Category: amides-buliding-blocks

Erdem, Rahsan published the artcileA Phase 2a randomized, single-center, double-blind, placebo-controlled study to evaluate the safety and preliminary efficacy of oral iOWH032 against cholera diarrhea in a controlled human infection model., Formula: C22H15Br2N3O4, the publication is PLoS neglected tropical diseases (2021), 15(11), e0009969, database is MEDLINE.

Cholera remains a major cause of infectious diarrhea globally. Despite the increased availability of cholera vaccines, there is still an urgent need for other effective interventions to reduce morbidity and mortality. Furthermore, increased prevalence of antibiotic-resistant Vibrio cholerae threatens the use of many drugs commonly used to treat cholera. We developed iOWH032, a synthetic small molecule inhibitor of the cystic fibrosis transmembrane conductance regulator chloride channel, as an antisecretory, host-directed therapeutic for cholera. In the study reported here, we tested iOWH032 in a Phase 2a cholera controlled human infection model. Forty-seven subjects were experimentally infected with V. cholerae El Tor Inaba strain N16961 in an inpatient setting and randomized to receive 500 mg iOWH032 or placebo by mouth every 8 hours for 3 days to determine the safety and efficacy of the compound as a potential treatment for cholera. We found that iOWH032 was generally safe and achieved a mean (± standard deviation) plasma level of 4,270 ng/mL (±2,170) after 3 days of oral dosing. However, the median (95% confidence interval) diarrheal stool output rate for the iOWH032 group was 25.4 mL/hour (8.9, 58.3), compared to 32.6 mL/hour (15.8, 48.2) for the placebo group, a reduction of 23%, which was not statistically significant. There was also no significant decrease in diarrhea severity and number or frequency of stools associated with iOWH032 treatment. We conclude that iOWH032 does not merit future development for treatment of cholera and offer lessons learned for others developing antisecretory therapeutic candidates that seek to demonstrate proof of principle in a cholera controlled human infection model study. Trial registration: This study is registered with ClinicalTrials.gov as NCT04150250.

PLoS neglected tropical diseases published new progress about 1191252-49-9. 1191252-49-9 belongs to amides-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,CFTR, name is 3-(3,5-Dibromo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxamide, and the molecular formula is C22H15Br2N3O4, Formula: C22H15Br2N3O4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Hijioka, Masanori published the artcileInhibition of leukotriene B₄ action mitigates intracerebral hemorrhage-associated pathological events in mice, Application of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Journal of Pharmacology and Experimental Therapeutics (2017), 360(3), 399-408, database is CAplus and MEDLINE.

Infiltration of neutrophils has been suggested to play an important role in the pathogenesis of intracerebral hemorrhage (ICH) for which effective therapeutic interventions remain unavailable. In the present study we focused on leukotriene B₄ (LTB₄) as a potent chemotactic factor for neutrophils in order to address its contribution to the pathol. events associated with ICH. ICH with hematoma expansion into the internal capsule that resulted in severe sensorimotor dysfunction was induced by injection of collagenase in mouse striatum. We found that LTB₄ as well as mRNAs of 5-lipoxygenase (5-LOX) and 5-LOXactivating protein were increased in the brain after ICH. Daily treatment with a 5-LOX inhibitor zileuton (3 or 10 mg/kg, i.v.) prevented ICH-induced increase in LTB₄, attenuated neutrophil infiltration into the hematoma, and ameliorated sensorimotor dysfunction. In addition, mice deficient in LTB₄ receptor BLT1 exhibited a lower number of infiltrating neutrophils in the hematoma and lower levels of sensorimotor dysfunction after ICH than did wild-type mice. Similarly, daily treatment of mice with BLT antagonist ONO-4057 (30 or 100 mg/kg, by mouth) from 3 h after induction of ICH inhibited neutrophil infiltration and ameliorated sensorimotor dysfunction. ONO-4057 also attenuated inflammatory responses of microglia/macrophages in the perihematoma region and axon injury in the internal capsule. These results identify LTB₄ as a critical factor that plays a major role in the pathogenic events in ICH, and BLT1 is proposed as a promising target for ICH therapy.

Journal of Pharmacology and Experimental Therapeutics published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Application of [(2-Hexylcyclopentylidene)amino]thiourea.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Brice, Reoyo-Prats published the artcileContinuous degradation of micropollutants in real world treated wastewaters by photooxidation in dynamic conditions, HPLC of Formula: 137862-53-4, the publication is Water Research (2022), 118777, database is CAplus and MEDLINE.

Wastewater is a major issue for the ecosystem because of its considerable quantities, the treatment methods adopted in the large majority of WWTPs, and its level of contamination by various types of pollutants, especially emerging ones. One of the solutions considered to reduce this pressure on water is the reuse of wastewater after treatment for watering green areas, road cleaning, industry, groundwater recharge but also for crop irrigation. This paper proposes to study the capabilities of a photoreactor for the removal of micropollutants contained in wastewater from wastewater treatment plants. The experiments are carried out under dynamic artificial irradiation conditions which can be controlled in order to apply irradiation representative of the sunshine conditions. The experiments aim at treating a real effluent from urban wastewater. On the basis of these data, the photo-oxidation mass capacities expressed per unit of irradiated surface and per day were evaluated. Our results show that the oxidation process acts in a selective and differentiated manner according to the categories of substances and within each category. Some mols. are not or only partially oxidized. Note that the photo-reactor fed continuously with wastewater from wastewater treatment plants containing about 80 substances, is subjected to a typical irradiation setpoint of a sunny day in Apr. This allows to define the instantaneous and daily capacities of the system with respect to the target mols.

Water Research published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, HPLC of Formula: 137862-53-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Abdellatif, Khaled R. A. published the artcileDesign, synthesis, and pharmacological evaluation of novel and selective COX-2 inhibitors based on celecoxib scaffold supported with in vivo anti-inflammatory activity, ulcerogenic liability, ADME profiling and docking study, Synthetic Route of 169590-42-5, the publication is Bioorganic Chemistry (2022), 105627, database is CAplus and MEDLINE.

Four new series of 1,2,4 triazole derivatives 4a,b 5a-d, 6a-f, and 7a,b possessing methylsulfonylphenyl moiety as COX-2 pharmacophore were designed and synthesized. The target compounds were prepared and evaluated in-vitro against COX-1 and COX-2 enzymes. Compounds 4a, 5b, 6a, and 7a showed the highest selectivity towards the COX-2 enzyme (S.I. = 8.64-14.58) in comparison to celecoxib (S.I. = . 6.44). Interestingly, compounds 4a, 6a, and 7a showed good anti-inflammatory activity with edema inhibition (54.17, 53.03, and 50.29 %, in order) relative to the reference drug celecoxib (49.60%) after 3 h. Addnl., these potent derivatives 4a, 5b, 6a and 7a were significantly less ulcerogenic (U.I. = 2.27-2.97) than both reference drugs celecoxib (U.I. = 2.99) and indomethacin (U.I. = 20.25). Besides, a histopathol. study of the stomach was also included. Moreover, docking simulation for the most selective compounds 4a, 5b, 6a, and 7a inside COX-2 active site was performed to explain their binding mode. Finally, an ADME study was applied and proved the promising activity of the new compounds as a new oral anti-inflammatory agent. In conclusion, the above findings reveal that newly developed compounds 4a, 6a, and 7a represent a potential selective COX-2 NSAID candidate with min. gastrointestinal risks.

Bioorganic Chemistry published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Synthetic Route of 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Abdellattif, Magda H. published the artcileNovel 2-hydroselenonicotinonitriles and selenopheno[2, 3-b]pyridines: efficient synthesis, molecular docking-DFT modeling, and antimicrobial assessment, Application of 2-Chloroacetamide, the publication is Frontiers in Chemistry (Lausanne, Switzerland) (2021), 672503, database is CAplus and MEDLINE.

Selenium containing heterocyclic compounds gained great interest as bioactive mols. as of late. This report explores the design, synthesis, characterization, and antimicrobial screening of new pyridine derivatives endowed with selenium moieties. A one-pot multicomponent system with a solvent-free, microwave irradiation environment was employed to afford this series. The spectroscopic techniques were exploited to verify the structures of the synthesized derivatives Addnl., the agar diffusion method was employed to determine the antimicrobial activity of all the desired compounds Of all the synthesized mols., few compounds exhibited well to remarkable antibacterial and antifungal activities. Moreover, derivative (E)-4,6-dimethyl-2-selenoxo-5-((3,4,5-trimethoxyphenyl)diazenyl)-1,2-dihydropyridine-3-carbonitrile demonstrated the most potent antibacterial and antifungal performance. The results were also supported by mol. docking studies, utilizing the MOE (mol. operating environment) which revealed the best binding mode with the highest energy interaction within the binding pocket. Lastly, theor. DFT calculations were carried out in a gas phase at B3LYP 6-311G (d,p) basis set to predict the mol. geometries and chem. reactivity descriptors. DFT results have been used to illustrate that mol. docking findings and biol. activity assessments.

Frontiers in Chemistry (Lausanne, Switzerland) published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Application of 2-Chloroacetamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

El-Awady, Mohamed I. published the artcileDecision-making tree for improving selectivity and sensitivity of sweeping-MEKC determination of hydrophobic analytes: Application to five cardiovascular drugs with greenness assessment, Category: amides-buliding-blocks, the publication is Microchemical Journal (2022), 107792, database is CAplus.

Efficient separation of five cardiovascular drugs has been achieved by a new micellar electrokinetic chromatog. method based on using a general strategy that can be applied for the separation of different hydrophobic analytes, while keeping the highest possible sweeping efficiency and hence the highest possible sensitivity. The studied drugs include valsartan, atorvastatin, ezetimibe, amlodipine, and simvastatin. The separation is accomplished in less than 12 min by applying a basic background electrolyte composed of 10 mM disodium tetraborate buffer of pH 10.5 containing 25 mM SDS and 11% n-propanol at 30 kv. Cromolyn sodium is used as an internal standard Variables that may influence the electrophoretic mobility of the five compounds are investigated. The calibration plots are linear within ranges of 0.5-20.0 μg/mL, 0.5-10.0 μg/mL and 10.0-100.0 μg/mL for valsartan, ezetimibe and simvastatin (at 200 nm) and 1.0-30.0 μg/mL for amlodipine, atorvastatin and simvastatin (at 240 nm). Correlation coefficients are ≥ 0.9997 and detection limits are ranged between 0.12 and 2.05 μg/mL. The developed procedure is successfully utilized to estimate the studied compounds in different pharmaceutical preparations The obtained data are statistically analyzed and evaluated. The greenness profile of the investigated approach has been assessed by a recent assessment tool to ensure the principles of green chem.

Microchemical Journal published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Category: amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zaki, Remon M. published the artcileA convenient synthesis, reactions and biological evaluation of novel pyrazolo[3,4-b]selenolo[3,2-e]pyrazine heterocycles as potential anticancer and antimicrobial agents, Application In Synthesis of 79-07-2, the publication is Medicinal Chemistry Research (2020), 29(12), 2130-2145, database is CAplus.

A novel series of 5-amino-6-substituted-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]selenolo[3,2-e]pyrazines was synthesized by the reaction of the chloro pyrazolo[3,4-b]pyrazine carbonitrile with selenium element in the presence of sodium borohydride and ethanol, followed by the reaction with α-halo alkylating agents to produce the selanyl-alkylated derivatives The latter compounds underwent Thorpe-Ziegler cyclization upon heating with ethanolic sodium ethoxide solution to afford the target selenolopyrazolopyrazine compounds The 5-amino-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]selenolo[3,2-e]pyrazine-6-carboxamide was used as a versatile precursor for synthesis of new heterocyclic fused to the pyrazoloselenolopyrazine moiety namely: pyrimidine and imidazopyrimidine. Assignment of the chem. structures for the newly synthesized compounds was confirmed on the bases of elemental and spectral techniques including FT-IR, ¹H NMR, ¹³C NMR, and mass spectra. Furthermore, certain compounds were screened for their antimicrobial activity which revealed remarkable activities against various pathogenic strains of bacteria and fungi. Alternatively, some of these compounds exhibited promising anticancer action against some colon and breast cancer cells.

Medicinal Chemistry Research published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C25H23NO4, Application In Synthesis of 79-07-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Ibara, Miho published the artcileChemo- and site-selective replacement of N-terminal carbamates in peptides, Name: H-Lys(Boc)-OH, the publication is Organic Letters (2022), 24(11), 2131-2136, database is CAplus and MEDLINE.

In peptide synthesis, it is important to distinguish the terminal amino group and carry out the selective transformation of only the N-terminal protecting group. We describe herein a reaction for the chemo- and site-selective replacement of carbamates with various other carbamates only at the N-terminus of peptides. We demonstrate the scope of carbamates and peptides and the introduction of fluorine into a peptide. This strategy is applicable to the late stage of peptide synthesis.

Organic Letters published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Name: H-Lys(Boc)-OH.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

El-Kafrawy, Dina S. published the artcileComparative study of two versatile multi-analyte chromatographic methods for determination of diacerein together with four non-steroidal anti-inflammatory drugs: Greenness appraisal using Analytical Eco-Scale and AGREE metrics, HPLC of Formula: 169590-42-5, the publication is Sustainable Chemistry and Pharmacy (2022), 100709, database is CAplus.

According to green anal. chem. (GAC) principles, multi-analyte methods are usually more preferred than methods determining one analyte at a time (principle 8) as they allow saving resources (time, reagents and money) (principle 9) and permit the reduction of generated waste (principle 7) as well as reduction of needed samples (principle 2). The present work herein, describes for the first time the development, validation and comparison of novel green versatile multi-analyte HPLC-DAD and HPTLC methods for the quant. estimation of five drugs (diacerein, aceclofenac, diclofenac sodium, celecoxib and meloxicam) within a single run in a short anal. time. For HPLC-DAD, separation was performed through using Zorbax SB C18 (4.6 x 250 mm, 5μm particle size) with the mobile phase composed of 0.05 M phosphate buffer pH 3.0 and acetonitrile (42:58, volume/volume) at a flow rate of 1 mL/min. The chromatograms were extracted at 258, 276 and 355 nm. In HPTLC procedure, precoated TLC silica gel aluminum plates 60 F254 were used with a mobile phase consisting of mixture of (chloroform: methanol: acetic acid, 92:8:0.25, volume/volume/v). The developed plates were scanned densitometrically at 258, 280 and 360 nm. Validation of the proposed methods was performed following the ICH guidelines for linearity, ranges, precision, accuracy, robustness, detection and quantification limits. Good linearities were confirmed by the high values of correlation coefficients (r > 0.9992). Appraisal of the greenness of the developed methods and comparison with different reported chromatog. methods was performed using the anal. Eco-scale (AES) approach and the novel Anal. GREEnness (AGREE) metric.

Sustainable Chemistry and Pharmacy published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, HPLC of Formula: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Ibrahim, Eman Ibrahim published the artcileA single oral dose of celecoxib-loaded solid lipid nanoparticles for treatment of different developmental stages of experimental schistosomiasis mansoni, Formula: C17H14F3N3O2S, the publication is Acta Tropica (2022), 106342, database is CAplus and MEDLINE.

Schistosomiasis, a neglected tropical parasitic disease, is associated with severe pathol., mortality and economic loss. The treatment and control of schistosomiasis depends mainly on a single dose of praziquantel (PZQ). Drug repurposing and nanomedicine attract great attention to improve anti-schistosomal therapy. Previously, we reported that celecoxib (CELE), the non-steroidal anti-inflammatory drug, showed potent anti-schistosomal efficacy in an oral dose of 20 mg/kg/day for five days against different developmental stages of Schistosoma mansoni (S. mansoni) infection in mice. The aim of the current study was to shorten the duration of CELE treatment to reach an effective single oral dose against different developmental stages of S. mansoni infection using solid lipid nanoparticles (SLNs) as nano-carriers. The latter enhance the solubility, bioavailability and drug delivery and hence can decrease the frequency of administration which is of great clin. value. CELE-loaded SLNs showed good colloidal properties, high entrapment efficiency and drug loading, sustained biphasic release pattern with excellent storage stability. The used regimen was efficient against different developmental stages of S. mansoni infection with the most pronounced effect against the juvenile stage where the worm load, the hepatic egg count and the intestinal egg count were reduced by 86.39%, 91.45% and 90.11%, resp. Meanwhile, when targeting the invasive and the adult stages, it induced reduction in the worm load by 73.55% and 78.22%, the hepatic egg count by 69.99% and 75.39% and the intestinal egg count by 77.57% and 79.89%, resp. Addnl., CELE-loaded SLNs caused extensive tegumental damage of adult worms and marked improvement in the liver pathol.

Acta Tropica published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Formula: C17H14F3N3O2S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics