Month: November 2022

Kim, Younggyu published the artcileNonradioactive, ultrasensitive site-specific protein-protein photocrosslinking: interactions of α-helix 2 of TATA-binding protein with general transcription factor TFIIA and transcriptional repressor NC2, Computed Properties of 359860-27-8, the publication is Nucleic Acids Research (2008), 36(19), 6143-6154, database is CAplus and MEDLINE.

The authors have developed an approach that enables nonradioactive, ultrasensitive (attamole sensitivity) site-specific protein-protein photocrosslinking, and we have applied the approach to the anal. of interactions of α-helix 2 (H2) of human TATA-element binding protein (TBP) with general transcription factor TFIIA and transcriptional repressor NC2. TBP H2 can be crosslinked to TFIIA in the TFIIA-TBP-DNA complex and in higher order transcription-initiation complexes, and the crosslink was mapped to the ‘connector’ region of the TFIIA α/β subunit (TFIIAα/β). Furthermore, TBP H2 can be crosslinked to NC2 in the NC2-TBP-DNA complex, and the crosslink was mapped to the C-terminal ‘tail’ of the NC2 α-subunit (NC2α). Interactions of TBP H2 with the TFIIAα/β connector and the NC2α C-terminal tail were not observed in crystal structures of TFIIA-TBP-DNA and NC2-TBP-DNA complexes, since relevant segments of TFIIA and NC2 were not present in truncated TFIIA and NC2 derivatives used for crystallization The authors propose that interactions of TBP H2 with the TFIIAα/β connector and the NC2α C-terminal tail provide an explanation for genetic results suggesting importance of TBP H2 in TBP-TFIIA interactions and TBP-NC2 interactions, and provide an explanation – steric exclusion – for competition between TFIIA and NC2.

Nucleic Acids Research published new progress about 359860-27-8. 359860-27-8 belongs to imidazoles-derivatives, auxiliary class Other Aliphatic Heterocyclic,Chiral,Amine,Amide,Ether,Inhibitor, name is N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, and the molecular formula is C18H34N4O5S, Computed Properties of 359860-27-8.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Algul, Oztekin published the artcileSynthesis and evaluation of antimicrobial activity of some 1,5(6)-H/or -methyl-2-substituted benzimidazole derivatives, COA of Formula: C9H10N2O, the publication is Asian Journal of Chemistry (2007), 19(4), 3085-3092, database is CAplus.

Benzimidazoles I (R = CH₂OH, CH₂NH₂, Me, Et, CH₂SH; R¹, R² = H, Me) were prepared by cyclocondensation of 1,2-benzenediamines with RCO₂H, followed, in some cases, by methylation with MeI. These compounds were tested in vitro against three Gram pos. (Enterococcus faecalis, Staphyloccus aureus and Staphyloccus epidermidis) and two Gram neg. bacteria (Escherichia coli, Pseudomonas aeruginosa). In addition, they were screened in vitro for their antifungal activities. All these compounds inhibited the growth of Gram pos. and Gram neg. bacteria at MIC values between 12.5 and 200 μg/mL and had MIC values between 50 and 200 μg/mL for the following fungi (Candida albicans, Candida krusei, Candida glabrata, Candida tropicalis and Candida parapsilosis).

Asian Journal of Chemistry published new progress about 7467-35-8. 7467-35-8 belongs to imidazoles-derivatives, auxiliary class Benzimidazole,Alcohol, name is (1-Methyl-1H-benzo[d]imidazol-2-yl)methanol, and the molecular formula is C9H10N2O, COA of Formula: C9H10N2O.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Carini, David J. published the artcileNonpeptide angiotensin II receptor antagonists: the discovery of a series of N-(biphenylylmethyl)imidazoles as potent, orally active antihypertensives, Formula: C8H13ClN2O, the publication is Journal of Medicinal Chemistry (1991), 34(8), 2525-47, database is CAplus and MEDLINE.

Nonpeptide angiotensin II receptor antagonists I (R = CH₂OH, CH₂OMe, CHO; R¹ = tetrazolyl, (un)substituted triazolyl, CO₂H, CONHR², R² = OH, OMe, OCH₂Ph, SO₂Ph, NHSO₂CF₃, COCF₃, SO₂CF₃) were prepared and produced a potent antihypertensive effect upon oral administration. The acidic group at the 2′-position of the biphenyl is essential. Only ortho-substituted acids possess both high affinity for the AII receptor and good oral antihypertensive potency. The carboxylic acid group has been replaced with a variety of acidic isosteres, and the tetrazole ring was the most effective.

Journal of Medicinal Chemistry published new progress about 79047-41-9. 79047-41-9 belongs to imidazoles-derivatives, auxiliary class Imidazole,Chloride,Alcohol, name is (2-Butyl-4-chloro-1H-imidazol-5-yl)methanol, and the molecular formula is C8H13ClN2O, Formula: C8H13ClN2O.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Carini, David J. published the artcilePart VI. Nonpeptide angiotensin II receptor antagonists: N-[(benzyloxy)benzyl]imidazoles and related compounds as potent antihypertensives, Application of (2-Butyl-4-chloro-1H-imidazol-5-yl)methanol, the publication is Journal of Medicinal Chemistry (1990), 33(5), 1330-6, database is CAplus and MEDLINE.

A series of title compounds (I, R¹ = Bu, SEt, SPr; R² = H, Cl, CH₂OH, CH₂OAc; R³ = CH₂OH, Cl, CH₂OAc, CH₂NHCO₂Me; R⁴ = CO₂H, NHSO₂CF₃; X = NHCO, CO, O, S, OCH₂ etc.; n = 0-1) was synthesized and demonstrated to be antagonists of the angiotensin II (AII) receptor. I are structurally related to the N-(benzamidobenzyl)imidazoles and extend the scope of this new class of nonpeptide AII antagonists. The amide linkage (X = NHCO) in the N-(benzamidobenzyl)imidazoles can be replaced successfully by a variety of groups (X = O, S, CO, OCH₂, CH:CH, NHCONH; n = 0-1); linkers of 0-1 atoms in length are most effective. When administered i.v. to awake renal hypertensive rats, these compounds exhibited potent antihypertensive activity.

Journal of Medicinal Chemistry published new progress about 79047-41-9. 79047-41-9 belongs to imidazoles-derivatives, auxiliary class Imidazole,Chloride,Alcohol, name is (2-Butyl-4-chloro-1H-imidazol-5-yl)methanol, and the molecular formula is C8H13ClN2O, Application of (2-Butyl-4-chloro-1H-imidazol-5-yl)methanol.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Srinivas, K. published the artcilePEG-600: a facile, eco-friendly, reaction medium for synthesis of 1-(arylsulfonyl) aryl/heteroarylmethanes, Synthetic Route of 4760-35-4, the publication is Chemica Sinica (2013), 4(3), 36-40, 5 pp., database is CAplus.

Reaction of arylmethyl/heteroaryl Me chlorides 1 with aryl sulfinate sodium salts 2 yields the corresponding sulfone derivatives promoted by polyethylene glycol-600 at room temperature

Chemica Sinica published new progress about 4760-35-4. 4760-35-4 belongs to imidazoles-derivatives, auxiliary class Chloride,Benzimidazole, name is 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, and the molecular formula is C7H9NO5S, Synthetic Route of 4760-35-4.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Srinivas, K. published the artcileZinc-mediated tandem-one-pot facile synthesis of 1-(arylsulfonyl) aryl/hetaryl methanes: A case of C-S bond formation, Safety of 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, the publication is Synthetic Communications (2011), 41(11), 1584-1592, database is CAplus.

Reaction of (arylmethyl)/(hetarylmethyl)zinc chloride, generated in situ from arylmethyl- and hetarylmethyl chloride., resp., and Zn, with arylsulfonyl chlorides in THF under mild conditions (i.e., at room temperature) furnished the corresponding 1-(arylsulfonyl)aryl/hetarylmethanes in good yields.

Synthetic Communications published new progress about 4760-35-4. 4760-35-4 belongs to imidazoles-derivatives, auxiliary class Chloride,Benzimidazole, name is 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, and the molecular formula is C7H10N2O2, Safety of 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Srinivas, K. published the artcileTriethanolamine: a resourceful, reusable, eco-friendly, reaction medium for phase transfer catalyst – free synthesis of 1-(arylsulfonyl)aryl/heterylmethanes, Formula: C9H9ClN2, the publication is Chemical Science Transactions (2014), 3(1), 375-381, 7 pp., database is CAplus.

Synthesis of sulfone derivatives I (R = X = H, CH₃; Ar = 4-CH₃C₆H₄, C₆H₅) from reaction of arylmethyl/heteryl Me chloride with aryl sulfinate sodium salt NaO-S(O)-Ar at room temperature as the eco-friendly solvent in good to excellent yields.

Chemical Science Transactions published new progress about 4760-35-4. 4760-35-4 belongs to imidazoles-derivatives, auxiliary class Chloride,Benzimidazole, name is 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, and the molecular formula is C30H32ClN7O2, Formula: C9H9ClN2.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Rao, S. Srinivas published the artcileSynthesis of N,N¹-(dialkyl)-bisbenzimidazole sulphides of potential pharmacological interest, Product Details of C9H9ClN2, the publication is Indian Journal of Heterocyclic Chemistry (2013), 22(3), 243-248, database is CAplus.

Condensation of 2-chloromethylbenzimidazole with 2-mercaptobenzimidazole in MeOH using Et₃N as a base under reflux for 3 h yielded 2-(thiomethyl-2¹-benzimidazolyl) benzimidazole which on alkylation using two equivalent of alkylating agent in DMF as solvent and K₂CO₃ as a base using Bu₄NBr as phase transfer catalyst gave N,N¹-dialkylbisbenzimidazolesulfides. Alternatively, N,N¹-dialkylbisbenzimidazolesulfides could also be prepared by condensing N-alkyl-2-chloromethylbenzimidazole and N-alkyl-2-mercaptobenzimidazole in a single step. Using this synthetic strategy, N,N¹-unsymmetricallydialkylbisbenzimidazolesulfides were prepared either by condensing 2-chloromethylbenzimidazole with N¹-alkyl-2-mercaptobenzimidazoles under PTC conditions or by condensing 1-alkyl-2-chloromethylbenzimidazoles with N-unsubstituted-2-mercaptobenzimidazole, under PTC conditions too. Direct condensation of N-substituted-2-chloromethylbenzimidazoles with N¹-alkyl-2-mercaptobenzimidazoles also gave the products.

Indian Journal of Heterocyclic Chemistry published new progress about 4760-35-4. 4760-35-4 belongs to imidazoles-derivatives, auxiliary class Chloride,Benzimidazole, name is 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, and the molecular formula is C9H9ClN2, Product Details of C9H9ClN2.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Kumar, N. D. Mahesh published the artcile“D-Glucose” phase transfer catalyzed synthesis of benzimidazolyl oxadiazole derivatives, Safety of 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, the publication is Pharma Chemica (2010), 2(4), 224-230, database is CAplus.

Condensation of 2-(chloromethyl)benzimidazole with 2-mercapto-1,3,4-oxadiazoles gave 2-[(5-phenyl-1,3,4-oxadiazol-2-yl)thiomethyl]-1H-benzimidazole (I). Alternatively, I was also prepared by treatment of 1,2-C₆H₄(NH₂)₂ with 1,3,4-oxadiazole-2-thioacetate under Philips conditions. Subsequent treatment with dialkyl sulfate in MeCN using D-glucose as phase-transfer catalyst (PTC) gave the corresponding N-alkylated 2-[(benzimidazol-2-ylmethyl)thio]-1,3,4-oxadiazoles. The latter were also prepared by the reaction of 2-(chloromethyl)-N-methylbenzimidazole with 2-mercapto-1,3,4-oxadiazoles. Even though, there are several other PTCs reported in literature, the authors employed D-glucose because it has got characteristics similar to that of crown ethers and polyethylene glycol. Furthermore, it is readily available, reasonably cheap, non-toxic, and eco-friendly.

Pharma Chemica published new progress about 4760-35-4. 4760-35-4 belongs to imidazoles-derivatives, auxiliary class Chloride,Benzimidazole, name is 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, and the molecular formula is C9H9ClN2, Safety of 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Li, Xie published the artcileResearch on synthesis of S-(-)-omeprazole sodium, HPLC of Formula: 161796-78-7, the publication is Huagong Shikan (2009), 23(2), 35-36, database is CAplus.

A method for the synthesis of the title compound [i.e., 6-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole sodium salt (1:1)] is reported here. (-)-Omeprazole was prepared from 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methylthio]benzimidazole (i.e., a sulfide derivative) and cumene hydroperoxide by an asym. oxidation method. The product was treated with sodium hydroxide to give S-(-)-omeprazole sodium.

Huagong Shikan published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, HPLC of Formula: 161796-78-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem