Tag: 200-300

Synthesis, Antioxidant, Anti-Inflammatory, and Antimicrobial Screening of Newer Thiophene-Fused Arylpyrazolyl 1,3,4-Oxadiazoles was written by Mahajan, Pravin;Nikam, Mukesh;Chate, Asha;Nimbalkar, Urja;Patil, Vrushali;Bobade, Anil;Chaudhari, Abhay;Deolankar, Dattatray;Javale, Balasaheb;Gill, Charansingh. And the article was included in Phosphorus, Sulfur and Silicon and the Related Elements in 2015.Category: bromides-buliding-blocks This article mentions the following:

A series of newer 1,3,4-oxadiazole derivatives containing a thiophene fused with pyrazole moiety of pharmacol. significance have been synthesized. The compounds were characterized by ¹H NMR, IR, and mass spectral techniques. The compounds were screened for their in vitro antioxidant, anti-inflammatory and antimicrobial activities. Several compounds showed significant antioxidant activity. One compound showed good anti-inflammatory activity. One compound showed activity . against bacterial and fungal strains. The synthesis of the target compounds was achieved using 3-methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid hydrazide as a starting material. The title compounds thus formed included 3-methyl-1-phenyl-5-(5-phenyl-1,3,4-oxadiazol-2-yl)-1H-thieno[2,3-c]pyrazole. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8Category: bromides-buliding-blocks).

3-(Bromomethyl)benzoic acid (cas: 6515-58-8) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Polyamine-Functionalized 2′-Amino-LNA in Oligonucleotides: Facile Synthesis of New Monomers and High-Affinity Binding towards ssDNA and dsDNA was written by Danielsen, Mathias B.;Christensen, Niels Johan;Joergensen, Per T.;Jensen, Knud J.;Wengel, Jesper;Lou, Chenguang. And the article was included in Chemistry – A European Journal in 2021.Recommanded Product: 954-81-4 This article mentions the following:

Attachment of cationic moieties to oligonucleotides (ONs) promises not only to increase the binding affinity of antisense ONs by reducing charge repulsion between the two neg. charged strands of a duplex, but also to augment their in vivo stability against nucleases. In this study, polyamine functionality was introduced into ONs by means of 2′-amino-LNA scaffolds. The resulting ONs exhibited efficient binding towards ssDNA, ssRNA and dsDNA targets, and the 2′-amino-LNA analog carrying a tri-aminated linker showed the most pronounced duplex- and triplex-stabilizing effect. Mol. modeling revealed that favorable conformational and electrostatic effects led to salt-bridge formation between pos. charged polyamine moieties and the Watson-Hoogsteen groove of the dsDNA targets, resulting in the observed triplex stabilization. All the investigated monomers showed increased resistance against 3′-nucleolytic digestion relative to the non-functionalized controls. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Recommanded Product: 954-81-4).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. For many applications, organobromides represent a compromise of reactivity and cost.Recommanded Product: 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

One-Pot Preparation of (NH)-Phenanthridinones and Amide-Functionalized [7]Helicene-like Molecules from Biaryl Dicarboxylic Acids was written by Murai, Takuya;Xing, Yongning;Kurokawa, Mayu;Kuribayashi, Toshifumi;Nikaido, Masanori;Elboray, Elghareeb E.;Hamada, Shohei;Kobayashi, Yusuke;Sasamori, Takahiro;Kawabata, Takeo;Furuta, Takumi. And the article was included in Journal of Organic Chemistry in 2022.Electric Literature of C8H6BrFO2 This article mentions the following:

A one-pot transformation of biaryl dicarboxylic acids to (NH)-phenanthridinone derivatives based on a Curtius rearrangement and subsequent basic hydrolysis was developed. This method is also applicable for the preparation of optically active amide-functionalized [7]helicene-like mols. Furthermore, aza[5]helicene derivatives with a phosphate moiety were isolated as a product of the Curtius rearrangement step in the case of substrates that bear chalcogen atoms. The stereostructures of these products, revealed by X-ray diffraction anal., suggested that chalcogen-bonding and pnictogen-bonding interactions might contribute to their stabilization. The configurational stability of the helicene-like mols. and their chiroptical properties were further investigated. In the experiment, the researchers used many compounds, for example, Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9Electric Literature of C8H6BrFO2).

Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Electric Literature of C8H6BrFO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Photocatalyzed site-selective C(sp³)-H sulfonylation of toluene derivatives and cycloalkanes with inorganic sulfinates was written by Zhang, Shaonan;Cao, Shi;Lin, Yu-Mei;Sha, Liyuan;Lu, Cheng;Gong, Lei. And the article was included in Chinese Journal of Catalysis in 2022.SDS of cas: 57293-19-3 This article mentions the following:

Herein, a convenient and economic approach to site-selective C(sp3)-H sulfonylation via photo-induced HAT catalysis was reported. Employing a conjugated polycyclic quinone as a direct HAT photocatalyst, com. available inorganic sulfinates as the sulfonylation source, copper triflate as an inexpensive oxidant, a variety of toluene derivatives and cycloalkanes were converted into biol. and synthetically interesting sulfone products I [Ar = 4-MeC₆H₄, 4-EtC₆H₄, 4-MeOC₆H₄, etc.; R¹ = H, Me; R² = Me, Et, Ph, etc.; R³ = Ph, Et, i-Pr, etc.], II [R⁴ = cyclopentyl, cyclohexyl, cycloheptyl, etc.] under mild conditions. The mechanistic studies reveal that the reaction sequence involved direct HAT-induced radical formation and a subsequent copper-mediated organometallic process for the C-S bond formation. This method offered an appealing opportunity to furnish high value-added products from abundant hydrocarbon starting materials and inexpensive reagents. In the experiment, the researchers used many compounds, for example, 1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3SDS of cas: 57293-19-3).

1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.SDS of cas: 57293-19-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Structure-activity relationship study of hypoxia-activated prodrugs for proteoglycan-targeted chemotherapy in chondrosarcoma was written by Ghedira, Donia;Voissiere, Aurelien;Peyrode, Caroline;Kraiem, Jamil;Gerard, Yvain;Maubert, Elise;Vivier, Magali;Miot-Noirault, Elisabeth;Chezal, Jean-Michel;Farhat, Farhat;Weber, Valerie. And the article was included in European Journal of Medicinal Chemistry in 2018.SDS of cas: 954-81-4 This article mentions the following:

Due to an abundant chondrogenic, poorly vascularized and particularly hypoxic extracellular matrix, chondrosarcoma, a malignant cartilaginous tumor, is chemo- and radio-resistant. Surgical resection with wide margins remains the mainstay of treatment. To address the lack of therapy, our strategy aims to increase anticancer drugs targeting and delivery in the tumor, by leveraging specific chondrosarcoma hallmarks: an extensive cartilaginous extracellular matrix, namely the high neg. fixed charge d. and severe chronic hypoxia. A dual targeted therapy for chondrosarcoma was investigated by conjugation of a hypoxia-activated prodrug (HAP) to quaternary ammonium (QA) functions which exhibit a high affinity for polyanionic sites of proteoglycans (PGs), the major components of the chondrosarcoma extracellular matrix. Based on preclin. results, an imidazole prodrug, ICF05016, was identified and provided the basis for a lead optimization study. A series of 27 QA-phosphoramide mustard conjugates, differing by the type of QA function and the length of the alkyl linker, was yielded by a common multi-step sequence involving phosphorylation of a key 2-nitroimidazole alc. Then, a screening was realized by surface plasmon resonance technol. to assess biomol. interactions between QA derivatives and aggrecan, the most abundant PG in chondrosarcoma. Results revealed that affinity depends more on the type of QA function, than on the linker length. Moreover, the presence of a benzyl group enhanced affinity to aggrecan. Twelve compounds were shortlisted and evaluated for antiproliferative activity (i.e., growth inhibiting concentration 50), under normoxic and hypoxic conditions using the human extraskeletal myeloid chondrosarcoma cell line (HEMC-SS). For all prodrugs, hypoxic selectivity was maintained and even increased, compared with the lead. From this study, compound I emerged as the most effective PG-targeted HAPs with a dissociation constant of 2.10 μM in the SPR experiment, a hypoxia cytotoxicity ratio of 24 and an efficient reductive cleavage under chem. and enzymic conditions. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4SDS of cas: 954-81-4).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon–bromine bond is electrophilic in nature. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. SDS of cas: 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Structure-Activity Relationships of 9-Substituted-9-Dihydroerythromycin-Based Motilin Agonists: Optimizing for Potency and Safety was written by Shaw, Simon J.;Chen, Yue;Zheng, Hao;Fu, Hong;Burlingame, Mark A.;Marquez, Saul;Li, Yong;Claypool, Mark;Carreras, Christopher W.;Crumb, William;Hardy, Dwight J.;Myles, David C.;Liu, Yaoquan. And the article was included in Journal of Medicinal Chemistry in 2009.Formula: C8H7BrO2 This article mentions the following:

A series of 9-dihydro-9-acetamido-N-desmethyl-N-iso-Pr erythromycin A analogs and related derivatives was generated as motilin agonists. The compounds were optimized for potency while showing both minimal antibacterial activity and hERG inhibition. As the substituent on the amide was increased in lipophilicity the potency and hERG inhibition increased, while polar groups lowered potency, without significantly impacting hERG inhibition. The N-Me acetamide (7a) showed the optimal in vitro profile and was probed further by varying the chain length to the macrocycle as well as changing the macrocycle scaffold. Compound 7a remained the compound with the best in vitro properties. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8Formula: C8H7BrO2).

3-(Bromomethyl)benzoic acid (cas: 6515-58-8) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Formula: C8H7BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

A multifunctional aggregation-induced emission (AIE)-active fluorescent chemosensor for detection of Zn²⁺ and Hg²⁺ was written by Tang, Aling;Yin, Ya;Chen, Zhao;Fan, Congbin;Liu, Gang;Pu, Shouzhi. And the article was included in Tetrahedron in 2019.COA of Formula: C12H7BrN2 This article mentions the following:

An aggregation-induced emission (AIE)-active fluorescent chemosensor based on a tetraphenylethene (TPE) unit was successfully designed and synthesized. The luminogen could detect Zn²⁺ selectively in a THF solution with the detection limit of 1.24 × 10^-6 mol L^-1. Meanwhile, the luminogen could also detect Hg²⁺ selectively in a THF-water mixture with the water content of 90%, and the detection limit was 2.55 × 10^-9 mol L^-1. Also, the solid-state mechanochromic fluorescence behavior of the luminogen was studied systematically. Indeed, the AIE-active luminogen also exhibited reversible mechanofluorochromic phenomenon involving fluorescent color change from blue to green, and powder x-ray diffraction results indicated that the switchable morphol. conversion between crystalline and amorphous states was responsible for this mechanochromism phenomenon. In the experiment, the researchers used many compounds, for example, 2-Bromo-1,10-phenanthroline (cas: 22426-14-8COA of Formula: C12H7BrN2).

2-Bromo-1,10-phenanthroline (cas: 22426-14-8) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.COA of Formula: C12H7BrN2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Total Synthesis of Dictyodendrins B and E was written by Liang, Jingjing;Hu, Weimin;Tao, Pengyu;Jia, Yanxing. And the article was included in Journal of Organic Chemistry in 2013.Computed Properties of C9H11BrO This article mentions the following:

The concise synthesis of the novel telomerase inhibitors dictyodendrins B and E, I and II, resp., was completed in only 9 and 11 steps (longest linear sequence). The highly convergent strategy employed a palladium-catalyzed Larock indole synthesis and a palladium-mediated one-pot consecutive Buchwald-Hartwig amination/C-H activation reaction as key steps. The present synthesis exhibits respectable levels of atom-, redox-, and step-economy. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Computed Properties of C9H11BrO).

1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon–bromine bond is electrophilic in nature. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Computed Properties of C9H11BrO

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Isomeric change in the phenol series. (Third notice.) was written by Ling, Arthur R.. And the article was included in Journal of the Chemical Society, Transactions in 1889.Recommanded Product: 4-Bromo-2-chloro-6-nitrophenol This article mentions the following:

An interesting and at a first sight rather complicated case of isomeric change takes place, when orthochloroparabromophenol is nitrated by warming it in an acetic acid solution with a slight excess of nitric acid, namely, together with the normal products, ortho-chloroparabromorthonitrophenol and orthochlororthoparadinitrophenol, which are formed in the largest quantity, a not inconsiderable amount of diorthochlorobromoparanitrophenol is also produced. The production of orthochlororthoparadinitrophenol, and the consequent elimination of bromine renders this case, however, equivalent to the action of bromine renders this case, however, equivalent to the action of bromine on orthochloroparabromoorthonitrophenol, the latter being without doubt the initial product of the reaction. The isomeric change of parachlororthobromorthonitrophenol into orthochloroparabromoorthonitrophenol does not take place at all, and that a mistake which must have arisen in working with impure materials is explained. In the experiment, the researchers used many compounds, for example, 4-Bromo-2-chloro-6-nitrophenol (cas: 58349-01-2Recommanded Product: 4-Bromo-2-chloro-6-nitrophenol).

4-Bromo-2-chloro-6-nitrophenol (cas: 58349-01-2) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Recommanded Product: 4-Bromo-2-chloro-6-nitrophenol

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Pyridine-2(1H)-thiones: Versatile Precursors for Novel Pyrazolo[3,4-b]pyridine, Thieno[2,3-b]pyridines, and Their Fused Azines was written by Sanad, Sherif M. H.;Abdel-Fattah, Azza M.;Attaby, Fawzy A.;Elneairy, Mohamed A. A.. And the article was included in Journal of Heterocyclic Chemistry in 2019.Computed Properties of C8H6Br2O2 This article mentions the following:

Pyridine-2(1H)-thiones were prepared and reacted with several active halogenated reagents to afford novel thieno[2,3-b]pyridines in excellent yields. Thieno[2,3-b]pyridine-2-carbohydrazide derivative was prepared by the reaction of either Et 2-((3-cyanopyridin-2-yl)thio)acetate derivative or thieno[2,3-b]pyridine-2-carboxylate derivative with hydrazine hydrate. On the other hand, the reaction of either pyridine-2(1H)-thione or Et 2-((pyridin-2-yl)thio)acetate derivative with hydrazine hydrate afforded the corresponding 1H-pyrazolo[3,4-b]pyridine derivative Thieno[2,3-b]pyridine derivatives reacted with several reagents to afford the corresponding pyrimidine-4(3H)-ones and [1,2,3]triazin-4-(3H)-one. Moreover, 2-carbohydrazide derivative reacted with β-dicarbonyl reagents to give 2-((3-methyl-1H-pyrazol-1-yl)carbonyl)thienopyridines. The structure of the target mols. is elucidated using elemental analyses and spectral data. In the experiment, the researchers used many compounds, for example, 3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1Computed Properties of C8H6Br2O2).

3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Computed Properties of C8H6Br2O2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary