Month: October 2022

On April 25, 2018, Gur, Zehra Tugce; Caliskan, Burcu; Garscha, UIrike; Olgac, Abdurrahman; Schubert, Ulrich S.; Gerstmeier, Jana; Werz, Oliver; Banoglu, Erden published an article.Formula: C6H5ClN2O4S The title of the article was Identification of multi-target inhibitors of leukotriene and prostaglandin E2 biosynthesis by structural tuning of the FLAP inhibitor BRP-7. And the article contained the following:

Leukotrienes (LTs) and prostaglandin (PG)E2 are enzymically produced from arachidonic acid and represent highly bioactive lipid mediators with pro-inflammatory functions. Here, the authors report on novel multi-target inhibitors that potently and dually interfere with 5-lipoxygenase-activating protein (FLAP) and microsomal prostaglandin E2 synthase (mPGES)-1 in LT and PGE2 biosynthesis, based on the previously identified selective FLAP inhibitor BRP-7 (8, IC50 = 0.31 μM). C -substitution of the benzimidazole ring of BRP-7 by carboxylic acid and its bioisosteres provided compounds, exemplified by 57 (5-{1-[(2-chlorophenyl)methyl]-2-{1-[4-(2-methylpropyl)phenyl]ethyl}-1H-benzimidazol-5-yl}-2,3-dihydro-1,3,4-oxadiazole-2-thione) that potently suppress LT formation (IC50 = 0.05 μM) by targeting FLAP along with inhibition of mPGES-1 (IC50 = 0.42 μM). Besides FLAP, also 5-lipoxygenase (5-LO) and LTC4 synthase activities were inhibited by 57, albeit with lower potency (IC50 = 0.6 and 6.2 μM) than FLAP. Docking studies and mol. dynamic simulations with FLAP, mPGES-1 and 5-LO provide valuable insights into potential binding interactions of the inhibitors with their targets. Together, these novel benzimidazole derivatives may possess potential as leads for development of effective anti-inflammatory drugs with multi-target properties for dually inhibiting LT and PGE2 production The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Formula: C6H5ClN2O4S

The Article related to multitarget inhibitor leukotriene prostaglandin e2 flap brp7 analog preparation, 5-lipoxygenase, 5-lipoxygenase-activating protein, benzimidazole, inflammation, leukotriene, microsomal prostaglandin e(2) synthase-1 and other aspects.Formula: C6H5ClN2O4S

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

On August 16, 2022, Liang, Chao; Zhang, Shan; Robinson, David; Ploeg, Matthew Vander; Wilson, Rebecca; Nah, Jiemin; Taylor, Dale; Beh, Sheryl; Lim, Radiance; Sun, Lei; Muoio, Deborah M.; Stroud, David A.; Ho, Lena published an article.Product Details of 79-07-2 The title of the article was Mitochondrial microproteins link metabolic cues to respiratory chain biogenesis. And the article contained the following:

Electron transport chain (ETC) biogenesis is tightly coupled to energy levels and availability of ETC subunits. Complex III (CIII), controlling ubiquinol:ubiquinone ratio in ETC, is an attractive node for modulating ETC levels during metabolic stress. Here, we report the discovery of mammalian Co-ordinator of mitochondrial CYTB (COM) complexes that regulate the stepwise CIII biogenesis in response to nutrient and nuclear-encoded ETC subunit availability. The COMA complex, consisting of UQCC1/2 and membrane anchor C16ORF91, facilitates translation of CIII enzymic core subunit CYTB. Subsequently, microproteins SMIM4 and BRAWNIN together with COMA subunits form the COMB complex to stabilize nascent CYTB. Finally, UQCC3-containing COMC facilitates CYTB hemylation and association with downstream CIII subunits. Furthermore, when nuclear CIII subunits are limiting, COMB is required to chaperone nascent CYTB to prevent OXPHOS collapse. Our studies highlight CYTB synthesis as a key regulatory node of ETC biogenesis and uncover the roles of microproteins in maintaining mitochondrial homeostasis. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Product Details of 79-07-2

The Article related to respiratory chain biogenesis mitochondrial microprotein homeostasis, cp: metabolism, cytb, seps, smim4, uqcc1, uqcc2, complex iii, electron transport chain, microproteins, nuclear-mitochondrial coordination, smorfs and other aspects.Product Details of 79-07-2

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

On August 31, 2015, Subbulakshmi, Karanth N.; Narayana, Badiadka; Yathirajan, Hemmige S.; Akkurt, Mehmet; Celik, Oemer; Ersanli, Cem Cueneyt; Glidewell, Christopher published an article.Category: amides-buliding-blocks The title of the article was Dihydrooxazolones and dihydroimidazolones derived from acylglycines: syntheses, molecular structures and supramolecular assembly. And the article contained the following:

Syntheses and structures are described for some alkylidene-substituted dihydrooxazolones and dihydroimidazoles derived from simple acylglycines. A second, triclinic, polymorph of 4-benzylidene-2-(4-methylphenyl)-1,3-oxazol-5(4H)-one, C17H13NO2, (I), has been identified and the structure of 2-methyl-4-[(thiophen-2-yl)methylidene]-1,3-oxazol-5(4H)-one, C9H7NO2S, (II), has been rerefined taking into account the orientational disorder of the thienyl group in each of the two independent mols. The reactions of phenylhydrazine with 2-phenyl-4-[(thiophen-2-yl)methylidene]-1,3-oxazol-5(4H)-one or 2-(4-methylphenyl)-4-[(thiophen-2-yl)methylidene]-1,3-oxazol-5(4H)-one yield, resp., 3-anilino-2-phenyl-5-[(thiophen-2-yl)methylidene]-3,5-dihydro-4H-imidazol-4-one, C10H15N3OS, (III), and 3-anilino-2-(4-methylphenyl)-5-[(thiophen-2-yl)methylidene]-3,5-dihydro-4H-imidazol-4-one, C21H17N3OS, (IV), which both exhibit orientational disorder in their thienyl groups. The reactions of 2-phenyl-4-[(thiophen-2-yl)methylidene]-1,3-oxazol-5(4H)-one with hydrazine hydrate or with water yield, resp., N-[3-hydrazinyl-3-oxo-1-(thiophen-2-yl)prop-1-en-2-yl]benzamide and 2-(benzoylamino)-3-(thiophen-2-yl)prop-2-enoic acid, which in turn react, resp., with thiophene-2-carbaldehyde to form 2-phenyl-5-[(thiophen-2-yl)methylidene]-3-{[(E)-(thiophen-2-yl)methylidene]amino}-3,5-dihydro-4H-imidazol-4-one, C19H13N3OS2, (V), which exhibits orientational disorder in only one of its thienyl groups, and with methanol to give Me (2Z)-2-(benzoylamino)-3-(thiophen-2-yl)prop-2-enoate, C15H13NO3S, (VI). There are no direction-specific intermol. interactions in the crystal structure of the triclinic polymorph of (I), but the mols. of (II) are linked by two independent C-H···O hydrogen bonds to form C 2 2(14) chains. Compounds (III) and (IV) both form centrosym. R 2 2(10) dimers built from N-H···O hydrogen bonds, while compound (V) forms a centrosym. R 2 2(10) dimer built from C-H···O hydrogen bonds. In the structure of compound (VI), a combination of N-H···O and C-H···π(arene) hydrogen bonds links the mols. into sheets. Comparisons are made with some similar compounds The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Category: amides-buliding-blocks

The Article related to dihydrooxazolone dihydroimidazolone acylglycine mol structure supramol assembly, erlenmeyer azlactones, crystal structure, hydrogen bonding, imidazolones, orientational disorder, oxazolones, supramolecular assembly and other aspects.Category: amides-buliding-blocks

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

On January 22, 2015, Bottegoni, Giovanni; De Simone, Alessio; Ruda, Gian Filippo; Cavalli, Andrea; Bandiera, Tiziano; Piomelli, Daniele published a patent.Product Details of 5455-98-1 The title of the patent was Preparation of phenyl carbamates as inhibitors of the fatty acid amide hydrolase (FAAH) enzyme and modulators of the D3 dopamine receptor (D3DR). And the patent contained the following:

Disclosed are compounds I [Ar = aromatic or heteroaromatic single or fused ring comprising heteroatoms selected from N, O and S; R1, R2 = independently H, halo, alkyl, etc.; X = N or CH; Y = -CH2(CH2)nCH2- or -CH2CH:CHCH2- (wherein Y is optionally substituted by B) ; n = 0-3; B = F, OH, CH2OH, etc.; R3 = aromatic or heteroaromatic ring, benzyl, benzoyl (optionally substituted by R5), etc.; R5 = OH, NH2, CN, etc.; R4 = H, halo, alkyl, etc.; or R3 and R4, together with the Ph ring to which they are connected, may form 9H-carbazole ring; or pharmaceutically acceptable salts thereof]. For example, compound II was prepared by following general procedure: to a solution of Boc2O (1.4 equiv) in acetonitrile were added DMAP (1 equiv)/acetonitrile and an amine (1 equiv)/acetonitrile, the resulting mixture was stirred at room temperature for 10 min, treated with an alc. derivative (1.2-1.4 equiv) at room temperature for 22 h, concentrated in vacuo, dissolved in Et acetate, washed with saturated aqueous NaHCO3, dried over Na2SO4, concentrated, and purified. The exemplified compound II exhibited IC50 of 4.4 nM for human FAAH and EC50 of 14.0 nM for D3DR. Compounds I are claimed useful for the treatment of nicotine use disorders, substance abuse addiction, eating diorders, etc. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Product Details of 5455-98-1

The Article related to fatty acid amide hydrolase faah inhibitor phenyl carbamate preparation, d3 dopamine receptor d3dr modulator phenyl carbamate preparation, nicotine eating disorder substance abuse addiction treatment phenyl carbamate and other aspects.Product Details of 5455-98-1

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

Wan, Zhaohua; Wang, Dan; Yang, Zixuan; Zhang, Heng; Wang, Shengchun; Lei, Aiwen published an article in 2020, the title of the article was Electrochemical oxidative C(sp3)-H azolation of lactams under mild conditions.Related Products of 685-91-6 And the article contains the following content:

An electrochem. oxidative direct C(sp3)-H azolation of lactams was reported under metal catalyst-free and external chem. oxidant-free conditions. This electrochem. C(sp3)-H/N-H coupling was characterized by its broad substrate scope of azoles and lactams under mild conditions at room temperature Mechanistic studies suggested that the reaction possibly involves a radical process. Moreover, the site selectivity was explained by DFT calculations More meaningfully, a gram-scale synthesis method of flow electrochem. was employed to show the scaled-up applicability of this transformation. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Related Products of 685-91-6

The Article related to azole lactam electrochem oxidative azolation, azolyl lactam preparation, amide azole electrochem oxidative azolation, amido azole preparation, pyrazole urea electrochem oxidative azolation, pyrazolyl urea preparation and other aspects.Related Products of 685-91-6

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

Zhou, Jiadi; Ren, Quanlei; Xu, Ning; Wang, Chaodong; Song, Shengjie; Chen, Zhi; Li, Jianjun published an article in 2021, the title of the article was K2S2O8-catalyzed highly regioselective amidoalkylation of diverse N-heteroaromatics in water under visible light irradiation.SDS of cas: 685-91-6 And the article contains the following content:

A K2S2O8-catalyzed versatile C(sp2)-C(sp3) bond formation with N-heteroaromatics and γ-lactams/amides was developed. Quinoxalin-2(1H)-one, quinoline, isoquinoline, phthalazine, and benzothiazole reacted with γ-lactams/amides to give the corresponding C(sp2)-H amidoalkylation products in moderate to good yields with high regioselectivity. This visible-light-induced photocatalyst-free reaction was conducted in H2O at ambient temperature, which comply with the principles of “green chem.”. The new K2S2O8 catalytic mechanism was investigated with control experiments The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).SDS of cas: 685-91-6

The Article related to lactam azaarene potassium persulfate catalyst regioselective photochem amidoalkylation, amide azaarene potassium persulfate catalyst regioselective photochem amidoalkylation, amidoalkyl azaarene preparation green chem and other aspects.SDS of cas: 685-91-6

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

On August 31, 2020, Sanad, Sherif M. H.; Mekky, Ahmed E. M. published an article.Recommanded Product: 2-Chloroacetamide The title of the article was Piperazine-mediated tandem synthesis of bis(thieno[2,3-b]pyridines): Versatile precursors for related fused [1,2,4]triazolo[4,3-a]pyrimidines. And the article contained the following:

In this study, the utility of bis(cyanoacetamides) as versatile precursors to the piperazine-mediated synthesis of a wide spectrum of bis(thieno[2,3-b]pyridine) derivatives, linked to aliphatic spacers via thioethers was reported. The proposed tandem protocol involved the reaction of bis(cyanoacetamides) with two equivalent of the appropriate cinnamonitriles in dioxane in the presence of six equivalent of piperazine was refluxed for 4 h which on further addition of halogen-containing reagents afforded bis(thieno[2,3-b]pyridine) derivatives I [Ar = 4-MeOC6H4, 4-ClC6H4; Y = CN, C(O)Me, C(O)NH2, etc.; Z = CH2, (CH2)3]. Compounds I were taken as a key intermediates and reacted with formic acid/acetic anhydride/carbon disulfide afforded bis(oxopyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine) derivatives II [R = H, Me; R1 = CH2, (CH2)3; Ar1 = 4-MeOC6H4, 4-ClC6H4] and III [R2 = CH2, (CH2)3]. Compounds III were reacted with the appropriate hydrazonyl chloride derivatives in dioxane in the presence of triethylamine afforded the corresponding bis([1,2,4]triazoles) with related fused pyridothienopyrimidine moiety IV [R3 = CH2, (CH2)3; Ar2 = Ph, 4-MeC6H4, 4-ClC6H4]. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Recommanded Product: 2-Chloroacetamide

The Article related to bis thienopyridine preparation, cyanoacetamide cinnamonitrile halogen reagent tandem four component piperazine mediated, oxopyridothienopyrimidine bis preparation, acetyl pyridothienotriazolopyrimidine bis preparation and other aspects.Recommanded Product: 2-Chloroacetamide

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

Kakeya, Nobuharu; Yata, Noboru; Kamada, Akira; Aoki, Masaru published an article in 1970, the title of the article was Biological activities of drugs. IX. Structure-activity relation of sulfonamide carbonic anhydrase inhibitors. 4.Application In Synthesis of 3-Nitro-4-chlorobenzenesulfonamide And the article contains the following content:

Hansch-Fujita’s equation has been applied to an anal. of the natriuretic activity of sulfonamide carbonic anhydrase inhibitors using π and πc as hydrophobic parameters, and σ, ΔpKa, Δppm and Δfr as electronic parameters. Sixteen benzenesulfonamide derivatives were satisfactorily applied to the structure-activity anal. of heterocyclic sulfonamides. It was concluded that a strong natriuretic activity was observed for sulfonamides which had an optimal hydrophobicity and low electronegativity at the sulfamoyl group or a strong inhibitory activity against carbonic anhydrase. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Application In Synthesis of 3-Nitro-4-chlorobenzenesulfonamide

The Article related to structure activity sulfonamides antienzymic, activity structure sulfonamides antienzymic, sulfonamides antienzymic structure activity, antienzymic sulfonamides structure activity, carbonic anhydrase inhibitor structure and other aspects.Application In Synthesis of 3-Nitro-4-chlorobenzenesulfonamide

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

On May 4, 2012, Hou, Wenduan; Zheng, Bo; Chen, Jun; Peng, Yungui published an article.COA of Formula: C15H15F3N2O2S The title of the article was Asymmetric Synthesis of Polysubstituted 4-Amino- and 3,4-Diaminochromanes with a Chiral Multifunctional Organocatalyst. And the article contained the following:

A series of multifunctional catalysts with two chiral diaminocyclohexane units were developed and successfully applied in the asym. oxa-Michael-aza-Henry cascade reaction of salicylaldimines with nitroolefins. This approach provides a simple and efficient entry to polysubstituted chiral 4-aminobenzopyrans with three consecutive stereocenters and in high yield (up to 97%) with excellent stereoselectivity (up to 98% ee and >99:1 dr). Facile access to the nonsym. optically pure 3,4-diaminochromanes was also obtained. The experimental process involved the reaction of N-[(1S,2S)-2-Amino-1,2-diphenylethyl]-1,1,1-trifluoromethanesulfonamide(cas: 167316-28-1).COA of Formula: C15H15F3N2O2S

The Article related to nitroolefin salicylaldimine chiral diaminocyclohexane thiourea asym michael henry, aminochromane stereoselective preparation, chiral diaminocyclohexane thiourea enantioselective diastereoselective michael henry catalyst and other aspects.COA of Formula: C15H15F3N2O2S

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

On June 25, 2009, Liu, Julie published a patent.Reference of (S)-2-Hydroxy-N-methyl-2-phenylacetamide The title of the patent was Preparation of tetrahydroisoquinoline derivatives as orexin receptor antagonists. And the patent contained the following:

This title compounds with general formula I [wherein each Z is independently selected from hydrogen or deuterium; each R is independently selected from CD3, CD2H, CDH2, or CH3, and when each R is CH3 then at least one Z is deuterium] or pharmaceutically acceptable salts thereof were prepared as dual OX-1/OX-2 orexin receptor antagonists for the treatment of obesity, bulimia, anorexia nervosa, insomnia, narcolepsy, sleep apnea, jet-lag syndrome, or memory impairment. For example, compound II·HCl was prepared in a multi-step synthesis, with the last step being the condensation of (1S)-[1,2,3,4-tetrahydro-3,3,4,4-d4]-[6,7-dimethoxy-d6]-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-isoquinoline hydrochloride (preparation given) and toluene-4-sulfonic acid [(S)-1-[(methyl-d3)carbamoyl]-1-phenylmethyl] ester (preparation given). The metabolic stability of compounds I has been tested using pooled liver microsomal incubation. The experimental process involved the reaction of (S)-2-Hydroxy-N-methyl-2-phenylacetamide(cas: 65645-88-7).Reference of (S)-2-Hydroxy-N-methyl-2-phenylacetamide

The Article related to preparation tetrahydroisoquinoline orexin receptor antagonist treatment eating disorder sleep, treatment obesity bulimia anorexia nervosa insomnia narcolepsy sleep apnea, human jet lag syndrome memory impairment treatment and other aspects.Reference of (S)-2-Hydroxy-N-methyl-2-phenylacetamide

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