Category: amides-buliding-blocks

Phytochemical, toxicity and antihyperglycaemic effects of Zea mays Linn leaves’ extracts was written by Kotin, Lucrece Mahoutin;Assogba, Fidele Mahoudo;Akakpo, Huguette Baie;Aikpe, Judith Fifamin Ahounou;Godonou, Jean-Benoit;Dansou, Pierre Houndjovi;Gbenou, Joachim Djimon. And the article was included in Journal of Drug Delivery and Therapeutics in 2022.Application of 10238-21-8 This article mentions the following:

In the Republic of Benin, several plants, including Zea mays Linn (Z. mays) are used for the treatment of diabetes without any scientific studies showing their effectiveness. The objective of this study is to investigate the effects of Z. mays leaves’ extracts on hyperglycemic rabbits using the Oral Glucose Tolerance Test (OGTT), 2 g/kg of (D) + glucose and on hepatic glucose liberation. Phytochem. screening revealed that the plant leaves contain alkaloids, tannins, mucilage flavonoids, anthocyanin, leuco-anthocyanin, coumarins, heteroside, flavonoid, triterpenoids, steroids, reducing compounds, saponins, oses and holosides. Cytotoxity tests showed that the aqueous and ethanolic extracts were free of toxicity. The extracts have shown anti-hyperglycemic activities dependent on specific dosage and timing. The ED is 500 mg/kg for the aqueous extract and for the ethanolic extract The extracts are effective as compared with glibenclamide (reference product). Moreover, the ex vivo test conducted on the liver revealed that Z. mays aqueous extract inhibits the hepatic glucose liberation and 500 mg/kg is the most ED. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Application of 10238-21-8).

5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Application of 10238-21-8

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

Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors was written by Kishore Kumar, G. D.;Chavarria, Gustavo E.;Charlton-Sevcik, Amanda K.;Arispe, Wara M.;MacDonough, Matthew T.;Strecker, Tracy E.;Chen, Shen-En;Siim, Bronwyn G.;Chaplin, David J.;Trawick, Mary Lynn;Pinney, Kevin G.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.COA of Formula: C10H10F3NO2 This article mentions the following:

A small library of 36 functionalized benzophenone thiosemicarbazone analogs was prepared by chem. synthesis and evaluated for their ability to inhibit the cysteine proteases cathepsin L and cathepsin B. The six most active inhibitors of cathepsin L (IC₅₀ < 85 nM) in this series were I (R = 2-F, 3-F₃C, 4-F, 2,3-F₂, 3,5-F₂, 2,3,4,5-F₄). These six analogs were selective for their inhibition of cathepsin L vs. cathepsin B (IC₅₀ > 10,000 nM). The most active analog in the series, thiosemicarbazone I (R = 2-F), also efficiently inhibited cell invasion of the DU-145 human prostate cancer cell line. In the experiment, the researchers used many compounds, for example, N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7COA of Formula: C10H10F3NO2).

N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.COA of Formula: C10H10F3NO2

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

Molecular encapsulation of berberine and ethidium bromide in anthraquinone-carboxamido-β-cyclodextrin conjugate: supramolecular association with DNA duplex and G-quadruplexes was written by Soundarapandian, Suganthi;Alexander, Aleyamma;Sumohan Pillai, Archana;Enoch, Israel V. M. V.;Yousuf, Sameena. And the article was included in Nucleosides, Nucleotides & Nucleic Acids in 2021.Recommanded Product: 2387-23-7 This article mentions the following:

G-quadruplex DNA in recognized as a potential target for anticancer drugs. In this work, an anthraquinonecarboxamido derivative of β-cyclodextrin (AQCC) is synthesized as a novel DNA binder that further can deliver an addnl. mol. at the target, carrying it in the cavity of modified cyclodextrin. The binding of AQCC with ethidium bromide (EtBr), berberine (Ber), duplex calf-thymus DNA (CT-DNA), quadruplexes, e.g. 5′-AGGGAGGGCGCTGGGAGGAGGG-3′ are studied. The compound acts as a host mol. for the encapsulation of DNA binders viz., EtBr, Ber and enhances their fluorescence due to the encapsulation in its AQCC’s cyclodextrin cavity. The conjugate displays a quenching of fluorescence selectively on the association with CT-DNA and quadruplexes. CT-DNA exhibits dissimilar fluorescence spectra in free- and EtBr-bound forms. In addition, the effect of Ber in binding to the target DNAs is pronounces since the Ber mol. has more affinity to bind to quadruplexes than the duplex. In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Recommanded Product: 2387-23-7).

1,3-Dicyclohexylurea (cas: 2387-23-7) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Recommanded Product: 2387-23-7

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

Efficient and general one-pot synthesis of β-chloro-β-trifluoromethylated enones from 3,3,3-trifluoropropyne was written by Jeon, Sung Lan;Kim, Dae Ho;Son, Jang Bae;Jeong, In Howa. And the article was included in Bulletin of the Korean Chemical Society in 2006.Product Details of 116332-61-7 This article mentions the following:

CF₃CCH reacted with Weinreb amides in BuLi/THF to give CF₃CCl:CHCOR [R = (un)substituted Ph, 1-naphthalenyl, 2-furanyl, cyclohexyl] as E-Z mixtures In the experiment, the researchers used many compounds, for example, N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7Product Details of 116332-61-7).

N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Product Details of 116332-61-7

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

Convenient cyclization of o-difunctional heterocycles with N,N-dimethylformamide dimethyl acetal was written by Stanovnik, B.;Tisler, M.. And the article was included in Synthesis in 1974.Reference of 50608-99-6 This article mentions the following:

0-Phenylenediamine cyclized readily with Me2NCH(OMe)2 when heated at 120-30° for 2 hr in DMF to give benzimidazole I (X = NH, X1 = CH). Analogously I (X = S, X1 = CH; X = S, X1 = N; X = NH X1 = N), II, and III (X = N, X1 = CH; X = CH, X1 = ) were prepared In the experiment, the researchers used many compounds, for example, 3-Aminopicolinamide (cas: 50608-99-6Reference of 50608-99-6).

3-Aminopicolinamide (cas: 50608-99-6) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Reference of 50608-99-6

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

Impact of FDA-Approved Drugs on the Prostaglandin Transporter OATP2A1/SLCO2A1 was written by Kamo, Shunsuke;Nakanishi, Takeo;Aotani, Rika;Nakamura, Yoshinobu;Gose, Tomoka;Tamai, Ikumi. And the article was included in Journal of Pharmaceutical Sciences in 2017.Electric Literature of C18H17NO5 This article mentions the following:

To understand interaction of drugs with the prostaglandin transporter OATP2A1/SLCO2A1 that regulates disposition of prostaglandins, we explored the impact of 636 drugs in an FDA-approved drug library on 6-carboxyfluorescein (6-CF) uptake by OATP2A1-expressing HEK293 cells (HEK/2A1). Fifty-one and 10 drugs were found to inhibit and enhance 6-CF uptake by more than 50%, resp. Effect of the 51 drugs on 6-CF uptake was pos. correlated with that on PGE₂ uptake (r = 0.64, p < 0.001). Among those, 5 drugs not structurally related to prostaglandins, suramin, pranlukast, zafirlukast, olmesartan medoxomil, and losartan potassium, exhibited more than 90% PGE₂ uptake inhibition. Inhibitory affinity of suramin to OATP2A1 was the highest (IC_50,2A1 of 0.17 μM), and its IC₅₀ values to MRP4-mediated PGE₂ transport (IC_50,MRP4) and PGE₂ synthesis in human U-937 cells treated with phorbol 12-myristate 13-acetate (IC_50,Syn) were 73.6 and 336.7 times higher than IC_50,2A1, resp. Moreover, structure-activity relationship study in 29 nonsteroidal anti-inflammatory drugs contained in the library displayed inhibitory activities of anthranilic acid derivatives, but enhancing effects of propionic acid derivatives These results demonstrate that suramin is a potent selective inhibitor of OATP2A1, providing a comprehensive information about drugs in clin. use that interact with OATP2A1. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Electric Literature of C18H17NO5).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Electric Literature of C18H17NO5

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

A new and efficient synthetic route for the anxiolytic agent CL285032 was written by Ghidu, Victor P.;Ilies, Marc A.;Cullen, Tom;Pollet, Robert;Abou-Gharbia, Magid. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Synthetic Route of C11H13NO2 This article mentions the following:

CL285032, i.e. 6-[3-(acetylmethylamino)phenyl]-3-methyl[1,2,4]triazolo[4,3-b]pyridazine, is an anxiolytic compound currently under investigation as a possible treatment for canine noise phobia associated anxiety. A robust scale-up and manufacturing process is essential for the development and marketability of the drug. The current synthetic route, although reliable, requires 7 steps and has a low overall yield (18%), leaving opportunity for improvement. The authors present an efficient alternative approach toward the synthesis of CL285032 from 3-AcMeNC₆H₄Ac over 3 steps with 65% overall yield. In the experiment, the researchers used many compounds, for example, N-(3-Acetylphenyl)-N-methylacetamide (cas: 325715-13-7Synthetic Route of C11H13NO2).

N-(3-Acetylphenyl)-N-methylacetamide (cas: 325715-13-7) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Synthetic Route of C11H13NO2

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

Oxidative Catalytic Spiroketalization Leading to Diastereoselective Synthesis of Spiro[benzofuran-2,1′-isochromene]s was written by Qiu, Jiang-Kai;Hao, Wen-Juan;Li, Guigen;Jiang, Bo. And the article was included in Advanced Synthesis & Catalysis in 2018.Application of 1146-43-6 This article mentions the following:

One-pot, two-step silver-catalyzed spiroketalization of the in-situ generated quinone imine ketals (QIKs) with β-alkynyl ketones was established, enabling multiple C-O and C-C bond-forming reactions to access densely functionalized spiro[benzofuran-2,1′-isochromene] derivatives with generally good yields. The use of β-alkynyl ketones bearing alkyl and aryl groups located at the α-position of the carbonyl group led to highly diastereoselective spiro[chromane-2,1′-isochromene] derivatives The reaction featured broad substrate scope, mild oxidative catalytic conditions and excellent diastereoselectivity. In the experiment, the researchers used many compounds, for example, N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6Application of 1146-43-6).

N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6) belongs to amides. Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Application of 1146-43-6

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

Cyclodimerization of isocyanates promoted by one large vertex metallaborane was written by Ma, Pei;Spencer, James T.. And the article was included in Polyhedron in 2018.Related Products of 2387-23-7 This article mentions the following:

The 10-vertex Manganese-decaborane [nido-6-Mn(CO)₃B₉H₁₃][NMe₄] was found to act as an efficient catalyst for the synthesis of ureas I [R = allyl, n-Bu, cyclohexyl, Ph, Bn] via cyclodimerization of isocyanates under photo-irradiation conditions. The reaction yields were comparable with other metal catalyst reported in literature. Compound I [R = Ph] was characterized by X-ray crystallog. study and reaction mechanism was also proposed. The results are very encouraging as they represent first examples of a large metallaborane compound to catalyze the cyclodimerization of isocyanates. In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Related Products of 2387-23-7).

1,3-Dicyclohexylurea (cas: 2387-23-7) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Related Products of 2387-23-7

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

Directed ortho Metalation (DoM)-Linked Corriu-Kumada, Negishi, and Suzuki-Miyaura Cross-Coupling Protocols: A Comparative Study was written by Quesnelle, Claude A.;Snieckus, Victor. And the article was included in Synthesis in 2018.Application In Synthesis of N,N-Diethylsalicylamide This article mentions the following:

A systematic study of the widely used, titled transition-metal-catalyzed cross-coupling reactions with attention to context with the directed orthometalation (DoM) was reported. In general, the Suzuki-Miyaura and Negishi protocols showed greater scope and better yields than the Corriu-Kumada variant, although the latter qual. proceeded at fastest rate but had low functional group tolerance. The Negishi process was shown to be useful for substrates with nucleophile and base-sensitive functionality and it was comparable to the Suzuki-Miyaura reaction in efficiency. The link of these cross-coupling reactions to the DoM strategy lends itself to the regioselective construction of diversely substituted aromatics and heteroaromatics In the experiment, the researchers used many compounds, for example, N,N-Diethylsalicylamide (cas: 19311-91-2Application In Synthesis of N,N-Diethylsalicylamide).

N,N-Diethylsalicylamide (cas: 19311-91-2) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Application In Synthesis of N,N-Diethylsalicylamide

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