Tag: 200-300

Design, synthesis, and pharmacological evaluation of multitarget-directed ligands with both serotonergic subtype 4 receptor (5-HT₄R) partial agonist and 5-HT₆R antagonist activities, as potential treatment of Alzheimer’s disease was written by Yahiaoui, Samir;Hamidouche, Katia;Ballandonne, Celine;Davis, Audrey;Santos, Jana Sopkova de Oliveira;Freret, Thomas;Boulouard, Michel;Rochais, Christophe;Dallemagne, Patrick. And the article was included in European Journal of Medicinal Chemistry in 2016.Recommanded Product: 2,4-Dimethoxybenzene-1-sulfonyl chloride This article mentions the following:

Seventeen novel derivatives of RS67333 (1) were synthesized and evaluated as potential dual-target compounds Among them, four agents showed nanomolar and submicromolar affinities toward 5-HT₄R and 5-HT₆R, resp.; one of them, 4-Amino-N-(2-(4-(3-(4-amino-5-chloro-2-methoxyphenyl)3-oxopropyl)piperidin-1-yl) ethyl)-3-bromobenzenesulfonamide, was selected on the basis of its in-vitro affinity (K_i5-HT4R = 5.3 nM, K_i5-HT6R = 219 nM) for further in-vivo experiments, where it also showed an antiamnesic effect in the mouse at 1 mg/kg i.p. In the experiment, the researchers used many compounds, for example, 2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2Recommanded Product: 2,4-Dimethoxybenzene-1-sulfonyl chloride).

2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2) 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. 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).Recommanded Product: 2,4-Dimethoxybenzene-1-sulfonyl chloride

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

Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties was written by Oost, Thorsten;Backfisch, Gisela;Bhowmik, Swati;van Gaalen, Marcel M.;Geneste, Herve;Hornberger, Wilfried;Lubisch, Wilfried;Netz, Astrid;Unger, Liliane;Wernet, Wolfgang. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Computed Properties of C8H9ClO4S This article mentions the following:

Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-di-Me amide moiety as an oxazole and attaching a benzylic amine moiety to the northern Ph ring resulted in potent and selective V1b receptor antagonists with improved metabolic stability and improved pharmacokinetic properties in rat. Compound 18c (I) was found to be efficacious in a rat model of anti-depressant activity. In the experiment, the researchers used many compounds, for example, 2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2Computed Properties of C8H9ClO4S).

2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2) 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. 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).Computed Properties of C8H9ClO4S

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

Design, Synthesis, and Biological Evaluation of Tetrahydro-β-carboline Derivatives as Selective Sub-Nanomolar Gelatinase Inhibitors was written by Mangiatordi, Giuseppe Felice;Guzzo, Tatiana;Rossano, Eugenio Claudio;Trisciuzzi, Daniela;Alberga, Domenico;Fasciglione, Giovanni;Coletta, Massimiliano;Topai, Alessandra;Nicolotti, Orazio. And the article was included in ChemMedChem in 2018.Name: 4-Butoxybenzene-1-sulfonyl chloride This article mentions the following:

Targeting matrix metalloproteinases (MMPs) is a pursued strategy for treating several pathol. conditions, such as multiple sclerosis and cancer. Herein, a series of novel tetrahydro-β-carboline derivatives with outstanding inhibitory activity toward MMPs are present. In particular, compounds 9f, 9g, 9h and 9i show sub-nanomolar IC₅₀ values. Interestingly, compounds 9g and 9i also provide remarkable selectivity toward gelatinases; IC₅₀=0.15 nM for both toward MMP-2 and IC₅₀=0.63 and 0.58 nM, resp., toward MMP-9. Mol. docking simulations, performed by employing quantum mechanics based partial charges, shed light on the rationale behind binding involving specific interactions with key residues of S1′ and S3′ domains. Taken together, these studies indicate that tetrahydro-β-carboline represents a promising scaffold for the design of novel inhibitors able to target MMPs and selectively bias gelatinases, over the desirable range of the pharmacokinetics spectrum. In the experiment, the researchers used many compounds, for example, 4-Butoxybenzene-1-sulfonyl chloride (cas: 1138-56-3Name: 4-Butoxybenzene-1-sulfonyl chloride).

4-Butoxybenzene-1-sulfonyl chloride (cas: 1138-56-3) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. 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.Name: 4-Butoxybenzene-1-sulfonyl chloride

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

Structure-activity Relationship Studies of Microbiologically Active Thiosemicarbazides Derived from Hydroxybenzoic Acid Hydrazides was written by Plech, Tomasz;Paneth, Agata;Kapron, Barbara;Kosikowska, Urszula;Malm, Anna;Strzelczyk, Aleksandra;Staczek, Pawel. And the article was included in Chemical Biology & Drug Design in 2015.Electric Literature of C7H3Cl2NS This article mentions the following:

Forty-five derivatives of thiosemicarbazide were synthesized, and their antibacterial activity against Gram-pos. and Gram-neg. bacteria was evaluated. Some of the described compounds exhibited interesting activity against reference strains of Gram-pos. bacteria, whereas only two derivatives had the ability to inhibit the growth of Gram-neg. species (Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 13883, Proteus mirabilis ATCC 12453). The most potent antimicrobial activity was observed in the cases of salicylic acid hydrazide derivatives The differences in activity inspired us to conduct conformational anal. using mol. mechanics level. The obtained results suggest that the mol. geometry, especially at the N4-terminus of thiosemicarbazide skeleton, determines the antibacterial activity. Unfortunately, in opposition to what we expected, only one of the tested compounds inhibited the activity of the topoIV enzyme, and none of them was active against DNA gyrase. In the experiment, the researchers used many compounds, for example, 2,4-Dichlorophenylisothiocyanate (cas: 6590-96-1Electric Literature of C7H3Cl2NS).

2,4-Dichlorophenylisothiocyanate (cas: 6590-96-1) 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. 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.Electric Literature of C7H3Cl2NS

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

Responsive Ionogel Surface with Renewable Antibiofouling Properties was written by Ye, Lijun;Chen, Fei;Liu, Jie;Gao, Aiting;Kircher, Gunnar;Liu, Wendong;Kappl, Michael;Wegner, Seraphine;Butt, Hans-Juergen;Steffen, Werner. And the article was included in Macromolecular Rapid Communications in 2019.Computed Properties of C18H37Cl This article mentions the following:

The synthesis of ionogels with a responsive, self-replenishing surface for combating biofouling is described. Ionogels are prepared by infiltrating poly(vinylidene fluoride-co-hexafluoropropylene) with binary mixtures of ionic liquids (IL): 1-octadecyl-3-methylimidazolium bis(trifluoromethyl sulfonyl)imide ([C₁₈C₁i.m.][NTf₂], m.p. T_m = 55 °C) and 1-hexyl-3-methylimidazolium bis(trifluoromethyl sulfonyl)imide ([C₆C₁i.m.][NTf₂], T_m = -9 °C). The IL mixtures release spontaneously from the gel matrix and eventually crystallize on the surface. This leads to self-replenishment of the surface of ionogels even after mech. damage. The incorporation of [C₆C₁i.m.][NTf₂] provides the antimicrobial efficacy of ionogels while the crystals of [C₁₈C₁i.m.][NTf₂] serve as a skeleton maintaining [C₆C₁i.m.][NTf₂] on the surface. By heating, the ionogel surface transforms from solid to liquid-infused state-the removal of biofilms/bacteria developed under a long time of colonization is facilitated. The antimicrobial efficacy is maintained even after several cycles of biofilm formation and detachment. This work provides an opportunity to apply ionogels as functional coatings with renewable antibiofouling properties. In the experiment, the researchers used many compounds, for example, 1-Chlorooctadecane (cas: 3386-33-2Computed Properties of C18H37Cl).

1-Chlorooctadecane (cas: 3386-33-2) 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. 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.Computed Properties of C18H37Cl

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

Study on synthesis and anticancer activity of 17beta-estradiol-phenol/aniline nitrogen mustard derivatives was written by Yin, Yu-dong;Liu, Jing-jing;Liao, Wen-fei;Guo, Xian-kun;Zhang, Li-shan;Mo, Wei-bin;Cheng, Ke-guang. And the article was included in Medicinal Chemistry Research in 2021.COA of Formula: C19H15Cl This article mentions the following:

As 17β-estradiol and its derivatives have good affinity with estrogen receptors and have unique antitumor properties, O¹-propargyl-N⁴,N⁴-bis(2-chloroethyl)-4-aminophenol and N⁴,N⁴-dipropargyl-N¹,N¹-bis(2-chloroethyl)-1,4-phenylenediamine were resp. combined with 17β-estradiol through linkers of different lengths. These targeted novel nitrogen mustard 17β-estradiol derivatives were tested antiproliferative activity using the MTT assay. The results illustrated that these compounds were less toxicity to HL-7702 (human liver cells) and SKOV-3, though all their activity potency was moderate or weak against the MDA-MB-231, MCF-7 and BEL-7404 cell lines. The inhibitory activity of the O¹-propargyl-N⁴,N⁴-bis (2-chloroethyl)-4-aminophenol derivatives were obviously better than the N⁴-dipropargyl-N¹, N¹-bis (2-chloroethyl) -1,4-phenylenediamine derivatives against tested tumor cell lines. And three hybrids exhibited good inhibitory activity against BEL-7404 cell line (IC₅₀ = 13.5, 15.3 and 13.9μM, resp.). After that, we performed KEGG pathway anal. on one compound, and the results showed that it mainly induced breast cancer cell apoptosis by regulating the expression of the proteins in NF-κ B pathway. In the experiment, the researchers used many compounds, for example, (Chloromethanetriyl)tribenzene (cas: 76-83-5COA of Formula: C19H15Cl).

(Chloromethanetriyl)tribenzene (cas: 76-83-5) 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. 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.COA of Formula: C19H15Cl

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

Effect of dielectric barrier discharge cold plasma treatments on flavor fingerprints of brown rice was written by Liu, Qiang;Wu, Haijing;Luo, Ji;Liu, Jiwei;Zhao, Siqi;Hu, Qiuhui;Ding, Chao. And the article was included in Food Chemistry in 2021.SDS of cas: 57045-82-6 This article mentions the following:

A non-thermal processing method was developed to promote preservation of brown rice using dielec. barrier discharge cold plasma (DBD-CP). Physicochem. properties including free fatty acid (FFA) content, surface color change, volatile organic components (VOCs) and flavor fingerprints were evaluated in brown rice submitted to DBD-CP. FFA levels were 25.2% lower in treated samples compared to the control, and a more stable surface color was obtained at the end of the storage period. A total of 35 major VOCs could be detected in treated samples, and reduced levels of hexanal can be used as an indicator of DBD-CP treatment in brown rice during storage. Moreover, the flavor fingerprints in DBD-CP treated groups can be successfully distinguished through headspace gas chromatog. ion mobility spectrometry. Collectively, application of DBD-CP treatment could be utilized as a feasible approach to promote stabilization of brown rice and preserve flavor during storage. In the experiment, the researchers used many compounds, for example, Chloroformicacidn-nonylester (cas: 57045-82-6SDS of cas: 57045-82-6).

Chloroformicacidn-nonylester (cas: 57045-82-6) 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: 57045-82-6

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

Palladium-Catalyzed α-Arylation of Tetramic Acids was written by Storgaard, Morten;Zaragoza Doerwald, Florencio;Peschke, Bernd;Tanner, David. And the article was included in Journal of Organic Chemistry in 2009.Recommanded Product: 18437-66-6 This article mentions the following:

A mild, racemization-free, palladium-catalyzed α-arylation of tetramic acids (2,4-pyrrolidinediones) has been developed. Various amino acid-derived tetramic acids were cleanly arylated by treatment with 2 mol % of Pd(OAc)₂, 4 mol % of a sterically demanding biaryl phosphine, 2.3 equiv of K₂CO₃ or K₃PO₄, and aryl chlorides, bromides, or triflates in THF. With conventional heating, conversions >95% could be attained after 1 h at 80 °C, whereas microwave-induced heating led to much shorter reaction times (5 min at 110 °C). The electron d. of the aryl electrophile had no effect on their reactivity: both electron-rich and electron-poor aryl chlorides and bromides or triflates led to good yields. Ortho-substituted aryl halides and heteroaryl halides, however, did not undergo the title reaction. In the experiment, the researchers used many compounds, for example, tert-Butyl (4-chlorophenyl)carbamate (cas: 18437-66-6Recommanded Product: 18437-66-6).

tert-Butyl (4-chlorophenyl)carbamate (cas: 18437-66-6) 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. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Recommanded Product: 18437-66-6

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

Solid-state structure, phase transition, and shape-memory properties of network copolymers with hyperbranched units containing s-benzenetricarbamide cores was written by Otsuki, Yuto;Yamaguchi, Junto;Tsukamoto, Tadashi;Shibasaki, Yuji;Fujimori, Atsuhiro. And the article was included in Polymer in 2022.Product Details of 4422-95-1 This article mentions the following:

This study is aimed at elucidating the origin of the shape-memory characteristics, associated with temperature changes of network copolymers consisting of hyperbranched units with s-benzenetricarbamide cores. For the copolymers used in this study, the trifunctional hyperbranched unit is designated as a hard segment (Hard-Sg), and polyethylene glycol (PEG), which is N-H group-capped at both ends and linked to Hard-Sg, is designated as a soft segment (Soft-Sg). When we use Hard-Sg obtained by linking five units of 4-methylaminobenzoic acid at the core and Hard-Sg with its -COOH terminal carbazidized, the solubility in the general solvents and the high-temperature behavior of the obtained copolymers are significantly different. Using carboazidization of the Hard-Sg terminal, the copolymers could be cured at 140 °C via the Curtius rearrangement, and thus they became insoluble, exhibited elongation and shrinking characteristics above the m.p., and regained their shape when the temperature was raised again. Reciprocal lattice anal. revealed that the PEG chain, i.e. the Soft-Sg, was the main component of crystallization, and the shape-memory characteristics repeat plasticization, structural fixation, and contraction restoration with the phase transition of this Soft-Sg unit. In the experiment, the researchers used many compounds, for example, Trimesoylchloride (cas: 4422-95-1Product Details of 4422-95-1).

Trimesoylchloride (cas: 4422-95-1) 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.Product Details of 4422-95-1

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

Synthesis and Biological Evaluation of Thieno[2,3-d]pyrimidine-amides as Potential Anticancer Agents was written by Ramya, Posa Venkata Sri;Thatikonda, Sowjanya;Angapelly, Srinivas;Babu, Bathini Nagendra;Naidu, Vegi Ganga Modi;Kamal, Ahmed. And the article was included in ChemistrySelect in 2018.Reference of 34662-36-7 This article mentions the following:

A new class of N-(3-(thieno[2,3-d]pyrimidin-4-ylamino)phenyl)amides I [R = Ph, 4-MeC₆H₄, 2-CF₃C₆H₄, etc.] were synthesized and examined for their anticancer activity towards different human cancer cell lines. Out of the tested derivatives, compounds I [R = 4-FC₆H₄, 2-NO₂-5-CH₃C₆H₃, 3-CF₃C₆H₄CH=CH, stereo = E] displayed potent growth inhibition on some of the cell lines, peculiarly I [R = 3-CF₃C₆H₄CH=CH, stereo = E] exhibited selective and promising activity on MDA-MB-453 and MCF-7 cell lines. In comparison to the standard ZSTK474, nearly 3 fold growth inhibitory effect was noticed with I [R = 3-CF₃C₆H₄CH=CH, stereo = E] against MCF-7 cell line. The morphol. and long term clonogenic survival of MCF-7 cells were affected by compound I [R = 3-CF₃C₆H₄CH=CH, stereo = E]. The results from AO/EB and DAPI staining studies as well as anal. of mitochondrial membrane potential divulged that the growth of MCF-7 cells was inhibited by I [R = 3-CF₃C₆H₄CH=CH, stereo = E] through the induction of apoptosis. From flow-cytometry anal., it was notable that I [R = 3-CF₃C₆H₄CH=CH, stereo = E] shows G0/G1 cell cycle arrest in MCF-7 cells. In the experiment, the researchers used many compounds, for example, 3-Chloro-5-nitrobenzoic acid (cas: 34662-36-7Reference of 34662-36-7).

3-Chloro-5-nitrobenzoic acid (cas: 34662-36-7) 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.Reference of 34662-36-7

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