingarts, Vitalii D.. And the article was included in Journal of Fluorine Chemistry in 1998.SDS of cas: 697-73-4 This article mentions the following:

Reactions of n-alkyl chlorides with the 2,6-difluorophenyl anion, prepared from 1,3-difluorobenzene by the action of sodium amide in liquid ammonia, give 2,6-difluoro-n-alkylbenzenes in high yields. 2,6-Difluorotoluene reacts with chlorine at 80掳 to give 2,6-difluorobenzyl chloride in 92% yield. 2,6-Difluorobenzaldehyde has been obtained from this chloride through Sommelet’s reaction in 62% yield. In the experiment, the researchers used many compounds, for example, 2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4SDS of cas: 697-73-4).

2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4) 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. 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.SDS of cas: 697-73-4

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

Structure-activity evaluation of new uracil-based non-nucleoside inhibitors of HIV reverse transcriptase was written by Matyugina, Elena S.;Valuev-Elliston, Vladimir T.;Geisman, Alexander N.;Novikov, Mikhail S.;Chizhov, Alexander O.;Kochetkov, Sergey N.;Seley-Radtke, Katherine L.;Khandazhinskaya, Anastasia L.. And the article was included in MedChemComm in 2013.Reference of 1711-11-1 This article mentions the following:

A new series of potential nonnucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs) based on the carbocyclic 5′-nor-uracil scaffold were designed and synthesized. Three different aspects of the scaffold were investigated: the effects of adding a linker between the carbocyclic and Ph fragments, introduction of different substituents on the benzoyl residue and replacing the central carbocyclic ring with a benzyl group. Analogs of 2′,3′-dideoxy-2′,3′-didehydro-5′-nor-uridine, bearing 3,5-dichloro- or 3,5-dimethylbenzoyl groups, showed inhibitory activity against HIV-RT wild-type (IC₅₀ 5-10 渭M) and mutants L100I (IC₅₀ 1.2-2.1 渭M) and K103N (IC₅₀ 8-17 渭M). In the experiment, the researchers used many compounds, for example, 3-Cyanobenzoyl chloride (cas: 1711-11-1Reference of 1711-11-1).

3-Cyanobenzoyl chloride (cas: 1711-11-1) 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. 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 1711-11-1

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

Synthesis and antimicrobial evaluation of nitazoxanide-based analogs: Identification of selective and broad spectrum activity was written by Ballard, T. Eric;Wang, Xia;Olekhnovich, Igor;Koerner, Taylor;Seymour, Craig;Salamoun, Joseph;Warthan, Michelle;Hoffman, Paul S.;MacDonald, Timothy L.. And the article was included in ChemMedChem in 2011.Name: 3-Cyanobenzoyl chloride This article mentions the following:

A library composed of nitazoxanide-based analogs was synthesized and assayed for increased antibacterial efficacy against the pyruvate-ferredoxin oxidoreductase (PFOR) using microorganisms Helicobacter pylori, Campylobacter jejuni and Clostridium difficile. Derivatives were found to recapitulate and improve activity against these organism,s and select analogs were tested for their ability to disrupt the PFOR enzyme directly. The library was also screened for activity against staphylococci and resulted in the identification of analogs capable of inhibiting both staphylococci and all PFOR organisms at low micromolar min. inhibitory concentrations with low toxicity to human foreskin cells. In the experiment, the researchers used many compounds, for example, 3-Cyanobenzoyl chloride (cas: 1711-11-1Name: 3-Cyanobenzoyl chloride).

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.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.Name: 3-Cyanobenzoyl chloride

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

Synthesis and in vitro antimicrobial evaluation of new 1,3,4-oxadiazoles bearing 5-chloro-2-methoxyphenyl moiety was written by Basavapatna, N. Prasanna Kumar;Kikkeri, N. Mohana;Lingappa, Mallesha;Kikkeri, P. Harish. And the article was included in International Journal of Medicinal Chemistry in 2013.Electric Literature of C8H7ClO3 This article mentions the following:

A series of new 1,3,4-oxadiazole derivatives containing 5-chloro-2-methoxy benzohydrazide moiety were synthesized by the reaction of 5-chloro-2-methoxybenzoate with different aromatic carboxylic acids. These newly synthesized compounds were characterized by FT-IR, ¹H NMR, mass spectra and also by elemental anal. All the newly synthesized compounds were screened for their antibacterial and antifungal activities. Antimicrobial studies revealed that some of the compounds showed significant activity against tested strains. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2Electric Literature of C8H7ClO3).

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.Electric Literature of C8H7ClO3

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

Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2 was written by Moustakim, Moses;Riedel, Kerstin;Schuller, Marion;Gehring, Andre P.;Monteiro, Octovia P.;Martin, Sarah P.;Fedorov, Oleg;Heer, Jag;Dixon, Darren J.;Elkins, Jonathan M.;Knapp, Stefan;Bracher, Franz;Brennan, Paul E.. And the article was included in Bioorganic & Medicinal Chemistry in 2018.Category: chlorides-buliding-blocks This article mentions the following:

The polyadenosine-diphosphate-ribose polymerase 14 (PARP14) has been implicated in DNA damage response pathways for homologous recombination. PARP14 contains three (ADP ribose binding) macrodomains (MD) whose exact contribution to overall PARP14 function in pathol. remains unclear. A medium throughput screen led to the identification of N-(2(-9H-carbazol-1-yl)phenyl)acetamide (GeA-69, 1) as a novel allosteric PARP14 MD2 (second MD of PARP14) inhibitor. We herein report medicinal chem. around this novel chemotype to afford a sub-micromolar PARP14 MD2 inhibitor. This chem. series provides a novel starting point for further development of PARP14 chem. probes. In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0Category: chlorides-buliding-blocks).

2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) 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. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Category: chlorides-buliding-blocks

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

An approach to 1-alkyl-3-phenylpiperidine derivatives containing 2,5-functionalized groups: 1-methyl-2-(4-chlorophenylthiomethyl)-3-(3-methoxyphenyl)-5-(methoxycarbonyl)piperidine was written by Kotzamani, Heleni K.;Gourdoupis, Christos G.;Stamos, Ioannis K.. And the article was included in Tetrahedron in 1994.Reference of 6834-42-0 This article mentions the following:

3-MeOC₆H₄CH₂COCH₂SC₆H₄Cl-4 (I) was synthesized by regiospecific addition of 4-chlorothiophenol to diazoketone 3-MeOC₆H₄CH₂COCHN₂ in the presence of a rhodium(II) acetate catalyst. Annulation of I with the enamine prepared from MeNH₂ and CH₂:C(CH₂Br)CO₂Me gave a tetrahydropyridine derivative Reduction of this compound with sodium cyanoborohydride in the presence of carboxylic acid produced the title compound In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0Reference of 6834-42-0).

2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) 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 6834-42-0

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