Month: February 2023

Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids as leukotriene biosynthesis inhibitors was written by Kolasa, Teodozyj;Gunn, David E.;Bhatia, Pramila;Woods, Keith W.;Gane, Todd;Stewart, Andrew O.;Bouska, Jennifer B.;Harris, Richard R.;Hulkower, Keren I.;Malo, Peter E.;Bell, Randy L.;Carter, George W.;Brooks, Clint D. W.. And the article was included in Journal of Medicinal Chemistry in 2000.COA of Formula: C7H7NO4 This article mentions the following:

A novel series of heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids was studied as leukotriene biosynthesis inhibitors. The hypothesis of structure-activity optimization by insertion of an oxime moiety was investigated using REV-5901 as a starting point. A systematic structure-activity optimization showed that the spatial arrangement and stereochem. of the oxime insertion unit proved to be important for inhibitory activity. A promising lead inhibited LTB₄ biosynthesis in the intact human neutrophil with IC₅₀ of 8 nM and had superior oral activity in vivo, in a rat pleurisy model (ED₅₀ = 0.14 mg/kg) and rat anaphylaxis model (ED₅₀ = 0.13 mg/kg). Spa. In a model of lung inflammation, the compound blocked LTE₄ biosynthesis (ED₅₀ of 0.1 mg/kg) and eosinophil influx (ED₅₀ of 0.2 mg/kg). In the experiment, the researchers used many compounds, for example, 3-(Hydroxymethyl)-4-nitrophenol (cas: 60463-12-9COA of Formula: C7H7NO4).

3-(Hydroxymethyl)-4-nitrophenol (cas: 60463-12-9) belongs to alcohols. Alcohols are among the most common organic compounds. They are used as sweeteners and in making perfumes, are valuable intermediates in the synthesis of other compounds, and are among the most abundantly produced organic chemicals in industry. Converting an alcohol to an alkene requires removal of the hydroxyl group and a hydrogen atom on the neighbouring carbon atom. Dehydrations are most commonly carried out by warming the alcohol in the presence of a strong dehydrating acid, such as concentrated sulfuric acid.COA of Formula: C7H7NO4

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Depolymerizable Poly(O-vinyl carbamate-alt-sulfones) as Customizable Macromolecular Scaffolds for Mucosal Drug Delivery was written by Kumar, Kaushlendra;Castano, Eduard Jimenez;Weidner, Andrew R.;Yildirim, Adem;Goodwin, Andrew P.. And the article was included in ACS Macro Letters in 2016.Recommanded Product: (R)-2-Aminobutan-1-ol This article mentions the following:

Interest in stimulus responsive materials and polymers has grown over the years, having shown great promise in a diverse set of applications. For drug delivery, stimulus-responsive polymers have been shown to encapsulate therapeutics such as small mol. drugs or proteins, deliver them to specific locations in the body, and release them so that they can induce a therapeutic effect in the patient. Most hydrolytically degradable polymers are synthesized via nucleophilic, anionic, or cationic polymerization, which generally requires protection of nucleophilic or protic side chains prior to polymerization Here, we report the synthesis of novel, alternating copolymers of sulfur dioxide and O-vinyl carbamate monomers that boast excellent functional group tolerance and pH-dependent instability. Alternating copolymers were synthesized containing pendant functionalities such as alc., carboxylic acid, ester, and azide without deprotection or postpolymn. modification. The copolymers were then formulated via nanopptn. into polymer nanoparticles capable of encapsulating small mol. dyes. The polymer nanoparticles were found to degrade rapidly at pH > 6 but were stable even in highly acidic conditions. Based on this observation, a proof-of-concept study for mucosal delivery was performed using polymer nanoparticles entrapped in a mucus model. At pH 8, the diffusion of encapsulated dye was found to be similar to free dye, while at pH 5 the diffusion coefficient was an order of magnitude lower. Cell viability was retained at 200 μg/mL particles after 24 h incubation. These polymers thus show promise as customizable scaffolds for mucosal drug delivery. In the experiment, the researchers used many compounds, for example, (R)-2-Aminobutan-1-ol (cas: 5856-63-3Recommanded Product: (R)-2-Aminobutan-1-ol).

(R)-2-Aminobutan-1-ol (cas: 5856-63-3) belongs to alcohols. The oxygen atom of the strongly polarized O―H bond of an alcohol pulls electron density away from the hydrogen atom. This polarized hydrogen, which bears a partial positive charge, can form a hydrogen bond with a pair of nonbonding electrons on another oxygen atom. Tertiary alcohols cannot be oxidized at all without breaking carbon-carbon bonds, whereas primary alcohols can be oxidized to aldehydes or further oxidized to carboxylic acids.Recommanded Product: (R)-2-Aminobutan-1-ol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Development of sodium alginate-based antioxidant and antibacterial bioactive films added with IRMOF-3/Carvacrol was written by Ning, Haoyue;Lu, Lixin;Xu, Jing;Lu, Lijing;Pan, Liao;Lin, Zidong. And the article was included in Carbohydrate Polymers in 2022.Synthetic Route of C10H14O This article mentions the following:

The purpose of this study was to compare the effects of different concentrations of the amine-functionalized isoreticular metal-organic framework-3 loaded with carvacrol (IRMOF-3/CA) on the properties of sodium alginate (SA) composite films, thus determining the optimal addition amount and further preparing bioactive packaging film with antibacterial and antioxidant activities. The morphol., structure, phys. properties, antioxidant and antibacterial activities of the films were characterized and analyzed. The results showed that the thermal stability and light barrier property of the films were improved by the addition of IRMOF-3/CA. When the addnl. concentration was 0.4 wt%, the tensile, water vapor barrier and hydrophobic properties of the films were increased by 30.13%, 9.06% and 46.43% resp. compared with those of pure SA film. Moreover, the film added with IRMOF-3/CA had sustained antioxidant and antibacterial activities, and had an apparent fresh-keeping effect on pork, suggesting its application potential in food packaging. In the experiment, the researchers used many compounds, for example, 5-Isopropyl-2-methylphenol (cas: 499-75-2Synthetic Route of C10H14O).

5-Isopropyl-2-methylphenol (cas: 499-75-2) belongs to alcohols. Because alcohols are easily synthesized and easily transformed into other compounds, they serve as important intermediates in organic synthesis. Tertiary alcohols cannot be oxidized at all without breaking carbon-carbon bonds, whereas primary alcohols can be oxidized to aldehydes or further oxidized to carboxylic acids.Synthetic Route of C10H14O

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Novel 1,4-dihydropyridine calcium antagonists. I. Synthesis and hypotensive activity of 4-(substituted pyridyl)-1,4-dihydropyridine derivatives was written by Ashimori, Atsuyuki;Ono, Taizo;Uchida, Takeshi;Ohtaki, Yutaka;Fukaya, Chikara;Watanabe, Masahiro;Yokoyama, Kazumasa. And the article was included in Chemical & Pharmaceutical Bulletin in 1990.Category: alcohols-buliding-blocks This article mentions the following:

A series of 4-(substituted pyridyl)-1,4-dihydropyridine derivatives I (R = H, halo, CF₃, etc.) were synthesized and their hypotensive effects examined Several compounds have a hypotensive activity parallel to that of nicardipine; the 4-(3-trifluoromethyl-2-pyridyl) and 4-(2-trifluoromethyl-3-pyridyl) derivatives, in particular, had approx. twice the duration of nicardipine, and the 4-(4-cyano-2-pyridyl) derivative had the most potent hypotensive activity of all the derivatives synthesized. In the experiment, the researchers used many compounds, for example, (6-(Trifluoromethyl)pyridin-2-yl)methanol (cas: 131747-53-0Category: alcohols-buliding-blocks).

(6-(Trifluoromethyl)pyridin-2-yl)methanol (cas: 131747-53-0) belongs to alcohols. Because alcohols are easily synthesized and easily transformed into other compounds, they serve as important intermediates in organic synthesis. The most common reactions of alcohols can be classified as oxidation, dehydration, substitution, esterification, and reactions of alkoxides.Category: alcohols-buliding-blocks

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Tertiary amines as highly efficient catalysts in the ring-opening reactions of epoxides with amines or thiols in H₂O: expeditious approach to β-amino alcohols and β-aminothioethers was written by Wu, Jie;Xia, Hong-Guang. And the article was included in Green Chemistry in 2005.Category: alcohols-buliding-blocks This article mentions the following:

Ring-opening of epoxides with various amines or thiols catalyzed by DABCO (1,4-diazabicyclic[2,2,2]octane) or Et₃N (1 mol%) in water afforded the corresponding products in good to excellent yields under mild reaction conditions. In the experiment, the researchers used many compounds, for example, Trans-2-(benzylamino)cyclohexanol (cas: 40571-86-6Category: alcohols-buliding-blocks).

Trans-2-(benzylamino)cyclohexanol (cas: 40571-86-6) belongs to alcohols. Similar to water, an alcohol can be pictured as having an sp3 hybridized tetrahedral oxygen atom with nonbonding pairs of electrons occupying two of the four sp3 hybrid orbitals. Converting an alcohol to an alkene requires removal of the hydroxyl group and a hydrogen atom on the neighbouring carbon atom. Dehydrations are most commonly carried out by warming the alcohol in the presence of a strong dehydrating acid, such as concentrated sulfuric acid.Category: alcohols-buliding-blocks

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

A study on prescription pattern of chronic kidney disease in tertiary care hospital was written by Saraswathi Pravallika, M.;Sampreethi, H.;Anusha, C. H.;Rohini, K.;Shete, Shivkumar. And the article was included in European Journal of Biomedical and Pharmaceutical Sciences in 2021.Recommanded Product: Calcium 2-hydroxypropanoate pentahydrate This article mentions the following:

The aim of the present investigation is to study the prescription pattern of chronic kidney disease in tertiary care hospital. The objective of the study was to study the prescription patterns of drugs used in chronic kidney disease and other comorbid conditions and to identify which drug is mostly prescribed at that hospital. To assess the rationality of prescription. To evaluate the medication adherence in CKD patients. The study on prescribing pattern definitely improves the quality of prescription writing, so study of drug prescribing pattern is relevant in the present scenario. To evaluate the prevalence of correct dosing in chronic kidney diseases depending on renal function estimation This is a retrospective, prospective observational study conducted over a period of six months. The study was conducted at Medicine ward of GLENEAGLES AWARE GLOBAL HOSPITAL LB.NAGAR. Patients who admitted to Nephrol. department of the hospital during a six- month period from Oct. 2021 to March 2021 are enrolled. CKD patients visiting the nephrologists are evaluated, diagnosed and prescribed with suitable therapy. All necessary details were collected from patient demographics, prescription chart, lab data, progress chart, medical records, doctor’s notes, nursing notes using a suitable designed data collection form. One hundred one patients were included in the project; with a mean age of 62.5. ± 18 years. More than half of patients were male, 77(76.2%). The mean BMI was 26 ± 1.15 kg/ m². The majority of patients were having normal weight 80 (79.2%), 15 (14.8%) patients had overweight, and obesity and only 6 (5.9%) patients were underweight. While 35 (34.6%) patients were smokers, 10 (9.9%) were ex-smokers and 56 (55.4%) patients were non- smokers. Anti- hypertensive agents are predominantly used among the patients. The most preferred options were beta blockers, calcium channel blockers and diuretics. Most of the physicians prescribed metoprolol (18.2%), amlodipine (38.3%), and cilnidipine (2%). Diuretics were the preferred option by the physician furosemide (92.3%), anti-platelets that are prescribed by the physicians are Aspirin (69.2%), clopidogrel (30.7%). Among the lipid lowering agents, atorvastatin (92.8%) was given to the most of the patients. sulbactam (20.4%), cefoperazone (20.4%), clarithromycin (10.25%), amoxycillin (10.25%) were mostly prescribed antibiotics in the study. The study concluded that most of the patients included in the study were suffering from chronic kidney disease. These may be due to their food habits, smoking, less exercise and poor health hygiene. The maximum number of patients was male; it may be due to smoking and alc. habits. Comorbidities such as hypertension, hyperglycemia, albuminuria, renal structure, and sex hormones, have been reported to have different effects on males and females. Thus, CKD progression may differ depending on sex. Early recognition with timely initiation of treatment in collaboration with nephrologists will improve the care for CKD patients. Thus, physicians and Nephrologists play an important outcome in patients with CKD. In the experiment, the researchers used many compounds, for example, Calcium 2-hydroxypropanoate pentahydrate (cas: 5743-47-5Recommanded Product: Calcium 2-hydroxypropanoate pentahydrate).

Calcium 2-hydroxypropanoate pentahydrate (cas: 5743-47-5) belongs to alcohols. Alcohols are among the most common organic compounds. They are used as sweeteners and in making perfumes, are valuable intermediates in the synthesis of other compounds, and are among the most abundantly produced organic chemicals in industry. Secondary alcohols are easily oxidized without breaking carbon-carbon bonds only as far as the ketone stage. No further oxidation is seen except under very stringent conditions.Recommanded Product: Calcium 2-hydroxypropanoate pentahydrate

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Evidence for distinct mechanisms of small molecule inhibitors of filovirus entry was written by Schafer, Adam;Xiong, Rui;Cooper, Laura;Nowar, Raghad;Lee, Hyun;Li, Yangfeng;Ramirez, Benjamin E.;Peet, Norton P.;Caffrey, Michael;Thatcher, Gregory R. J.;Saphire, Erica Ollmann;Cheng, Han;Rong, Lijun. And the article was included in PLoS Pathogens in 2021.Synthetic Route of C24H23ClO2 This article mentions the following:

Many small mols. have been identified as entry inhibitors of filoviruses. However, a lack of understanding of the mechanism of action for these mols. limits further their development as anti-filoviral agents. Here we provide evidence that toremifene and other small mol. entry inhibitors have at least three distinctive mechanisms of action and lay the groundwork for future development of anti-filoviral agents. The three mechanisms identified here include: (1) direct binding to the internal fusion loop region of Ebola virus glycoprotein (GP); (2) the HR2 domain is likely the main binding site for Marburg virus GP inhibitors and a secondary binding site for some EBOV GP inhibitors; (3) lysosome trapping of GP inhibitors increases drug exposure in the lysosome and further improves the viral inhibition. Importantly, small mols. targeting different domains on GP are synergistic in inhibiting EBOV entry suggesting these two mechanisms of action are distinct. Our findings provide important mechanistic insights into filovirus entry and rational drug design for future antiviral development. In the experiment, the researchers used many compounds, for example, (Z)-2-(4-(4-Chloro-1,2-diphenylbut-1-en-1-yl)phenoxy)ethan-1-ol (cas: 128607-22-7Synthetic Route of C24H23ClO2).

(Z)-2-(4-(4-Chloro-1,2-diphenylbut-1-en-1-yl)phenoxy)ethan-1-ol (cas: 128607-22-7) belongs to alcohols. Alkyl halides are often synthesized from alcohols, in effect substituting a halogen atom for the hydroxyl group. Under carefully controlled conditions, simple alcohols can undergo intermolecular dehydration to give ethers. This reaction is effective only with methanol, ethanol, and other simple primary alcohols.Synthetic Route of C24H23ClO2

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Synthesis of (3RS,3aSR,8aSR)-3-phenyloctahydrocyclohepta[b]pyrrol-4(1H)-one via the aza-Cope-Mannich rearrangement was written by Belov, Dmitry S.;Lukyanenko, Evgeny R.;Kurkin, Alexander V.;Yurovskaya, Marina A.. And the article was included in Tetrahedron in 2011.Safety of Trans-2-(benzylamino)cyclohexanol This article mentions the following:

A convenient and scalable method for the preparation of (3RS,3aSR,8aSR)-phenyloctahydrocyclohepta[b]pyrrol-4(1H)-one based on the aza-Cope-Mannich rearrangement is described. This approach allows us to synthesize the target compound in nine steps in a high overall yield (42%) with complete stereocontrol and up to 100 g scale. In the experiment, the researchers used many compounds, for example, Trans-2-(benzylamino)cyclohexanol (cas: 40571-86-6Safety of Trans-2-(benzylamino)cyclohexanol).

Trans-2-(benzylamino)cyclohexanol (cas: 40571-86-6) belongs to alcohols. Under appropriate conditions, inorganic acids also react with alcohols to form esters. To form these esters, a wide variety of specialized reagents and conditions can be used. Converting an alcohol to an alkene requires removal of the hydroxyl group and a hydrogen atom on the neighbouring carbon atom. Dehydrations are most commonly carried out by warming the alcohol in the presence of a strong dehydrating acid, such as concentrated sulfuric acid.Safety of Trans-2-(benzylamino)cyclohexanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Anthranilamide (aam)-substituted diboron: palladium-catalyzed selective B(aam) transfer was written by Kamio, Shintaro;Kageyuki, Ikuo;Osaka, Itaru;Hatano, Sayaka;Abe, Manabu;Yoshida, Hiroto. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2018.Reference of 68716-49-4 This article mentions the following:

An unsym. diboron bearing an anthranilamide (aam) substituent was synthesized and was found to be coupled with aryl halides through the palladium-catalyzed Miyaura-Ishiyama-type reaction. The selective transfer of aam-substituted boryl moiety led to exclusive formation of diverse Ar-B(aam). In the experiment, the researchers used many compounds, for example, 2-(4-Bromophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (cas: 68716-49-4Reference of 68716-49-4).

2-(4-Bromophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (cas: 68716-49-4) belongs to alcohols. Alcohols are among the most common organic compounds. They are used as sweeteners and in making perfumes, are valuable intermediates in the synthesis of other compounds, and are among the most abundantly produced organic chemicals in industry. Under carefully controlled conditions, simple alcohols can undergo intermolecular dehydration to give ethers. This reaction is effective only with methanol, ethanol, and other simple primary alcohols.Reference of 68716-49-4

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Bifunctional Metal-free Heterogeneous Catalyst for the Synthesis of Methanol and Diols from CO₂ and Epoxide was written by Chatterjee, Rupak;Bhattacharjee, Sudip;Bhaumik, Asim. And the article was included in Asian Journal of Organic Chemistry in 2022.Product Details of 57-55-6 This article mentions the following:

Currently world is facing a serious environmental concern in the steady increase in the CO₂ concentration in air and this is directly related to climate change. Thus, successful utilization of CO₂ into valuable chems. is one of our primary goals. Herein, we have successfully fabricated a porous organic polymer PDVTA-1 via the free radical cross coupling between divinylbenzene and triallyl amine. This porous polymer is found to possess permanent porosity with a very high BET surface area of 915 m² g^-1. Furthermore, upon sulfonation PDVTA-1 is found to be very active as a bifunctional catalyst with a high BET surface area of 477 m²g^-1 and it efficiently catalyzes the synthesis of methanol and diols from CO₂ and resp. epoxide under solvent-free process and relatively milder reaction conditions. In this method 34% yield of methanol and 53% propylene glycol are produced from CO₂ and propylene oxide by using considerably mild reducing agent Et₃SiH. In the experiment, the researchers used many compounds, for example, 1,2-Propanediol (cas: 57-55-6Product Details of 57-55-6).

1,2-Propanediol (cas: 57-55-6) belongs to alcohols. A strong base can deprotonate an alcohol to yield an alkoxide ion (R―O−). For example, sodamide (NaNH2), a very strong base, abstracts the hydrogen atom of an alcohol. Alcohols may be oxidized to give ketones, aldehydes, and carboxylic acids. These functional groups are useful for further reactions. Oxidation of organic compounds generally increases the number of bonds from carbon to oxygen (or another electronegative element, such as a halogen), and it may decrease the number of bonds to hydrogen.Product Details of 57-55-6

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts