Month: February 2023

Applying different techniques to improve the bioavailability of candesartan cilexetil antihypertensive drug was written by Aly, Usama Farghaly;Sarhan, Hatem Abdel-Monsef;Ali, Taha F. S.;Abd El-Bakey Sharkawy, Hosny. And the article was included in Drug Design, Development and Therapy in 2020.HPLC of Formula: 145040-37-5 This article mentions the following:

Purpose: The objective of this study was to compare different techniques to enhance the solubility and dissolution rate, and hence the bioavailability of candesartan cilexetil. Methods: To achieve this target, various techniques were employed such as solid dispersions, inclusion complexes, and preparation of candesartan nanoparticles. Following the preparations, all samples were characterized for their physicochem. properties, and the samples of the best results were subjected to further bioavailability studies. Results: Results of dissolution studies revealed an increase in the dissolution rate of all samples. The highest dissolution rate was achieved using solid dispersion of the drug with PVP K-90 (1:4). Physicochem. investigations (XR, DSC, and FT-IR) suggested formation of hydrogen bonding and changing in the crystalline structure of the drug. Regarding the inclusion complexes, more stable complex was formed between HP-β-CD and CC compared to β-CD, as indicated by phase solubility diagrams. Antisolvent method resulted in the preparation of stable nanoparticles, as indicated by ζ potential, with average particle size of 238.9 ± 19.25 nm using PVP K-90 as a hydrophilic polymer. The best sample that gave the highest dissolution rate (CC/PVP K-90 1:4) was allowed for further pharmacokinetic studies using UPLC MS/MS assay of rabbit plasma. Results showed a significant increase in the bioavailability of CC from ~15% to ~48%. Conclusion: The bioavailability of CC was significantly improved from ~15% to ~48% when formulated as SDs with PVP K-90 with 1:4 drug:polymer ratio. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5HPLC of Formula: 145040-37-5).

1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. Imidazole also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes.HPLC of Formula: 145040-37-5

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Heptadentate, Octadentate, Or Even Nonadentate? Denticity in the Unexpected Formation of an All-Carbon Donor-Atom Ligand in Rh^III(Cp*)(Anthracenyl-NHC) Complexes was written by Lee, Betty Y. T.;Phillips, Andrew D.;Hanif, Muhammad;Tong, Kelvin K. H.;Sohnel, Tilo;Hartinger, Christian G.. And the article was included in Inorganic Chemistry in 2021.Computed Properties of C8H8N2 This article mentions the following:

Investigations on incorporating an N-flanking anthracenyl moiety to [Rh(Cp*)(NHC)Cl₂] complexes surprisingly led to the formation of an intramol. C-C bond between the Cp* and anthracenyl moieties, with addnl. auxiliary interactions between the metal and the anthracenyl ring system. In silico modeling supports a reaction mechanism whereby Rh(η⁴-tetramethylfulvene) intermediates undergo metallocycloaddn. and the abstraction of a chlorido ligand, affording unique cationic complexes that feature Rh centers coordinated by a nonadentate ligand with exclusively carbon donor atoms. Some Rh-C interactions were extremely weak but nevertheless exhibited covalent bonding character. These weak Rh-C interactions were readily displaced by stronger electron donors, and the nonadentate ligand reverted to the heptadentate coordination mode observed in the intermediate. As far as we are aware, this study provides the first conclusive evidence of complexes bearing a single nonadentate κ⁹-coordinating ligand that features only carbon donors bound to a metal center. In the experiment, the researchers used many compounds, for example, 1-Methylbenzimidazole (cas: 1632-83-3Computed Properties of C8H8N2).

1-Methylbenzimidazole (cas: 1632-83-3) belongs to imidazole derivatives. Imidazole is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. This ring system is present in important biological building blocks, such as histidine and the related hormone histamine.Computed Properties of C8H8N2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The accumulation of 4-amino-5-imidazolecarboxamide in Escherichia coli was written by Alimchandani, H. R.;Sreenivasan, A.. And the article was included in Journal of Bacteriology in 1957.COA of Formula: C4H5N3O This article mentions the following:

The effects of pteroylglutamic acid (I), leucovorin (II), vitamin B₁₂ (III), and methionine (IV) on the accumulation of 4-amino-5-imidazolecarboxamide by E. coli during sulfadiazine (V) bacteriostasis were studied. I and II were ineffective in reversing V growth inhibition or in influencing amine accumulation per unit growth to different degrees, III being the more effective. Amine accumulation, when expressed as a variable against growth, was more in the presence of IV and least in the control set without added III or IV, the III effect being intermediate. These observations are interpreted to mean that the primary effects of III or IV are on the growth and other aspects of cell metabolism that are interfered with by sulfonamides. Their involvement in amine to purine conversion is only indirect. Ethionine and a III oxidation product depressed growth, but no amine accumulation was observed. The inability of an E. coli mutant to accumulate the amine under conditions of deficiency of III or IV also suggested that these 2 metabolites are involved only indirectly in purine synthesis. 27 references. In the experiment, the researchers used many compounds, for example, 1H-Imidazole-4-carboxamide (cas: 26832-08-6COA of Formula: C4H5N3O).

1H-Imidazole-4-carboxamide (cas: 26832-08-6) belongs to imidazole derivatives. The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . In contrast, the solubility of benzimidazoles in alcohols (C3–C6) is higher than in water and generally decreases with a Many drugs contain an imidazole ring, such as certain antifungal drugs, the nitroimidazole series of antibiotics, and the sedative midazolam.COA of Formula: C4H5N3O

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Relationship between mesoscale dynamics and shear relaxation of ionic liquids with long alkyl chain was written by Yamaguchi, Tsuyoshi;Mikawa, Ken-ichi;Koda, Shinobu;Fujii, Kenta;Endo, Hitoshi;Shibayama, Mitsuhoro;Hamano, Hiroshi;Umebayashi, Yasuhiro. And the article was included in Journal of Chemical Physics in 2012.SDS of cas: 404001-48-5 This article mentions the following:

The shear relaxation spectra of three imidazolium-based ionic liquids, 1-methyl-3-octylimidazolium chloride (C₈mimCl), 1-methyl-3-octylimidazolium hexafluorophosphate (C₈mimPF₆), and 1-dodecyl-3-methylimidazolium bis(trifluoromethanesulfonyl)amide (C₁₂mimTFSA) were measured and compared with the intermediate scattering functions determined with neutron spin echo (NSE) spectroscopy. The shear relaxation is slower than that predicted from the relaxation of the main peak of the structure factor that is common to other mol. liquids, whereas it is faster than that from the relaxation of the pre-peak, that corresponds to the correlation length of about 10 nm specific to ionic liquids with an intermediately long alkyl chain. The role of the pre-peak structure in the mechanism of shear viscosity of ionic liquids is discussed based on the comparison between NSE and shear relaxations. (c) 2012 American Institute of Physics. In the experiment, the researchers used many compounds, for example, 3-Dodecyl-1-methyl-1H-imidazol-3-ium bis((trifluoromethyl)sulfonyl)amide (cas: 404001-48-5SDS of cas: 404001-48-5).

3-Dodecyl-1-methyl-1H-imidazol-3-ium bis((trifluoromethyl)sulfonyl)amide (cas: 404001-48-5) belongs to imidazole derivatives. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. Imidazole has been usedin the lysis, wash and elution buffer for the purification of histidine tagged Sonic Hedgehog(shh-N) protein, in elution buffer in stepwise gradient for the purification of histidine tagged aldo keto reductases using nickel affinity chromatography, as a component of homogenization buffer for the purification of phagosomal compartments from dendritic cells.SDS of cas: 404001-48-5

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

N-alkylation of N-H compounds in N, N-dimethylformamide dialkyl acetal was written by Zhao, Hui;Zhu, Xiaoyun;Hu, Xiaoxia;Liu, Yan-ge;Tang, Chunlei;Feng, Bainian. And the article was included in Youji Huaxue in 2019.Quality Control of 4-Bromo-1-methylimidazole This article mentions the following:

The N, N-dimethylformamide dialkyl acetal was used as the alkyl source to achieve different nitrogen alkylation reactions of N-H compounds The reaction has the advantages of cheap raw materials, easy operation, mild reaction conditions, broad substrate scope and no metal participation. By studying the effects of solvents, temperature, reaction time, and the amount of N, N-dimethylformamide dialkyl acetal on the reaction, the optimal reaction conditions were obtained. The effect of different N, N-dimethylformamide dialkyl acetals on the alkylation ability of the substrate was investigated. In the experiment, the researchers used many compounds, for example, 4-Bromo-1-methylimidazole (cas: 25676-75-9Quality Control of 4-Bromo-1-methylimidazole).

4-Bromo-1-methylimidazole (cas: 25676-75-9) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. Imidazole is incorporated into many important biological compounds. The most pervasive is the amino acid histidine, which has an imidazole side-chain. Histidine is present in many proteins and enzymes, e.g. by binding metal cofactors, as seen in hemoglobin.Quality Control of 4-Bromo-1-methylimidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Optimized scale up of 3-pyrimidinylpyrazolo[1,5-a]pyridine via Suzuki coupling; a general method of accessing a range of 3-(hetero)arylpyrazolo[1,5-a]pyridines was written by Bethel, Paul A.;Campbell, Andrew D.;Goldberg, Frederick W.;Kemmitt, Paul D.;Lamont, Gillian M.;Suleman, Abid. And the article was included in Tetrahedron in 2012.Product Details of 25676-75-9 This article mentions the following:

We have developed an improved synthesis of 3-(hetero)aryl pyrazolo[1,5-a]pyridines [such as 3-(2,5-dichloropyrimidin-4-yl)pyrazolo[1,5-a]pyridine (I)] via an optimized synthesis and Suzuki coupling of 3-pyrazolo[1,5-a]pyridine boronic ester (II). These conditions are applicable to both high throughput chem. and large scale synthesis of these medicinally important compounds The scope of this chem. has been further extended to include the synthesis and coupling of a novel boronic ester, 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine. In the experiment, the researchers used many compounds, for example, 4-Bromo-1-methylimidazole (cas: 25676-75-9Product Details of 25676-75-9).

4-Bromo-1-methylimidazole (cas: 25676-75-9) belongs to imidazole derivatives. Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. The pharmacophore of imidazole exists in bioactive compounds including amino acids, plant growth regulators and therapeutic agents.n increase of the alkyl chain length of the alcohols. Product Details of 25676-75-9

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Ligand effect on ethylene trimerisation with [NNN]-heteroscorpionate pyrazolyl Cr(III) catalysts was written by Zhang, Jun;Li, Aifang;Hor, T. S. Andy. And the article was included in Dalton Transactions in 2009.Quality Control of 1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde This article mentions the following:

Cr(III) complexes with [NNN]-heteroscorpionate pyrazolyl ligands of the type Pz’₂CHX (Pz’ = pyrazol-1-yl (Pz), or 3,5-dimethylpyrazol-1-yl (Pz^Me); X = N-containing heterocyclic ring or amine CH₂NR¹R²; R¹, R² = H or alkyl) have been prepared Upon activation with MAO, they are active for selective ethylene trimerization to 1-hexene. The effects of the hetero-functional group and chelate ring size on the catalytic performance have been examined The pre-catalysts with an N-heterocycle substituent show highest activity [32,400-53,000 g/(g/Cr/h^-1)] and total C₆ selectivities (>97.6%) as well as 1-hexene selectivity (>96.0%) among hexenes. The X-ray single-crystal crystallog. anal. of CrCl₃[Pz^Me₂CH₂NCH₂Ph] and CrCl₃[Pz^Me₂CH₂NCH₂Fc] (Fc = ferrocenyl) shows a tridentate coordination on the fac-octahedral Cr(III) sphere with the Cr-N bond length dependent on the N-substituent. In the experiment, the researchers used many compounds, for example, 1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde (cas: 3012-80-4Quality Control of 1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde).

1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde (cas: 3012-80-4) belongs to imidazole derivatives. The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . In contrast, the solubility of benzimidazoles in alcohols (C3–C6) is higher than in water and generally decreases with a Many drugs contain an imidazole ring, such as certain antifungal drugs, the nitroimidazole series of antibiotics, and the sedative midazolam.Quality Control of 1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Inhibition of photosynthesis in Anacystis by alkylbenzimidazoles was written by Buechel, Karl H.;Roechling, Hans;Baedelt, H.;Gerhardt, Bernt;Trebst, Achim. And the article was included in Zeitschrift fuer Naturforschung, Teil B: Anorganische Chemie, Organische Chemie, Biochemie, Biophysik, Biologie in 1967.Electric Literature of C15H22N2 This article mentions the following:

Seventeen 2-alkylbenzimidazoles were tested for their ability to inhibit photosynthesis in A. nidulans. Inhibition increased with increasing chain length reaching a maximum with 2-undecylbenzimidazole, with 11 carbons in the side chain, which inhibited photosynthesis by 50% at 4.4 γ/ml. compared with 4650 γ/ml. for 2-propylbenzimidazole or 55 γ/ml. for 2-(dodecylamino)benzimidazole. The photosynthetic inhibition was due to an uncoupling of photophosphorylation. Noncyclic photophosphorylation coupled to ferricyanide reduction in the cell-free alga preparation was more sensitive to 2-undecylbenzimidazole than was cyclic photophosphorylation. In the experiment, the researchers used many compounds, for example, 2-Octylbenzimidazole (cas: 13060-24-7Electric Literature of C15H22N2).

2-Octylbenzimidazole (cas: 13060-24-7) belongs to imidazole derivatives. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. The pharmacophore of imidazole exists in bioactive compounds including amino acids, plant growth regulators and therapeutic agents.n increase of the alkyl chain length of the alcohols. Electric Literature of C15H22N2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Heterocyclic ambident nucleophiles. V. Alkylation of benzimidazoles was written by Howell, John R.;Rasmussen, Malcolm. And the article was included in Australian Journal of Chemistry in 1993.Reference of 4887-83-6 This article mentions the following:

Alkylation of 5-substituted benzimidazole anions with a variety of primary alkyl halides in both protic and aprotic solvents showed only small regioselectivity, with a slight preference for reaction at N(1) for 5-nitro and N(3) for 5-methoxy systems. With 4-substituted benzimidazole anions, alkylation gave more divergent results, with the N(1) to N(3) regioselectivity varying between 100:0 and 29:71. These alkylation patterns are interpreted as deriving from an interplay of electrostatic, thermodn., steric and associative control factors within the variable S_N2 transition state structures involved. In the 4-substituted series, proximity effects, both electrostatic field and steric non-bonded, are clearly dominant. In the experiment, the researchers used many compounds, for example, 7-Methyl-1H-benzo[d]imidazole (cas: 4887-83-6Reference of 4887-83-6).

7-Methyl-1H-benzo[d]imidazole (cas: 4887-83-6) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. This ring system is present in important biological building blocks, such as histidine and the related hormone histamine.Reference of 4887-83-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

N-alkylation of N-H compounds in N, N-dimethylformamide dialkyl acetal was written by Zhao, Hui;Zhu, Xiaoyun;Hu, Xiaoxia;Liu, Yan-ge;Tang, Chunlei;Feng, Bainian. And the article was included in Youji Huaxue in 2019.Synthetic Route of C4H5N3O2 This article mentions the following:

The N, N-dimethylformamide dialkyl acetal was used as the alkyl source to achieve different nitrogen alkylation reactions of N-H compounds The reaction has the advantages of cheap raw materials, easy operation, mild reaction conditions, broad substrate scope and no metal participation. By studying the effects of solvents, temperature, reaction time, and the amount of N, N-dimethylformamide dialkyl acetal on the reaction, the optimal reaction conditions were obtained. The effect of different N, N-dimethylformamide dialkyl acetals on the alkylation ability of the substrate was investigated. In the experiment, the researchers used many compounds, for example, 1-Methyl-4-nitroimidazole (cas: 3034-41-1Synthetic Route of C4H5N3O2).

1-Methyl-4-nitroimidazole (cas: 3034-41-1) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division.Synthetic Route of C4H5N3O2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem