Tag: M.W:200-300

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Stereoselective Synthesis of Cyclohepta[b]indoles by Visible-Light-Induced [2+2]-Cycloaddition/retro-Mannich-type Reactions, the main research direction is pyrrolocycloheptaindole stereoselective preparation; iridium photocatalyst tandem cycloaddition retro Mannich reaction indolylalkyl enaminone; stereoselective photochem cycloaddition retro Mannich reaction indolylalkyl enaminone; [2+2]/retro-Mannich-type cycloaddition; amine radical cation; cyclohepta[b]indole; photoredox catalysis.HPLC of Formula: 7524-52-9.

A novel method for the concise synthesis of cyclohepta[b]indoles in high yields was developed. The method involves a visible-light-induced, photocatalyzed [2+2]-cycloaddition/ retro-Mannich-type reaction of enaminones such as I to yield cycloheptaindoles such as II. Exptl. and computational studies suggested that the reaction is a photoredox process initiated by single-electron oxidation of enaminones, which undergo subsequent cyclobutane formation and rapid fragmentation of the intermediate radical cations to form cyclohepta[b]indoles.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called I+/TBHP Catalysis For Tandem Oxidative Cyclization To Indolo[2,3-b]quinolines, published in 2021-01-31, which mentions a compound: 7524-52-9, mainly applied to indoloquinoline preparation chemoselective; indole aniline sulfonamide tandem oxidative cyclization tetrabutylammonium iodide catalyst, Application In Synthesis of H-Trp-OMe.HCl.

A chemoselective tandem oxidative cyclization/aromatization of indole derivatives tethered to aniline sulfonamides using catalytic amount of tetrabutylammonium in the presence of tert-Bu hydroperoxide (TBHP) as an oxidant under nearly neutral conditions at room temperature is reported. The corresponding indolo[2,3-b]quinolines were obtained as sulfonate salts, which could be easily isolated in anal. pure form via only a simple filtration of the crude reaction mixture The natural product quinindoline could be easily obtained after basic work-up of the sulfonate salt. Control experiments revealed that both ionic and radical active species could be generated in situ under mild conditions for the corresponding oxidative transformations to proceed in a chemoselective manner.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Safety of H-Trp-OMe.HCl. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Synthesis, molecular docking and biological evaluation of some new benzotriazines. Author is El Rayes, Samir M.; Ali, Ibrahim A. I.; Fathalla, Walid; Mahmoud, Mostafa A. A..

Me 2-(4-oxobenzotriazin-3(4H)-yl)alkanoates I [X = CH2, CH2CH2, CH(i-Pr); X1 = MeO] proved to be important intermediates for the preparation of some biol. interesting compounds containing the benzotriazinone ring system. The above compounds were prepared by direct diazotization of Me anthranilate followed by addition of amino acid esters hydrochloride in a one-pot strategy. An equivocal synthesis of compound I (X = CH2; X1 = MeO) was achieved by alkylation of benzotriazin-4(3H)-one with Me chloroacetate. A series of N-alkyl-2-(4-oxobenzotriazin-3(4H)-yl) alkanamides I (X = CH2, CH2CH2; X1 = NR1R2; R1 = i-Pr, n-Bu, t-Bu, cyclohexyl, etc., R2 = H; R1R2N = 1-piperidinyl, 4-morpholinyl) and Me 2-(2-(4-oxobenzotriazin-3(4H)-yl)alkanamido)alkanoates (dipeptides) I [X = CH2, CH2CH2; X1 = NHR3; R3 = MeO2CCH2, MeO2CCH(i-Bu), MeO2C(CH2)3, MeO2CCH(indol-3-ylmethyl)] were prepared via azide coupling from compounds I (X = CH2, CH2CH2; X1 = MeO). Esters I (X = CH2, CH2CH2; X1 = MeO) were converted into the corresponding hydrazides followed by condensation with aldehydes, such as 4-methoxybenzaldehyde, 4-dimethylaminobenzaldehyde and arabinose, to afford the corresponding hydrazone derivatives. All the synthesized compounds were subjected to the mol. docking using MOE 2008-10 software as agonists for E. coli Fab-H receptor and Vitamin D receptor for antibacterial and anticancer evaluation, resp. The most pronounced strong binding affinity towards the target E. coli Fab-H receptor was shown by the parent benzotriazin-4(3H)-one and compounds I [X = CH2, X1 = i-PrNH; X = CH2CH2, X1 = MeO2CCH2, MeO2C(CH2)3; X = CH2, X1 = 4-MeOC6H4CH:NN, 4-Me2NC6H4CH:NN; X = CH2CH2, X1 = 4-Me2NC6H4CH:NN]. On the other hand, the most pronounced strong binding affinity towards the target Vitamin D receptor were benzotriazin-4(3H)-one and compounds I [X = CH2, X1 = MeO2C(CH2)3; X = CH2CH2, X1 = MeO2CCH(indol-3-ylmethyl); X = CH2, X1 = 4-MeOC6H4CH:NN]. The in-vitro antibacterial activity of highest binding affinity docked compounds were tested against E. coli, Staphylococcus aureus and Salmonella spp. All the tested compounds gave effective pos. results against E. coli with inhibitory zone of about 1.1 cm, while were inactive against Staphylococcus aureus and Salmonella spp. The in-vitro cytotoxic activity of the highest binding affinity docked compounds were tested against human liver carcinoma cell line (HepG2) cancer cell lines. Many compounds showed potent cytotoxic activity with low IC50 values, especially benzotriazin-4(3H)-one (6.525μM) and I (X = CH2; X1 = 4-MeOC6H4CH:NN) (10.97μM) compared to standard drug doxorubicin (5.8μM).

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Synthesis of Four Optical Isomers of Antiviral Agent NK0209 and Determination of Their Configurations and Activities against a Plant Virus, the main research direction is NK0209 isomer preparation antiviral tobacco mosaic virus antiviral; NK0209; antiviral activity; isomers; spatial configuration; synthesis.Related Products of 7524-52-9.

Previously, we reported for the first time that harmala alkaloids harmine and tetrahydroharmine exhibit activity against plant viruses, and we developed an analog, designated NK0209, that efficiently prevents and controls plant virus diseases. Here, to investigate the influence of the spatial configuration of NK0209 on its antiviral activities, we synthesized its four optical isomers, determined their configurations, and evaluated their activities against tobacco mosaic virus. All four isomers were significantly more active than ningnanmycin, which is one of the most successful com. antiviral agents, with in vivo inactivation, cure, and protection rates of 57.3±1.9%, 54.2±3.3%, 55.0±4.1% at 500μg/mL. Furthermore, anal. of structure-activity relationships demonstrated for the first time that the spatial conformation of NK0209 is an important determinant of its antiviral activity, and our results provide information about the possible optimum configuration for interaction of this mol. with its target protein.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Application of 7524-52-9. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about A fast and direct iodide-catalyzed oxidative 2-selenylation of tryptophan. Author is Gao, Yu-Ting; Liu, Shao-Dong; Cheng, Liang; Liu, Li.

A metal-free 2-selenylation of tryptophan derivatives is reported, where the use of iodide as the catalyst and oxone as the oxidant is key to obtain high yields. Various functional groups within the di-selenyl and the indole ring are tolerated, and no racemization is generally observed

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Biosynthesis of penicillins. VI. N-2-Hydroxyethyl amides of some polycyclic and heterocyclic acetic acids as precursors》. Authors are Jones, Reuben G.; Soper, Quentin F.; Behrens, Otto K.; Corse, Joseph W..The article about the compound:2-Bromo-6-(bromomethyl)naphthalenecas:305798-02-1,SMILESS:BrCC1=CC2=CC=C(Br)C=C2C=C1).Reference of 2-Bromo-6-(bromomethyl)naphthalene. Through the article, more information about this compound (cas:305798-02-1) is conveyed.

2,6-MeC10H6NH2 (78 g.) in 80 mL. concentrated HCl and 200 mL. H2O at 0°, treated at 5° with 35 g. NaNO2 in 50 mL. H2O and, after 0.5 h., with 130 g. ice-cold 42% HBF4, gives 90% of the 2-diazonium fluoroborate, decomposition of which yields 69% 2-methyl-6-fluoronaphthalene (I), m. 77°. I (40 g.) at 210°, treated (15 min.) with 40 g. Br (with illumination with a 100-w. lamp), gives 82% 2-(bromomethyl)-6-fluoronaphthalene (II), b2 125-30°, m. 53°. II (48 g.), added to a refluxing solution of 30 g. KCN in 60 mL. H2O and 200 mL. EtOH, the EtOH removed after refluxing 4 h., 500 mL. H2O added, the solution extracted with ether, and the residue from the ether boiled 5 h. with 40 g. KOH in 40 mL. H2O and 200 mL. EtOH, gives 74% 6-fluoro-2-naphthaleneacetic acid, m. 138-9° (Me ester, b2 163-6°, m. 48-9°). 2,6-MeC10H6NH2 (63 g.) in 100 mL. H2O and 700 g. 48% HBr, treated (3-4 h.) at 5° with 45 g. NaNO2 in 75 mL. H2O and the diazonium solution poured (10 min.) into 170 g. CuBr in 800 mL. 48% HBr at 70-80°, gives 40% 6-bromo-2-methylnaphthalene (III), m. 142° III yields 80% 6-bromo-2-(bromomethyl)naphthalene, m. 124-5° this gives 69% 6-bromo-2-naphthaleneacetic acid, m. 175-6° (Me ester, b2 187-93°, m. 67-9°). 3,2-ClC10H6CHO (32.5 g.), 35 g. hippuric acid, 14.5 g. anhydrous AcONa, and 50 mL. Ac2O, heated on the steam bath 1 h., give 75% 2-phenyl-4-(3-chloro-2-naphthylmethylene)-5(4H)-oxazolone (IV), bright yellow, m. 192° 40 g. IV in 200 mL. 10% NaOH, refluxed 9 h., the mixture diluted to 1500 mL. with H2O, washed with ether, the aqueous solution treated with 20 mL. 12.5 N NaOH and 15 mL. 30% H2O2, allowed to stand overnight, the filtrate acidified with HCl, extracted with ether-C6H6, and the residue esterified, gives 37% Me 3-chloro-2-naphthaleneacetate, b2 163-5°, m. 49-50° the free acid m. 193-4°. 6,2-MeOC10H6Ac (100 g.), 25.5 g. S, and 87 g. morpholine, heated 18 h. at 140°, part of the morpholine removed in vacuo, 250 mL. AcOH and 350 mL. concentrated HCl added, and the mixture refluxed 24 h., give 67% 6-methoxy-2-naphthaleneacetic acid, m. 203-5° (Me ester, b1 192-3°, m. 86°, 73%). 5,6,7,8-Tetrahydro-2-acetonaphthone (50 g.), 13 g. S, and 40 mL. morpholine, refluxed overnight, 400 mL. concentrated HCl and 300 mL. H2O added, and the mixture again refluxed overnight, followed by esterification with EtOH and H2SO4, give Et 5,6,7,8-tetrahydro-2-naphthaleneacetate, b0.5 140-3°. 2-Acetylphenanthrene (13.2 g.), 3.2 g. S, and 10.5 g. morpholine, heated 15 h. at 160°, the mixture treated with 150 mL. AcOH and 36% HCl, and refluxed 24 h., give 81% 2-phenanthreneacetic acid, m. 187-8° the 3-isomer m. 174-5°, 84% (Me ester, b1.5 203-5°, 89%). 8-(Bromomethyl)quinoline (120 g.) in 250 mL. warm EtOH, added (0.5 h.) to 50 g. KCN in 100 mL. warm H2O and the mixture refluxed 1.5 h., gives 78% 8-(cyanomethyl)quinoline, m. 86-7°; hydrolysis with aqueous alc. KOH and esterification give 91% Et 8-quinolineacetate, b3 158-60°. Et 3-quinolinecarboxylate (70 g.), 62 g. AcOEt, and EtONa (12 g. Na and 0.52 mol absolute EtOH) in 100 cc. dry C6H6, refluxed 20 h., the cooled solution poured onto ice, diluted to 5 l. with H2O, treated with 50 mL. 12 N NaOH, washed with two 300 mL. portions of ether, and the aqueous solution neutralized with dilute H2SO4 and extracted with two 500-mL. portions of ether, give 75% Et 3-quinolylformylacetate, m. 84° 27 g. of the keto ester in 125 g. 25% H2SO4, heated 30 min. at 100°, gives 95% 3-acetylquinoline (V). V (7 g.), 5 g. S, 50 mL. (NH4)2S, and 25 mL. H2O, heated 20 h. at 145-50°, the residue extracted with two 300-mL. portions boiling 5% HCl, the solution refluxed 3 h., and the crude acid esterified, give 19% Et 3-quinolineacetate, b2.5 140-2°. pH2NC6H4CH2CO2H (46 g.), 10.5 g. FeSO4, 115 g. C3H5(OH)3, 23 g. PhNO2, and 53 mL. concentrated H2SO4, boiled 5 h., give 37 g. crude acid which, esterified with EtOH and HCl, gives 39% Et 6-quinolineacetate, b3 160° the free acid (VI) m. 218-20°. Et 6-quinolinecarboxylate and AcOEt, condensed with EtONa, give 87% Et 6-quinolineacetate, hydrolysis of which with 25% H2SO4 at 100° gives 90% 6-acetylquinoline, m. 76° the Willgerodt reaction gives 87.5% VI. 3,4 O2N(H2N)C6H3CO2H (108 g.) in 350 mL. concentrated HCl, treated with 125 g. Sn in portions (temperature below 90°), gives 87% (3,4-diaminophenyl)acetic acid-2HCl (VII), m. 222-4° (decomposition); Et ester-2HCl (VIII), m. 185-7° (decomposition); 3 g. VII and 20 mL. 98-100% HCO2H, heated several hrs., give 100% 5-benzimidazoleacetic acid-HCl, m. 240-2° the Et ester m. 65-6°, 75%. VIII (14 g.) in 200 mL. ice H2O, treated with excess COCl2, gives 95% Et 2-hydroxy-5-benzimidazoleacetate, m. 208-9°. NCCH2CO2Et (113 g.) and 15 g. (HOCH2CH2)3N in 100 mL. absolute EtOH, treated with a slow stream of H2S, the mixture poured after 5 days into ice-H2O, and 38 g. of the resulting oil and 23.1 g. ClCH2Ac in 300 cc. anhydrous ether kept 4 days, give 20.6 g. Et 4-methyl-2-thiazoleacetate, b17 136-9°. Thiaxanthydrol (42 g.), 30 g. CH2(CO2H)2, and 80 mL. C5H5N, heated 2 h. at 60-70° and 2 h. at 90-5° and the liquid poured into 600 mL. 2 N HCl, give 90% 9-thiaxantheneacetic acid, m. 167-8° (Me ester, b2 182-4°). The Ag salt of 2-benzylimidazole (53 g.) and 50 g. BrCH2CO2Et in 200 mL. xylene, refluxed 48 h., give 25.4% of the Et ester, m. 70-70.5°, of 2-benzyl-1-imidazoleacetic acid, m. 173-4°. Me 1-acenaphtheneacetate, b4 176-8°. N-2-Thienylacetyl-DL-valine m. 110-12°. Amides were prepared by heating the Me or Et ester of the various acids with a slight excess of HOCH2CH2NH2 at 100-150° for several hrs.; R in RCH2CONHCH2CH2OH is given, together with S (see part V). 2-C10H7 m. 125-7°, S 1.3; 1-bromo-2-naphthalene m. 155-6°, S 0.5; 6-fluoro-2-naphthalene m. 145-6°, S 1.2; 3-chloro-2-naphthalene m. 150-1°, S 0.3; 6-bromo-2-naphthalene m. 167-8°, S 0.9; 5,6,7,8-tetrahydro-2-naphthalene m. 88-90°, S 0.9; 1-nitro-2-naphthalene m. 154-5°, S 0.9; 6-methoxy-2-naphthalene m. 160°, S 1.1; 1-acenaphthene m. 160°, S 1.1; 9-fluorene m. 127-8°, S 0.7; 2-phenanthrene m. 135-7°, S 0.5; 3-isomer m. 133-5°, S 0.5; 1-pyrrole m. 85-7°, S 0.9; 2-thiophene m. 66-7°, S 1.8; 2-furan oil, S 0.4; 2,6-dihydroxy-5-pyrimidine m. 271-2°, S 1; 2-methyl-4-hydroxy-5-pyrimidine m. 184°, S 0.9; 3,4-methylenedioxyphenyl m. 99-100°, S 1; 2-methyl-4-thiazole m. 93-4°, S 0.85; 4-methyl-2-thiazole m. 80-2°, S 0.9; 2-pyridine m. 93-4°, S 1; 3-isomer m. 94° S 1; 6-methyl-2-pyridine m. 49-50°, S 1; 2-benzyl-1-imidazole m. 177-9°, S 1; 3-quinoline m. 151-2°, S 1; 6-isomer m. 135°, S 1; 8-isomer m. 92-3°, S 1; 2-benzimidazole m. 185-90°, S 1; 5-isomer m. 160-2°, S 1; 2-hydroxy-5-benzimidazole m. 245-6°, S 1; 7-hydroxy-4-coumarin m. 114-16°, S 1; 9-xanthene m. 157-8°, S 0.8; 9-thiaxanthene m. 148-9°, S 0.7; 5-hydantoin m. 160-2°, S 0.9. Only a few of these compounds appeared to be utilized readily by the mold for the formation of new penicillins. Several of the compounds appeared to effect some increase in penicillin yield or to change the differential assay value of the crude penicillin produced in their presence.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Chan, Hwai-Chien; Bueno, Bianca; Le Roch, Adrien; Gagnon, Alexandre published the article 《Copper-promoted N-arylation of the imidazole side chain of protected histidine by using triarylbismuth reagents》. Keywords: dipeptide arylated histidine synthesis functional group; histidine imidazole arylation copper catalyst triarylbismuth reagent; arylation reaction mechanism; N-arylation; copper catalysis; histidine; imidazole; organobismuthines.They researched the compound: H-Trp-OMe.HCl( cas:7524-52-9 ).SDS of cas: 7524-52-9. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:7524-52-9) here.

The N-arylation of the side chain of histidine by using triarylbismuthines is reported. The reaction is promoted by copper(II) acetate in dichloromethane at 40°C under oxygen in the presence of diisopropylethylamine and 1,10-phenanthroline and allows the transfer of aryl groups with substituents at any position of the aromatic ring. The reaction shows excellent functional group tolerance and is applicable to dipeptides where the histidine is located at the N terminus. A histidine-guided backbone N-H arylation was observed in dipeptides where the histidine occupies the C terminus.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Journal of Medicinal Chemistry called Antiparasitic thiocyanatobenzothiazoles, Author is Alaimo, Robert J.; Pelosi, Stanford S.; Hatton, Christopher J.; Gray, Joseph E., which mentions a compound: 25150-27-0, SMILESS is NC1=NC2=CC=C(Cl)C(Cl)=C2S1, Molecular C7H4Cl2N2S, Electric Literature of C7H4Cl2N2S.

A series of 7 title compound was prepared by the reaction of the appropriate aniline derivative with thiocyanogen [505-14-6] generated in situ followed by thermal cyclization. The activity of 2-amino-6-ethyl-4-thiocyanatobenzothiazole (I) [37069-20-8] against Ascaris suum and Hymenolepis nana in mice was comparable to that of dl-tetramisole [5036-02-2] and bunamidine [3748-77-4], resp. 2-Amino-7-chloro-6-fluoro-4-thiocyanatobenzothiazole (II) [37525-33-0] and 2-amino-6,7-dichloro-4-thiocyanatobenzothiazole (III) [37069-18-4] were active in vitro against several yeast species, including Candida albicans and Microsporum canis.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Quality Control of H-Trp-OMe.HCl. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about A new class of α-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities. Author is Wang, Juan; Liang, Boqiang; Chen, Yiling; Fuk-Woo Chan, Jasper; Yuan, Shuofeng; Ye, Hui; Nie, Linlin; Zhou, Jiao; Wu, Yi; Wu, Meixian; Huang, Lina S.; An, Jing; Warshel, Arieh; Yuen, Kwok-Yung; Ciechanover, Aaron; Huang, Ziwei; Xu, Yan.

Inhibitors of the proteasome have been extensively studied for their applications in the treatment of human diseases such as hematol. malignancies, autoimmune disorders, and viral infections. Many of the proteasome inhibitors reported in the literature target the non-primed site of proteasome′s substrate binding pocket. In this study, we designed, synthesized and characterized a series of novel α-keto phenylamide derivatives aimed at both the primed and non-primed sites of the proteasome. In these derivatives, different substituted Ph groups at the head group targeting the primed site were incorporated in order to investigate their structure-activity relationship and optimize the potency of α-keto phenylamides. In addition, the biol. effects of modifications at the cap moiety, P1, P2 and P3 side chain positions were explored. Many derivatives displayed highly potent biol. activities in proteasome inhibition and anticancer activity against a panel of six cancer cell lines, which were further rationalized by mol. modeling analyses. Furthermore, a representative α-ketoamide derivative was tested and found to be active in inhibiting the cellular infection of SARS-CoV-2 which causes the COVID-19 pandemic. These results demonstrate that this new class of α-ketoamide derivatives are potent anticancer agents and provide exptl. evidence of the anti-SARS-CoV-2 effect by one of them, thus suggesting a possible new lead to develop antiviral therapeutics for COVID-19.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Lu, Meng-Chen; Zhang, Xian; Wu, Feng; Tan, Shi-Jie; Zhao, Jing; You, Qi-Dong; Jiang, Zheng-Yu published an article about the compound: H-Trp-OMe.HCl( cas:7524-52-9,SMILESS:N[C@@H](CC1=CNC2=CC=CC=C12)C(OC)=O.[H]Cl ).Safety of H-Trp-OMe.HCl. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:7524-52-9) through the article.

The transcription factor Nrf2 is a key regulator of cytoprotective system, and enhancing Nrf2 activity can protect cells from various insults and threats. Directly disrupting Keap1-Nrf2 protein-protein interactions has been regarded as a promising way to activate Nrf2. We reported here the first identification of amino acids as preferred substituents to design potent Keap1-Nrf2 inhibitors. Comprehensive structure-activity anal. identified Pro as a preferred substituent, obtaining a potent inhibitor 35 with an IC50 of 43 nM in the competitive fluoresce polarization (FP) assay and a Kd value of 53.7 nM for Keap1 protein in the isothermal titration calorimetry (ITC) assay. The Pro analog 35 exhibited tight and prolonged Keap1 binding in vitro and in cells, and treatment with 35 activated Nrf2-regulated cytoprotective response and antagonized acetaminophen-induced liver injury both in cellular and in vivo models. This work not only provides a useful tool to further explore the therapeutic potential of Keap1-Nrf2 inhibition but also enriches the diversity of chem. structures suitable for the Keap1-Nrf2 interface.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem