Month: November 2022

Siddique, Nadeem Ahmad; Mujeeb, Mohd.; Najmi, Abul Kalam; Aftab, A.; Aslam, Junaid published an article in 2011, the title of the article was Free radical scavenging and hepatoprotective activity of Aegle marmelos (Linn.) corr leaves against carbon tetrachloride.Related Products of 456-12-2 And the article contains the following content:

Aegle marmelos L. belongs to the family Rutaceae; an important medicinal plant being used in the folk therapy. It is the most useful medicinal plant of India. Its medicinal properties have been described in the ancient medical literature. All parts of the tree (stem, bark, root, leaves and fruit at all stages of maturity) have medicinal virtues and have been used as medicine for a long time. A number of chem. constituents have been isolated from various plant parts including alkaloids, coumarin and steroids. The leaves contain skimianinc, sterol and aegelin. In the present investigation antioxidant and hepatoprotective activity of the methanolic extract of A. marmelos leaves (MEAML) was examined on carbon tetrachloride (CCl4) intoxicated rats. MEAML hold considerable amount of phenolic (9.8367 ± 0.0235 mg/kg) and flavonoid (8.248 ± 0.029 mg/kg) contents, which confirmed the antioxidant property of the leaves. The MEAML with different doses (50, 100, 200 mg/kg body weight) and standard silymarin (40 mg/kg body weight) were orally administered to CCl4 treated rats and the effect was studied on serum enzymes [(aspartate transaminase (AST), alanine transaminase (ALT), alk. phosphatase (ALP), and bilurubin, protein, albumin, thiobarbutiric acid (TBARS), reduced glutathione (GSH)]. In addition, in-vitro antioxidant activity of MEAML was also evaluated using 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical. We noticed a significant hepatoprotective activity of MEAML on CCl4 intoxicated rats which support folkloric utilization of A. marmelos, and it was further confirmed by the histol. investigation. The findings of the present investigation revealed that the MEAML possess significant hepatoprotective activity by suppressing CCl4 induced cellular oxidative stress. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Related Products of 456-12-2

The Article related to oxidative stress, hepatoprotectant free radical scavenger aegle leaf carbon tetrachloride antioxidant, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Related Products of 456-12-2

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On November 22, 2019, Sulake, Rohidas Shivaji; Mitra, Rangan; Kadam, Navnath Ambadas; Siyan, Rajinder Singh; Bhise, Nandu Baban; Singh, Girij Pal published a patent.HPLC of Formula: 5455-98-1 The title of the patent was Process for preparation of Neratinib intermediates. And the patent contained the following:

The present invention relates to a process for the preparation of Neratinib intermediates of compound I and compound II [X = halo]. The process involves reaction of compound III [LG = a leaving group] with acetonitrile to yield compound IV [LG is as defined above], reaction of IV with dimethylacetamide to yield compound V [LG is as defined above]; cyclizing V to yield compound VI; halogenation of VI to yield compound VII [X = halo] and reduction of VII to yield II [X = halo]; optionally II can be protected to yield compound VIII [X = halo]. E.g., a multi-step synthesis of VIII [X = Cl], starting from III [LG = OEt] (preparation given) and acetonitrile, was described. The process for the preparation of compound I which comprises the steps of: (a) reacting compound IX [R = alkyl] with alkyl acetate to give compound X [R = alkyl], (b) reducing X 7 in the presence of reducing agent to obtain a compound XI [R = alkyl], and (c) converting XI to compound I, was disclosed. For example, reacting IX [R = Et] with tert-Bu acetate followed by reducing X [R = Et] using NaBH4, and treating XI [R = Et] with Et3N, MsCl in DCM, and hydrolysis of resulting tert-Bu (E)-4-(dimethylamino)but-2-enoate in EtOAc-HCl solution afforded I.HCl. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).HPLC of Formula: 5455-98-1

The Article related to neratinib intermediate preparation, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.HPLC of Formula: 5455-98-1

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On November 21, 2019, Morrow, Benjamin Joseph; Camerino, Michelle Ang; Walker, Scott Raymond; Stevenson, Graeme Irvine; Stupple, Paul Anthony published a patent.Category: amides-buliding-blocks The title of the patent was Substituted condensed thiophenes as modulators of STING protein and their preparation. And the patent contained the following:

The invention relates to substituted benzothiophenes, thienopyridines and thienopyrimidines of formula I and their use as pharmaceuticals for treating diseases ameliorated by modulation of STING protein. Compound of formula I wherein R1 is H, C3-6 cycloalkyl, (un)substituted C3-7 heterocyclyl and (un)substituted (un)branched C1-4 alkyl; A1 is CRA or N; A2 is CRB or N; A3 is CRC or N; A4 is CRD or N; where no more than two of A1, A2, A3, and A4 may be N; one or two of RA, RB, RC, and RD are selected from H, F, Cl, Br, Me, CF3, cyclopropyl, cyano, OMe, OEt, CH2OH, CH2OMe and CH2NMe2; the remainder of RA, RB, RC, and RD are H; Y is O, NH or CH2; R’ is (un)substituted arylcarboxamide, (un)substituted heteroarylcarboxamide and (un)substituted 3-aminobenzisoxazol-6-yl; are claimed. Example compound II was prepared by hydrolysis of Et 3-((4-carbamoylphenoxy)methyl)-4-fluorobenzo[b]thiophene-2-carboxylate. The invention compounds were evaluated for their STING modulatory activity (data given). The experimental process involved the reaction of 2-Fluoro-4-hydroxybenzamide(cas: 1133122-96-9).Category: amides-buliding-blocks

The Article related to condensed thiophene preparation sting modulator, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenothiophenes and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On June 30, 1995, Cash, Gordon G. published an article.Safety of 3-Nitro-4-chlorobenzenesulfonamide The title of the article was Prediction of inhibitory potencies of arenesulfonamides toward carbonic anhydrase using easily calculated molecular connectivity indices. And the article contained the following:

Previous literature reports described the correlation of arenesulfonamide inhibitory potency toward carbonic anhydrase with a quantum mech. descriptor, namely, the total charge on the sulfonamide oxygens, and an indicator variable. The present paper attempts to correlate the same inhibitory potency data with the much more easily calculated mol. connectivity indexes (MCIs) for the same set of compounds A good (r = 0.91) two-variable correlation was found for an subset, from which compounds with a certain structural characteristic had been excluded. This result is consistent with many previous reports that MCIs do well in predicting relative biol. activities of a homologous series of compounds but less well for groups of compounds that differ at several sites. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Safety of 3-Nitro-4-chlorobenzenesulfonamide

The Article related to carbonic anhydrase inhibitor arenesulfonamide qsar, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Safety of 3-Nitro-4-chlorobenzenesulfonamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On January 1, 2011, Munei, Yohei; Shimamoto, Kazunori; Harada, Masataka; Yoshida, Tatsusada; Chuman, Hiroshi published an article.Computed Properties of 97-09-6 The title of the article was Correlation analyses on binding affinity of substituted benzenesulfonamides with carbonic anhydrase using ab initio MO calculations on their complex structures (II). And the article contained the following:

We proposed a novel QSAR (quant. structure-activity relationship) procedure called LERE (linear expression by representative energy terms)-QSAR involving mol. calculations such as ab initio fragment MO and generalized Born/surface area ones. We applied LERE-QSAR to two datasets for the free-energy changes during complex formation between carbonic anhydrase and a series of substituted benzenesulfonamides. The first compound set (Set I) and the second one (Set II) include relatively small substituents and alkyl chains of different lengths in the benzene ring, resp. Variation of the inhibitory activity in Set I is expressed as the combination of Hammett σ and the hydrophobic substituent constant π in classical QSAR, and variation in Set II only by π. LERE-QSAR analyses clearly revealed that effects of σ and π on the activity variations in Sets I and II are consistently explainable with the energy terms in the LERE formulation, and provide more detailed and direct information as to the binding mechanism. The proposed procedure was demonstrated to provide a quant. basis for understanding ligand-protein interactions at the electronic and at. levels. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Computed Properties of 97-09-6

The Article related to benzenesulfonamide carbonic anhydrase ab initio mo, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Computed Properties of 97-09-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 31, 1981, Kumar, Kamal; Bindal, Mahesh C.; Singh, Prithvi; Gupta, Satya P. published an article.SDS of cas: 97-09-6 The title of the article was Effect of molecular size on carbonic anhydrase inhibition by sulfonamides. And the article contained the following:

Mol. size plays an important role in carbonic anhydrase inhibition by sulfonamides. Significant correlation is obtained between the inhibitory power of meta-substituted analogs and the van der Waals volume of the substituents. This provides a theor. basis for mapping the active sites in the enzyme and determining the nature of sulfonamide-receptor binding. It is inferred that, in addition to the well-known binding of the sulfamyl group with the Zn2+ ion of the enzyme, the meta substituent of sulfonamides interacts with some secondary binding site; this interaction is argued to be of van der Waals type. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).SDS of cas: 97-09-6

The Article related to carbonic anhydrase inhibition sulfonamide mol volume, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.SDS of cas: 97-09-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On December 15, 2005, Weller, Thomas; Koberstein, Ralf; Aissaoui, Hamed; Clozel, Martine; Fischli, Walter published a patent.Name: (S)-2-Hydroxy-N-methyl-2-phenylacetamide The title of the patent was Preparation of substituted 1,2,3,4-tetrahydroisoquinolines as orexin receptor antagonists. And the patent contained the following:

Title compounds I [R1-2 = H, alkoxy; R3 = alkyl; X = CH, N] are prepared For instance, II is prepared from a Ru-catalyzed enantioselective alkylation of 6,7-dimethoxy-1-methyl-3,4-dihydroisoquinoline with 1-bromomethyl-4-trifluoromethylbenzene followed by alkylation of the resulting isoquinoline with (S)-α-(4-toluenesulfonyloxy)-N-methylphenylacetamide (preparation given). Compounds of the invention are orexin antagonists with activity in the nanomolar range. I are useful for the treatment of, e.g., anxiety and depression. The experimental process involved the reaction of (S)-2-Hydroxy-N-methyl-2-phenylacetamide(cas: 65645-88-7).Name: (S)-2-Hydroxy-N-methyl-2-phenylacetamide

The Article related to tetrahydroisoquinoline orexin receptor antagonist process preparation, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Name: (S)-2-Hydroxy-N-methyl-2-phenylacetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On May 31, 2010, Yoshida, Tatsusada; Munei, Yohei; Hitaoka, Seiji; Chuman, Hiroshi published an article.Recommanded Product: 3-Nitro-4-chlorobenzenesulfonamide The title of the article was Correlation Analyses on Binding Affinity of Substituted Benzenesulfonamides with Carbonic Anhydrase Using ab Initio MO Calculations on Their Complex Structures. And the article contained the following:

Quant. structure-activity relationship analyses on the free energy change during complex formation between substituted benzenesulfonamides (BSAs) and bovine carbonic anhydrase II (bCA II) were performed using generalized Born/surface area (GB/SA) and ab initio fragment MO (FMO) calculations for the whole complex structures. The result shows that the overall free energy change is governed by the contribution from solvation and dissociation free energy changes accompanying complex formation. The FMO-IFIE (interfragment interaction energy) anal. quant. revealed that the intrinsic interaction energy of bCA II with BSAs is mostly from interactions with amino acid residues in the active site of bCA II. The “Zn block” (Zn2+ and three histidine residues coordinated to Zn2+) in the active site shows the lowest interaction energy and the greatest variance of interaction energy with BSAs through their coordination interaction. The proposed procedure was demonstrated to provide a quant. basis for understanding a ligand-protein interaction at electronic and at. levels. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Recommanded Product: 3-Nitro-4-chlorobenzenesulfonamide

The Article related to binding affinity model benzenesulfonamide derivative carbonic anhydrase, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Recommanded Product: 3-Nitro-4-chlorobenzenesulfonamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On November 23, 2021, Fan, Qinghua; Zhang, Shanshan; Chen, Fei; He, Yanmei published a patent.Recommanded Product: 167316-28-1 The title of the patent was Asymmetric hydrogenation kinetic resolution of racemic polysubstituted dihydroisoquinoline. And the patent contained the following:

The invention discloses an asym. hydrogenation kinetic resolution method of racemic polysubstituted dihydroisoquinoline, which can realize the resolution of racemic polysubstituted dihydroisoquinoline compounds, and obtain a single optical isomer of polysubstituted chiral tetrahydroisoquinoline compounds and polysubstituted chiral dihydroisoquinoline compounds with certain optical purity. The asym. hydrogenation kinetic resolution method comprises the following steps: in the presence of chiral diamine metal catalyst, the mixture containing enantiomers of polysubstituted dihydroisoquinoline compounds is asym. hydrogenated with hydrogen. The experimental process involved the reaction of N-[(1S,2S)-2-Amino-1,2-diphenylethyl]-1,1,1-trifluoromethanesulfonamide(cas: 167316-28-1).Recommanded Product: 167316-28-1

The Article related to asym hydrogenation kinetic resolution racemic polysubstituted dihydroisoquinoline, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Recommanded Product: 167316-28-1

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 31, 2022, Marae, Islam S.; Ibrahim, Omaima F.; Abdel-Hafez, Shams H.; Mohamed, Shaaban K.; Mague, Joel T.; Bakhite, Etify A.-G. published an article.Synthetic Route of 79-07-2 The title of the article was Synthesis, characterization and crystal structure of some novel partially hydrogenated isoquinolines and their fused heterocyclic systems. And the article contained the following:

Ketonic hydrolysis of 7-acetyl-4-cyano-1,6-dimethyl-6-hydroxy-8-phenyl-5,6,7,8-tetrahydro-isoquinoline-3(2H)-thione via heating with aqueous solution of potassium hydroxide resulted in both deacetylation and dehydration affording new 7,8-dihydroisoquinoline scaffold (7,8-DHISQ) I. Two simple mechanistic approaches are postulated for this synthesis. One of them was supported by converting II into I via heating with aqueous solution of potassium hydroxide. I was used as a key intermediate for synthesizing other 7,8-DHISQ’s III and IV, as well as 7,8-dihydrothienoisoquinoline. Reaction of compound II with 2-chloroacetamide by refluxing in ethanol containing sodium acetate gave 7-acetyl-1-amino-5,8-dimethyl-6-phenyl-6,7-dihydrothieno[2,3-c] isoquinoline-2-carboxamide which was converted into full aromatized pyrimidothienoisoquinoline on treatment with tri-Et orthoformate. Reaction of II with both hydrazine hydrate and hydroxylamine hydrochloride afforded tetrahydropyrazolo-isoquinoline and tetrahydroisoxazoloisoquinoline, resp. Reaction of tetrahydroisoxazoloisoquinoline with N-(4-chlorophenyl)-2-chloroacetamide produced (N-phenylcarbamoylmethylthio)tetra-hydroisoxazoloisoquinoline which was converted into tetrahydroisoxazolothieno-isoquinoline upon heating with sodium ethoxide. Also, crystal structures of compounds III and another tetrahydropyrazoloisoquinoline were determined via X-rays diffraction anal. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Synthetic Route of 79-07-2

The Article related to hydrogenated isoquinoline fused heterocyclic system preparation crystal structure, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Synthetic Route of 79-07-2

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics