Day: November 25, 2022

Sayed, Ahmed M. published the artcileArylpyrazole as selective anti-enterococci; synthesis and biological evaluation of novel derivatives for their antimicrobial efficacy, HPLC of Formula: 197958-29-5, the publication is Journal of Heterocyclic Chemistry, database is CAplus.

Condensation of the 1-(1-[4-substituted aryl]phenyl-5-methyl-1H-pyrazol-4-yl)ethan-1-ones with the aminoguanidinehydrochloride gave target compounds 2-(1-(1-(4-[aryl or alkyl] phenyl)-5-methyl-1Hpyrazol-4-yl)ethylidene)hydrazine-1-carboximidamides I [R = Ph, Bn, 4-MeC₆H₄, etc.]. Exploring the structure-activity relationships (SAR) of a new set of phenylpyrazoles I [R = Ph, Bn, 4-MeC₆H₄, etc.] unveiled a potential anti-enterococcus lead compound I [R = benzofuran-2-yl]. The benzofuran moiety linked to the phenylpyrazole I [R = benzofuran-2-yl] was 32 times better than vancomycin against Enterococcus fecalis ATCC 51299. Besides, compound I [R = benzofuran-2-yl] is expected to have an excellent oral bioavailability according to the in silico studies. In SAR anal., it was found that the benzofuran side chain was essential for the activity. Changing the benzofuran with either benzothiophene, Ph, pyridinyl, tolyl, or naphthyl reduces/nullifies the pharmacol. action. Besides the anti-enterococcal activity, derivatives I [R = furan-2-yl, Ph] could be used to develop new broad-spectrum antibiotics as they exhibited activity against the wild-type highly virulent Escherichia coli isolate. Moreover, compound I [R = benzothiophen-2-yl] was proved to show antifungal activity (MIC = 4 μg/mL) against the Candida albicans SS5314 (wild type).

Journal of Heterocyclic Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, HPLC of Formula: 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Mohamad, Ahmad Desoky M. published the artcileTemperature and salt effects of the kinetic reactions of substituted 2-pyridylmethylene-8-quinolyl iron (II) complexes as antimicrobial, anti-cancer, and antioxidant agents with cyanide ions, Product Details of C12H9NO, the publication is Canadian Journal of Chemistry (2021), 99(9), 763-772, database is CAplus.

Kinetics of substitution reaction of three high-spin pyridylmethylene-8-quinolyl iron (II) complexes by CN^– ions were studied spectrophotometrically in various ratios of aqueous-methanol binary mixtures at 298 ± 0.2 K. Kinetics of the substitution reaction follow the rate law (k₂[CN^–][complex]) on applying of the conditions of the pseudo first order reaction. Reactivity of the reaction was investigated in terms of ligand moiety and solvent effects. The rate of the reaction increased as the co-solvent methanol ratio increased. This reactivity trend is predominantly due to increases in the activity coefficient of those hydrophobic complexes in the organic methanol co-solvent, depending upon the hydrophobicity of the substituent groups (R) in the coordinated ligand in the complexes. Reactivity trends of the prepared complexes in the presence of the inserted hydrophobic salts such as tetrabutylammonium bromide (TBAB), tetraethylammonium bromide (TEAB), and tetramethylammonium bromide (TMAB) or hydrophilic salt potassium bromide (KBr) were studied. The observed decrease in the rate constants with increasing salt concentration was due to the cationic character of the reacting complexes. In addition, the synthesized compounds were tested for antimicrobial activity against selected strains of microbes. The results showed that the order of reactivity of the investigated complexes against the selected microbes were as follows: ppaqFe > paaqFe > pmaqFe. In addition, the investigated ligands and their Fe(II) complexes were screened for anticancer activities against several cell lines of cancer. The ppaqFe complex showed the best cytotoxic efficiency against the selected cancer lines (IC₅₀ = 8.75-21.50μg/μl), whereas the pmaq ligand showed the lowest cytotoxic efficiency (IC₅₀ = 58.25- 72.40). Furthermore, the antioxidant potential of the presented compounds was studied by applying DPPH assays and showed a potential activity compared with standard vitamin C. The excellent antimicrobial and anticancer activities of the investigated Fe(II) chelates compared with literature values are promising and deserve further study.

Canadian Journal of Chemistry published new progress about 91-02-1. 91-02-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene,Ketone, name is Phenyl(pyridin-2-yl)methanone, and the molecular formula is C12H9NO, Product Details of C12H9NO.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Hashemi, Marzieh published the artcileEnhancing the Anticonvulsant Effects of Nifedipine in Rats Through Encapsulation with Water-Soluble β-Cyclodextrin Polymer, Related Products of pyridine-derivatives, the publication is Pharmaceutical Chemistry Journal (2022), 55(10), 1023-1027, database is CAplus.

Encapsulation is one of the efficient methods recently developed for improving drug delivery. The present study was designed to encapsulate nifedipine (NIF) by water-soluble β-cyclodextrin polymer (β-CDP) and to evaluate the effects of this carrier on NIF-induced anticonvulsant effects. Adult male Wistar rats weighting 200 – 250 g (n = 7) received NIF or encapsulated NIF (β-CDP/NIF) (5, 10 and 20 mg/kg, i.p.), diazepam (2 mg/kg, i.p. as pos. control), and vehicle. Then, pentylenetetrazol (PTZ, 80 mg/kg, i.p.) was injected about 30 min after the drug injection. Changes in the onset time of seizures and duration of their different stages (tonic and tonic-clonic) and total convulsions duration, percentage mortality and percentage of seizure protection were assessed in all test groups. Latency of the seizure onset and duration of tonic and tonic-clonic seizures were significantly decreased in β-CDP/NIF group in comparison with NIF-treated rats (p < 0.05). On the other hand, percentage mortality was significantly decreased and percentage protection was increased by β-CDP/NIF in comparison to NIF (p < 0.05). Therefore, it was concluded that the encapsulation of NIF by β-CDP led to enhancement of the anticonvulsant effects of NIF in rats.

Pharmaceutical Chemistry Journal published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Related Products of pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Lee, Hon Cheung published the artcileStructural determinants of nicotinic acid adenine dinucleotide phosphate important for its calcium-mobilizing activity, Name: Pyridine-3-sulfonic acid, the publication is Journal of Biological Chemistry (1997), 272(33), 20378-20383, database is CAplus and MEDLINE.

Nicotinic acid adenine dinucleotide phosphate (NAADP) mobilizes Ca²⁺ through a mechanism totally independent of cyclic ADP-ribose or inositol trisphosphate. The structural determinants important for its Ca²⁺ release activity were investigated using a series of analogs. It is shown that changing the 3-carboxyl group of the nicotinic acid (NA) moiety in NAADP to either an uncharged carbinol or from the 3-position to the 4-position of the pyridine ring totally eliminates the Ca²⁺ release activity. Conversion of the 3-carboxyl to other neg. charged groups, either 3-sulfonate, 3-acetate, or 3-quinoline carboxylate, retains the Ca²⁺ release activity, although their half-maximal effective concentrations (EC₅₀) are 100-200-fold higher. Changing the 6-amino group of the adenine to a hydroxyl group results in more than a 1000-fold decrease in the Ca²⁺ release activity. Conversion of the 2′-phosphate to 2′,3′-cyclic phosphate or 3′-phosphate likewise increases the EC₅₀ by about 5- and 20-fold, resp. Similar to NAADP, all of the active analogs can also desensitize the Ca²⁺ release mechanism at subthreshold concentrations, suggesting that this novel property is intrinsic to the release mechanism. The series of analogs used was produced by using ADP-ribosyl cyclase to catalyze the exchange of the nicotinamide group of various analogs of NADP with various analogs of NA. An important determinant in NA that is crucial to the base exchange reaction was shown to be the 2-position of the pyridine ring. Neither pyridine-2-carboxylate nor 2-methyl-NA support the exchange reaction. The neg. charge and the position of the 3-carboxyl group ware nonessential since both pyridine-3-carbinol and pyridine-4-carboxylate support the base exchange reaction. In addition to the information on the structure-activity relationships of NAADP and NA, this study also demonstrates the utility of the base exchange reaction as a general approach for synthesizing NAADP analogs.

Journal of Biological Chemistry published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, Name: Pyridine-3-sulfonic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Johnson, Ted W. published the artcileDiscovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations, Related Products of pyridine-derivatives, the publication is Journal of Medicinal Chemistry (2014), 57(11), 4720-4744, database is CAplus and MEDLINE.

Although crizotinib demonstrates robust efficacy in anaplastic lymphoma kinase (ALK)-pos. non-small-cell lung carcinoma patients, progression during treatment eventually develops. Resistant patient samples revealed a variety of point mutations in the kinase domain of ALK, including the L1196M gatekeeper mutation. In addition, some patients progress due to cancer metastasis in the brain. Using structure-based drug design, lipophilic efficiency, and phys.-property-based optimization, highly potent macrocyclic ALK inhibitors were prepared with good absorption, distribution, metabolism, and excretion (ADME), low propensity for p-glycoprotein 1-mediated efflux, and good passive permeability. These structurally unusual macrocyclic inhibitors were potent against wild-type ALK and clin. reported ALK kinase domain mutations. Significant synthetic challenges were overcome, utilizing novel transformations to enable the use of these macrocycles in drug discovery paradigms. This work led to the discovery of 8k (PF-06463922), combining broad-spectrum potency, central nervous system ADME, and a high degree of kinase selectivity.

Journal of Medicinal Chemistry published new progress about 1454848-00-0. 1454848-00-0 belongs to pyridine-derivatives, auxiliary class Aromatic Fluorinated Building Blocks, name is (R)-Methyl 2-(1-((2-amino-5-bromopyridin-3-yl)oxy)ethyl)-4-fluorobenzoate, and the molecular formula is C15H14BrFN2O3, Related Products of pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem