Tag: 400-500

Recommanded Product: 324017-21-2On September 20, 2021 ,《Fluorosulfuryl Isocyanate Enabled SuFEx Ligation of Alcohols and Amines》 was published in Angewandte Chemie, International Edition. The article was written by Sun, Shoujun; Gao, Bing; Chen, Junyu; Sharpless, K. Barry; Dong, Jiajia. The article contains the following contents:

Fluorosulfuryl isocyanate (FSI, FSO2NCO) is established as a reliable bis-electrophilic linker for stepwise attachment of an alc. bearing module to an amine bearing module and thence a new module RO-C(=O)-NH-SO2-NR1R2 e.g., I is created. FSI’s isocyanate motif fuses directly and quickly with alcs. and phenols, affording fluorosulfuryl carbamates in nearly quant. yield. A new reagent and process to deliver the FSI-derived fluorosulfuryl carbamate fragment to amines are also developed. The resulting SVI-F motifs from step-1 are remarkably stable, given the great structural complexities in diverse products. In the step-2 reaction with amines, the best yield of the S-N linked products arise with water alone. This “”on water”” interfacial reactivity phenomenon is crucial, revealing the latent reactivity of SVI-F probe for potential covalent capture of proteins in vivo which is important in today’s drug discovery. The scope of the SuFEx chem. is largely expanded thereby and the facile entry to these phosphate-like connections should prove useful to click chem. across diverse fields. In the part of experimental materials, we found many familiar compounds, such as Fmoc-D-Phe(4-NH2)-OH(cas: 324017-21-2Recommanded Product: 324017-21-2)

Fmoc-D-Phe(4-NH2)-OH(cas: 324017-21-2) belongs to ethers.Although ethers resist hydrolysis, they are cleaved by hydrobromic acid and hydroiodic acid. Hydrogen chloride cleaves ethers only slowly. Recommanded Product: 324017-21-2

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Synthetic Route of C24H22N2O4On November 30, 2016 ,《Synthesis of new tetrazolyl derivatives of L- and D-phenylalanine》 appeared in Russian Journal of Organic Chemistry. The author of the article were Tolstyakov, V. V.; Tolstobrova, E. S.; Zarubina, O. S.; Popova, E. A.; Protas, A. V.; Chuprun, S. S.; Trifonov, R. E.. The article conveys some information:

(2S)- and (2R)-3-[4-(1H-Tetrazol-1-yl)phenyl]-2-aminopropionic acids were synthesized starting from L- and D-phenylalanine via azidation of Pr esters of (2S)- and (2R)-2-{[(9H-fluoren-9-ylmethoxy)carbonyl]amino}-3-(4-aminophenyl)propionic acids. The experimental process involved the reaction of Fmoc-D-Phe(4-NH2)-OH(cas: 324017-21-2Synthetic Route of C24H22N2O4)

Fmoc-D-Phe(4-NH2)-OH(cas: 324017-21-2) belongs to ethers.Although ethers resist hydrolysis, they are cleaved by hydrobromic acid and hydroiodic acid. Hydrogen chloride cleaves ethers only slowly. Synthetic Route of C24H22N2O4

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Electric Literature of C28H28O3In 2022 ,《Therapeutic Options for the Treatment of Darier′s Disease: A Comprehensive Review of the Literature》 appeared in Journal of Cutaneous Medicine and Surgery. The author of the article were Hanna, Nardin; Lam, Megan; Fleming, Patrick; Lynde, Charles W.. The article conveys some information:

A review. Darier′s disease (also known as keratosis follicularis or dyskeratosis follicularis) is an autosomal dominant inherited disorder which manifests as hyperkeratotic greasy papules in the first or second decade of life. Aside from symptom management and behavioral modifications to avoid triggers, there are currently no validated treatments for Darier′s disease (DD). However, a variety of treatments have been proposed in the literature including retinoids, steroids, vitamin D analogs, photodynamic therapy, and surgical excision. The purpose of this review article is to identify therapeutic options for treating DD and to outline the evidence underlying these interventions. A search was conducted in Medline for English language articles from inception to July 4, 2020. Our search identified a total of 474 nonduplicate studies, which were screened by title and abstract Of these, 155 full text articles were screened against inclusion/exclusion criteria, and 113 studies were included in our review. We identified Grade B evidence for the following treatments of DD: oral acitretin, oral isotretinoin, systemic Vitamin A, topical tretinoin, topical isotretinoin, topical adapalene gel, topical 5-flououracil, topical calciptriol and tacalcitol (with sunscreen), grenz ray radiation, and x-ray radiation. All other evidence for treatments of DD consisted of case reports or case series, which is considered grade C evidence. Considering the quality and quantity of evidence, clinicians may consider initiating a trial of select topical or oral retinoids first in patients with localized or generalized DD, resp. In the experiment, the researchers used many compounds, for example, 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Electric Literature of C28H28O3)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.Electric Literature of C28H28O3

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Category: ethers-buliding-blocksIn 2021 ,《An overview of adapalene and benzoyl peroxide once-daily topical gel as a therapeutic option for acne》 appeared in Expert Opinion on Pharmacotherapy. The author of the article were Emmerich, Veronica K.; Purvis, Caitlin G.; Feldman, Steven R.. The article conveys some information:

A review. Acne vulgaris is the most common skin condition worldwide, and it is associated with substantial psychol. comorbidity. Topical therapies – including retinoids, antibiotics, and benzoyl peroxide – are the cornerstones of treatment for patients with acne. The main barriers to care in the treatment of acne are poor adherence to therapy and lack of tolerability. Herein, the authors review the safety and efficacy of adapalene/benzoyl peroxide combination gel (0.1%/2.5% and 0.3%/2.5%), as well as its specific mechanisms of action that target acne vulgaris. The authors also offer an expert opinion on the use of adapalene/benzoyl peroxide gel compared with other topical therapies. Adapalene/benzoyl peroxide gel is safe and highly effective in the treatment of acne vulgaris. Its efficacy, tolerability, and ease-of-use are superior to other topical acne therapies, and its use does not contribute to antibiotic resistance. However, the cost of adapalene/benzoyl peroxide gel and lack of available generics may prohibit its use. In the part of experimental materials, we found many familiar compounds, such as 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Category: ethers-buliding-blocks)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.Category: ethers-buliding-blocks

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Najafi-Taher, Roqya; Jafarzadeh kohneloo, Aarefeh; Eslami Farsani, Vahid; Mehdizade Rayeni, Neda; Moghimi, Hamid Reza; Ehsani, Amirhooshang; Amani, Amir published an article in 2022. The article was titled 《A topical gel of tea tree oil nanoemulsion containing adapalene versus adapalene marketed gel in patients with acne vulgaris: a randomized clinical trial》, and you may find the article in Archives of Dermatological Research.Name: 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid The information in the text is summarized as follows:

Adapalene is used for treatment of acne vulgaris, a common dermatol. disease. Nano-based carriers have been developed to improve solubility and bioavailability of adapalene and other acne treatment drugs. In our previous report, tea tree oil nanoemulsion containing adapalene gel (TTO NE + ADA Gel) showed appropriate phys. and biol. properties such as stability, viscosity, pH, size, morphol. and biocompatibility in an animal model. The present study was designed to assess efficacy and safety of the TTO NE + ADA Gel in comparison with 0.1% adapalene marketed gel (ADA Marketed Gel). A total of 100 patients were randomized to receive TTO NE + ADA Gel or ADA Marketed Gel, once daily at night, for 12 wk. Anal. for efficacy was conducted by acne lesion count (total, inflammatory and non-inflammatory) and acne severity index at weeks 4, 8 and 12 using generalized estimating equation along with the safety assessments in each measurement for assessing dryness, erythema, burning sensation and irritation. Significantly better reduction in total, inflammatory, and non-inflammatory acne lesions were reported for TTO NE + ADA Gel as compared to the ADA Marketed Gel overall and on each measurement occasion (p value < 0.001 for all). Mean acne severity index also reduced with TTO NE + ADA Gel significantly in comparison with ADA Marketed Gel (p value < 0.001). Dryness was the most common adverse effect reported in both groups and it was higher in TTO NE + ADA Gel group. In conclusion, TTO NE + ADA Gel compared to ADA Marketed Gel appears more effective in the treatment of acne vulgaris, with no important change in adverse effects. In the experiment, the researchers used many compounds, for example, 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Name: 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) may be used as a pharmaceutical reference standard for the quantification of the analyte in topical gel formulations using high-performance liquid chromatography technique.Name: 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Najafi-Taher, Roqya; Jafarzadeh kohneloo, Aarefeh; Eslami Farsani, Vahid; Mehdizade Rayeni, Neda; Moghimi, Hamid Reza; Ehsani, Amirhooshang; Amani, Amir published an article in 2022. The article was titled 《A topical gel of tea tree oil nanoemulsion containing adapalene versus adapalene marketed gel in patients with acne vulgaris: a randomized clinical trial》, and you may find the article in Archives of Dermatological Research.Name: 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid The information in the text is summarized as follows:

Adapalene is used for treatment of acne vulgaris, a common dermatol. disease. Nano-based carriers have been developed to improve solubility and bioavailability of adapalene and other acne treatment drugs. In our previous report, tea tree oil nanoemulsion containing adapalene gel (TTO NE + ADA Gel) showed appropriate phys. and biol. properties such as stability, viscosity, pH, size, morphol. and biocompatibility in an animal model. The present study was designed to assess efficacy and safety of the TTO NE + ADA Gel in comparison with 0.1% adapalene marketed gel (ADA Marketed Gel). A total of 100 patients were randomized to receive TTO NE + ADA Gel or ADA Marketed Gel, once daily at night, for 12 wk. Anal. for efficacy was conducted by acne lesion count (total, inflammatory and non-inflammatory) and acne severity index at weeks 4, 8 and 12 using generalized estimating equation along with the safety assessments in each measurement for assessing dryness, erythema, burning sensation and irritation. Significantly better reduction in total, inflammatory, and non-inflammatory acne lesions were reported for TTO NE + ADA Gel as compared to the ADA Marketed Gel overall and on each measurement occasion (p value < 0.001 for all). Mean acne severity index also reduced with TTO NE + ADA Gel significantly in comparison with ADA Marketed Gel (p value < 0.001). Dryness was the most common adverse effect reported in both groups and it was higher in TTO NE + ADA Gel group. In conclusion, TTO NE + ADA Gel compared to ADA Marketed Gel appears more effective in the treatment of acne vulgaris, with no important change in adverse effects. In the experiment, the researchers used many compounds, for example, 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Name: 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) may be used as a pharmaceutical reference standard for the quantification of the analyte in topical gel formulations using high-performance liquid chromatography technique.Name: 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Category: ethers-buliding-blocksIn 2021 ,《An overview of adapalene and benzoyl peroxide once-daily topical gel as a therapeutic option for acne》 appeared in Expert Opinion on Pharmacotherapy. The author of the article were Emmerich, Veronica K.; Purvis, Caitlin G.; Feldman, Steven R.. The article conveys some information:

A review. Acne vulgaris is the most common skin condition worldwide, and it is associated with substantial psychol. comorbidity. Topical therapies – including retinoids, antibiotics, and benzoyl peroxide – are the cornerstones of treatment for patients with acne. The main barriers to care in the treatment of acne are poor adherence to therapy and lack of tolerability. Herein, the authors review the safety and efficacy of adapalene/benzoyl peroxide combination gel (0.1%/2.5% and 0.3%/2.5%), as well as its specific mechanisms of action that target acne vulgaris. The authors also offer an expert opinion on the use of adapalene/benzoyl peroxide gel compared with other topical therapies. Adapalene/benzoyl peroxide gel is safe and highly effective in the treatment of acne vulgaris. Its efficacy, tolerability, and ease-of-use are superior to other topical acne therapies, and its use does not contribute to antibiotic resistance. However, the cost of adapalene/benzoyl peroxide gel and lack of available generics may prohibit its use. In the part of experimental materials, we found many familiar compounds, such as 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Category: ethers-buliding-blocks)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.Category: ethers-buliding-blocks

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Electric Literature of C28H28O3In 2022 ,《Therapeutic Options for the Treatment of Darier′s Disease: A Comprehensive Review of the Literature》 appeared in Journal of Cutaneous Medicine and Surgery. The author of the article were Hanna, Nardin; Lam, Megan; Fleming, Patrick; Lynde, Charles W.. The article conveys some information:

A review. Darier′s disease (also known as keratosis follicularis or dyskeratosis follicularis) is an autosomal dominant inherited disorder which manifests as hyperkeratotic greasy papules in the first or second decade of life. Aside from symptom management and behavioral modifications to avoid triggers, there are currently no validated treatments for Darier′s disease (DD). However, a variety of treatments have been proposed in the literature including retinoids, steroids, vitamin D analogs, photodynamic therapy, and surgical excision. The purpose of this review article is to identify therapeutic options for treating DD and to outline the evidence underlying these interventions. A search was conducted in Medline for English language articles from inception to July 4, 2020. Our search identified a total of 474 nonduplicate studies, which were screened by title and abstract Of these, 155 full text articles were screened against inclusion/exclusion criteria, and 113 studies were included in our review. We identified Grade B evidence for the following treatments of DD: oral acitretin, oral isotretinoin, systemic Vitamin A, topical tretinoin, topical isotretinoin, topical adapalene gel, topical 5-flououracil, topical calciptriol and tacalcitol (with sunscreen), grenz ray radiation, and x-ray radiation. All other evidence for treatments of DD consisted of case reports or case series, which is considered grade C evidence. Considering the quality and quantity of evidence, clinicians may consider initiating a trial of select topical or oral retinoids first in patients with localized or generalized DD, resp. In the experiment, the researchers used many compounds, for example, 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Electric Literature of C28H28O3)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.Electric Literature of C28H28O3

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

《Dermal delivery and follicular targeting of adapalene using PAMAM dendrimers》 was written by Gokce, Beyza B.; Boran, Tugce; Emlik Calik, Filiz; Ozhan, Gul; Sanyal, Rana; Gungor, Sevgi. Category: ethers-buliding-blocks And the article was included in Drug Delivery and Translational Research in 2021. The article conveys some information:

The aims of this study were to develop and optimize adapalene (ADA)-loaded PAMAM dendrimer-based nanocarriers for topical acne treatment and to prepare gel formulations of the selected nanocarriers and to characterize their rheol. properties and spreadability. ADA accumulation in HFs and in the skin from PAMAM dendrimers’ aqueous colloidal formulations and their gel formulations were quant. determined using punch biopsy technique. Follicular targeting efficiency from PAMAM dendrimers and their gel formulation was compared with the com. gel product, Differin Gel. The localisation of fluorescently labeled PAMAM dendrimers was visualised using a confocal microscope, which confirmed a successful delivery of the carrier system to the HFs. It was also quantified that PAMAM dendrimers improved follicular localisation and skin deposition of ADA. PAMAM dendrimers’ gel formulation including lower ADA doses compared with the com. product exhibited efficient performance in terms of drug accumulation in HFs. In vitro cell viability studies showed the relative safety of G2-PAMAM dendrimers which could be considered to possibly be well tolerated by the skin. Overall, PAMAM dendrimers’ potential to selectively target drugs to the site of action, reduce dose administrated, therefore minimise side effects and provide efficiency in topical treatment of dermatol. diseases such as acne was shown. The experimental part of the paper was very detailed, including the reaction process of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Category: ethers-buliding-blocks)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) may be used as a pharmaceutical reference standard for the quantification of the analyte in topical gel formulations using high-performance liquid chromatography technique.Category: ethers-buliding-blocks

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Related Products of 106685-40-9In 2021 ,《In-silico screening for identification of potential inhibitors against SARS-CoV-2 transmembrane serine protease 2 (TMPRSS2)》 was published in European Journal of Pharmaceutical Sciences. The article was written by Barge, Sagar; Jade, Dhananjay; Gosavi, Gokul; Talukdar, Narayan Chandra; Borah, Jagat. The article contains the following contents:

A new severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), a respiratory infection out broke in Dec. 2019 in Wuhan, Hubei province, China, resulted in pandemic conditions worldwide. COVID-19 spread swiftly around the world over with an alert of an emergency for an adequate drug. Therefore, in this research, we repurposed the FDA-approved medicines to find the prominent drug used to cure the COVID infected patients. We performed homol. modeling of the transmembrane serine protease 2 (TMPRSS2), responsible for the viral entry. The prediction of the transmembrane region and the Conserved Domain in TMPRSS2 protein was made for docking. 4182 FDA-approved compounds from the ZINC database were downloaded and used for the calculation of physicochem. properties. Two thousand eight hundred fifteen screened compounds were used for mol. docking against the modelled protein structure. From which top hit compounds based on binding energy were extracted At 1st site pose, ZINC3830554 showed the highest binding energy -12.91kcal/mol by forming Salt Bridge at LYS143, Hydrogen bond at ALA8, VAL45, HIS47, SER142, ASN277, ASN359, and TRP363. The hydrophobic Interactions at PHE3, LEU4, ALA7, ALA8, ALA139, PRO197, and PHE266. In the 2nd site pose, ZINC203686879 shows the highest binding energy (-12.56 kcal/mol) and forms a hydrophobic interaction with VAL187, VAL189, HIS205, LYS301, GLN347, TRP370 and hydrogen bond was at GLY300, THR302, GLN347, SER350 residues. These hit compounds were subjected to stability checks between the protein-ligand complex through the dynamics simulation (MD), and binding free energy was calculated through the Mol. Mechanics energies combined with Poisson-Boltzmann (MM/PBSA) method. We hope that hit compounds would be an efficient inhibitor that can block the TMPRSS2 activity and resist the entry of the SARS-CoV-2 virus into targeted human cells by reducing the virus′s infectivity and transmissibility.6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Related Products of 106685-40-9) was used in this study.

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.Related Products of 106685-40-9

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem