Tag: 100-200

《Defence against Bremia lactucae conferred by the resistance gene Dm7 in lettuce is broken by treatment with dichloroisonicotinic acid》 was written by Oikonomou, Adriana; Bennett, Mark H.; Parker, Adam A. H.; Ton, Jurriaan; Mansfield, John W.. Category: chlorides-buliding-blocks And the article was included in Plant Pathology on April 30 ,2022. The article conveys some information:

The effect of inducers of systemic acquired resistance, dichloroisonicotinic acid (DCINA) and acibenzolar-S-Me (BION), on compatible interactions between Bremia lactucae and lettuce were examined using a detached cotyledon infection assay. Treatment with both activators caused a reduction in sporulation on susceptible cultivars Cobham Green challenged with isolate CL9W and Diana inoculated with isolate Tv, with DCINA being more effective than BION on an equimolar basis. Unexpectedly, treatment with both compounds suppressed the resistance conferred by the Dm7 gene in cv. Diana challenged by isolate CL9W (A7). The frequency of sporulation was greatly increased by DCINA in the incompatible interaction. The suppression of defense was associated with a delay in the onset of the Dm7-based hypersensitive reaction as indicated by the extended viability of penetrated epidermal cells, and reductions in both the accumulation of the phytoalexin lettucenin A and the deposition of autofluorescent phenolics such as syringaldehyde on plant and oomycete cell walls. The anal. of DCINA homologues indicated that 2-chloroisonicotinic acid was as effective as the dichloro-derivative in suppressing resistance in cv. Diana, whereas the absence of the carboxyl group rendered 2,6-dichloropyridine inactive. Infection of cotyledons by Botrytis cinerea was also found to be enhanced by DCINA treatment. Based on our results, we discuss the possibility that DCINA reduces Dm7 transcription through an epigenetic mechanism, as is supported by bioinformatic analyses of the resistance gene, and that it suppresses jasmonate-dependent resistance to B. cinerea. The results came from multiple reactions, including the reaction of 2-Chloroisonicotinic acid(cas: 6313-54-8Category: chlorides-buliding-blocks)

2-Chloroisonicotinic acid(cas: 6313-54-8) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.Category: chlorides-buliding-blocks

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

The author of 《Synthesis, antimicrobial activities, and molecular docking studies of dihydrotriazine derivatives bearing a quinoline moiety》 were Bai, Xueqian; Chen, Ying; Liu, Zhe; Zhang, Linhao; Zhang, Tianyi; Feng, Bo. And the article was published in Chemistry & Biodiversity in 2019. Recommanded Product: 3-Chlorobenzylchloride The author mentioned the following in the article:

In this article, three series of dihydrotriazine derivatives bearing a quinoline moiety (5a, 5b, 8a-8c, and 9a-9m) have been designed, synthesized, and evaluated as antibacterial agents. Compounds 8a-8c were found to be the most potent of all of the compounds tested with an MIC value of 1 μg/mL against several Gram-pos. (S. aureus 4220 and MRSA CCARM 3506) and Gram-neg. (E. coli 1924) strains of bacteria. In addition, 3-[4-amino-6-(phenethylamino)-2,5-dihydro-1,3,5-triazin-2-yl)-6-[(3-chlorobenzyl)oxy]quinolin-2-ol (8a) showed potent inhibitory activity (MIC=2 μg/mL) against Pseudomonas aeruginosa 2742, indicating that its antibacterial spectrum is similar to those of the pos. controls gatifloxacin and moxifloxacin. Structure-activity relationships (SAR) analyses and docking studies implicated the dihydrotriazine group in increasing the antimicrobial potency of the quinoline compounds In vitro enzyme study implied that compound 8a also displayed DHFR inhibition. In addition to this study using 3-Chlorobenzylchloride, there are many other studies that have used 3-Chlorobenzylchloride(cas: 620-20-2Recommanded Product: 3-Chlorobenzylchloride) was used in this study.

3-Chlorobenzylchloride(cas: 620-20-2) has been used in the reaction of 3-methoxybenzyl chloride and ethyl 4-bromobenzoate in pure water, using zinc dust and a Pd catalyst.Recommanded Product: 3-Chlorobenzylchloride

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Application of 620-20-2On November 30, 2020 ,《Design and synthesis of C-ring quinoxaline-substituted sinomenine 1,2,3-triazole derivatives via click reactions》 appeared in Journal of Chemical Research. The author of the article were Lu, Tong; Dong, Ling; Pan, Hongmei; Wu, Xuedan; Chen, Xia; Gu, Chengwen; Tao, Naili; Wang, Ao; Zhang, Kehua; Jin, Jie. The article conveys some information:

The synthesis of C-ring quinoxaline-substituted sinomenine 1,2,3-triazole derivatives at the 4-OH via click reactions was accomplished, and a total of 16 novel sinomenine double N-heterocyclic derivatives are obtained in 74%-95% yields. The C-ring is first transformed into a 1,2-diketone structure under the action of hydrochloric acid, and then reacted with o-phenylenediamine to obtain a C-ring quinoxaline-substituted structure. The 4-OH of sinomenine reacted with chloropropyne to give an alkynyl sinomenine, and then reacts with sodium azide and various benzyl chlorides to give the target compounds All the synthesized derivatives were characterized by Fourier-transform IR spectrometry, high resolution mass spectrometry, 1H NMR, and 13C NMR spectroscopy. In the experimental materials used by the author, we found 3-Chlorobenzylchloride(cas: 620-20-2Application of 620-20-2)

3-Chlorobenzylchloride(cas: 620-20-2) has been used in the reaction of 3-methoxybenzyl chloride and ethyl 4-bromobenzoate in pure water, using zinc dust and a Pd catalyst.Application of 620-20-2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Related Products of 620-20-2On March 31, 2022, Xiao, Yulong; Li, Hongsen; Shao, Qun; Liu, Yuan; Xie, Yonghai; Zhao, Linjing; Li, Ya published an article in Chemistry & Biodiversity. The article was 《Design, Synthesis, and Antifungal Activity of Sulfoximine Derivatives Containing Nitroguanidine Moieties》. The article mentions the following:

To discover novel pesticide candidates, a series of sulfoximine derivatives were designed and synthesized via the oxidation coupling reaction of sulfides and N-alkyl nitroguanidines. The compounds were evaluated for their antifungal activity against six phytopathogenic fungi. Most of them exhibited a broad spectrum of fungicidal activity in vitro. Compound 8IV-b displayed good fungicidal activity against Sclerotinia sclerotiorum, Rhizoctonia solani, Botrytis cinerea, Fusarium graminearum, and Phytophthora capsici, with EC50 value of 12.82, 12.50, 17.25, 31.08, and 30.11 mg/L, resp. In addition, compounds 8III-c and 8IV-e had EC50 values of 22.23 and 20.67 mg/L against P. capsic, which were significantly better than that of the com. procymidone (118.15 mg/L). Strikingly, 8IV-d exhibited satisfactory fungicidal activity against B. cinerea, which was comparable to control procymidone in terms of their EC50 values (7.42 vs. 10.83 mg/L), and the bioassays in vivo further confirmed that 8IV-d possessed potent protective effect against B. cinerea at 200 mg/L (72.2 %). These present findings will facilitate the design and development of novel potent fungicides. The results came from multiple reactions, including the reaction of 3-Chlorobenzylchloride(cas: 620-20-2Related Products of 620-20-2)

3-Chlorobenzylchloride(cas: 620-20-2) has been used in the reaction of 3-methoxybenzyl chloride and ethyl 4-bromobenzoate in pure water, using zinc dust and a Pd catalyst.Related Products of 620-20-2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Synthetic Route of C6H3ClFNO2On October 31, 2021 ,《Ligand-based substituent-anchoring design of selective receptor-interacting protein kinase 1 necroptosis inhibitors for ulcerative colitis therapy》 appeared in Acta Pharmaceutica Sinica B. The author of the article were Zhu, Jing; Xin, Meng; Xu, Congcong; He, Yuan; Zhang, Wannian; Wang, Zhibin; Zhuang, Chunlin. The article conveys some information:

Receptor-interacting protein (RIP) kinase 1 is involved in immune-mediated inflammatory diseases including ulcerative colitis (UC) by regulating necroptosis and inflammation. Our group previously identified TAK-632 (5) as an effective necroptosis inhibitor by dual-targeting RIP1 and RIP3. In this study, using ligand-based substituent-anchoring design strategy, we focused on the benzothiazole ring to obtain a series of TAK-632 analogs showing significantly improving on the anti-necroptosis activity and RIP1 selectivity over RIP3. Among them, a conformational constrained fluorine-substituted derivative (25) exhibited 333-fold selectivity for RIP1 (Kd = 15 nmol/L) than RIP3 (Kd > 5000 nmol/L). This compound showed highly potent activity against cell necroptosis (EC50 = 8 nmol/L) and systemic inflammatory response syndrome (SIRS) induced by TNF-α in vivo. Especially, it was able to exhibit remarkable anti-inflammatory treatment efficacy in a DSS-induced mouse model of UC. Taken together, the highly potent, selective, orally active anti-necroptosis inhibitor represents promising candidate for clin. treatment of UC. The experimental part of the paper was very detailed, including the reaction process of 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Synthetic Route of C6H3ClFNO2)

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. Many organochlorine compounds have been isolated from natural sources ranging from bacteria to humans. Synthetic Route of C6H3ClFNO2 Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Category: chlorides-buliding-blocksIn 2020 ,《The continuous-flow electrosynthesis of 4-(sulfonylmethyl)isoquinoline-1,3(2H,4H)-diones from N-alkyl-N-methacryloyl benzamides under metal-free and oxidant-free conditions》 was published in Organic Chemistry Frontiers. The article was written by Xu, Jia; Yang, Zhao; Hua, Jiawei; Lin, Yang; Bian, Mixue; Li, Yuguang; Liu, Chengkou; He, Wei; Fang, Zheng; Guo, Kai. The article contains the following contents:

An efficient and green electrochem. continuous-flow approach was developed for the synthesis of 4-(sulfonylmethyl)isoquinoline-1,3(2H,4H)-diones I [R1 = H, 8-Fe, 5,7-di-Me, etc.; R2 = Me, Et, Ph, etc.; R3 = Me, Ph, 2-thienyl, etc.] through the sulfonylation of alkenes with sulfonylhydrazides. The reaction proceeded in a continuous-flow electrolytic cell under metal-free and oxidant-free conditions. A series of activated alkenes were suitable for this system, and the corresponding products I were obtained in moderate to good yields. Moreover, reaction scale-up was smoothly achieved using the electrochem. continuous-flow system without changing the reaction conditions. The results came from multiple reactions, including the reaction of Thiophene-2-sulfonyl chloride(cas: 16629-19-9Category: chlorides-buliding-blocks)

Thiophene-2-sulfonyl chloride(cas: 16629-19-9) is a member of sulfonyl chlorides. Sulfonyl chlorides are reactive sulfonic acid derivatives similar in properties and reactivity to acid chlorides of carboxylates. The sulfonic acid group, however, is a highly hindered molecule, containing a tetrahedral configuration of substituents. Category: chlorides-buliding-blocks

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Safety of (3-Fluorophenyl)boronic acidIn 2021 ,《Synthesis and evaluation of pyridine-derived bedaquiline analogues containing modifications at the A-ring subunit》 appeared in RSC Medicinal Chemistry. The author of the article were Barbaro, Lisa; Nagalingam, Gayathri; Triccas, James A.; Tan, Lendl; West, Nicholas P.; Baell, Jonathan B.; Priebbenow, Daniel L.. The article conveys some information:

Despite promising efficacy, the clin. use of the anti-tubercular therapeutic bedaquiline has been restricted due to safety concerns. To date, limited SAR studies have focused on the quinoline ring (A-ring), and as such, we set out to explore modifications within this region in an attempt to discover new bedaquiline variants with an improved safety profile. We herein report the development of unique synthetic strategies that facilitated access to novel bedaquiline analogs leading to the discovery that anti-tubercular activity could be retained following replacement of the quinoline motif with pyridine heterocycles. This discovery is anticipated to open up multiple new avenues for exploration in the design of improved anti-tubercular therapeutics. The results came from multiple reactions, including the reaction of (3-Fluorophenyl)boronic acid(cas: 768-35-4Safety of (3-Fluorophenyl)boronic acid)

(3-Fluorophenyl)boronic acid(cas: 768-35-4) can be used to make novel liquid crystalline fluorobiphenylcyclohexenes and difluoroterphenyls by palladium-catalyzed cross-couplings also used in the synthesis of o-phenylphenols as potent leukotriene B4 receptor agonists.Safety of (3-Fluorophenyl)boronic acid

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

In 2019,Journal of Organic Chemistry included an article by Xu, Tong; Shao, Yinlin; Dai, Ling; Yu, Shulin; Cheng, Tianxing; Chen, Jiuxi. Recommanded Product: (3-Fluorophenyl)boronic acid. The article was titled 《Pd-Catalyzed Tandem Reaction of 2-Aminostyryl Nitriles with Arylboronic Acids: Synthesis of 2-Arylquinolines》. The information in the text is summarized as follows:

In the presence of Pd(O2CCF3)2, 2,2′-bipyridine, and p-toluenesulfonic acid, (E)-β-arylacrylonitriles underwent chemoselective tandem arylation and cyclocondensation reactions with arylboronic acids to yield 2-arylquinolines. In addition to this study using (3-Fluorophenyl)boronic acid, there are many other studies that have used (3-Fluorophenyl)boronic acid(cas: 768-35-4Recommanded Product: (3-Fluorophenyl)boronic acid) was used in this study.

(3-Fluorophenyl)boronic acid(cas: 768-35-4) can be used to make novel liquid crystalline fluorobiphenylcyclohexenes and difluoroterphenyls by palladium-catalyzed cross-couplings also used in the synthesis of o-phenylphenols as potent leukotriene B4 receptor agonists.Recommanded Product: (3-Fluorophenyl)boronic acid

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Wu, Jie; Ma, Song; Zhang, Tian-Yi; Wei, Zhi-Yu; Wang, Hui-Min; Guo, Fang-Yan; Zheng, Chang-Ji; Piao, Hu-Ri published an article in Medicinal Chemistry Research. The title of the article was 《Synthesis and biological evaluation of ursolic acid derivatives containing an aminoguanidine moiety》.Recommanded Product: 3-Chlorobenzylchloride The author mentioned the following in the article:

Three series of ursolic acid derivatives containing an aminoguanidine moiety were designed, synthesized, and evaluated for anti-bacterial and anti-inflammatory activity. Some compounds displayed potent anti-bacterial activity against Gram-pos. bacterial strains (including multidrug-resistant clin. isolates) and Gram-neg. bacterial strains, with min. inhibitory concentration (MIC) values in the range of 2-64 μg/mL. Compounds 3a, 5a, and 7l showed significant inhibitory activity against the Gram-pos. bacterial strain Staphylococcus aureus RN 4220, the Gram-neg. bacterial strain Escherichia coli 1924, and four multidrug-resistant Gram-pos. bacterial strains, with MIC values of 2 and 4 μg/mL. In anti-inflammatory tests, most of the compounds exhibited potent activity, in particular compound 3a displayed the most potent activity with 81.61% inhibition after i.p. administration, which was more potent than ursolic acid and the reference drugs (ibuprofen and indomethacin). The cytotoxic activity of compound 3a was assessed in HeLa, Hep3B, and A549 cells. In the experimental materials used by the author, we found 3-Chlorobenzylchloride(cas: 620-20-2Recommanded Product: 3-Chlorobenzylchloride)

3-Chlorobenzylchloride(cas: 620-20-2) has been used in the reaction of 3-methoxybenzyl chloride and ethyl 4-bromobenzoate in pure water, using zinc dust and a Pd catalyst.Recommanded Product: 3-Chlorobenzylchloride

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

In 2021,RSC Medicinal Chemistry included an article by Lin, Runfeng; Zhang, Zheng; Cao, Shengtian; Yang, Wen; Zuo, Yinglin; Yang, Xinye; Zhang, Jiancun; Xu, Juan; Li, Jing; Wang, Xiaojun. Name: 3-Chloro-4-fluoronitrobenzene. The article was titled 《The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis》. The information in the text is summarized as follows:

Idiopathic pulmonary fibrosis (IPF) is a chronic progressive lung disease with a typical survival time between three to five years. Two drugs, pirfenidone and nintedanib have been approved for the treatment of IPF, but they have limited efficacy. Thus, the development of new drugs to treat IPF is an urgent medical need. In this paper we report the discovery of a series of orally active pyrimidin-4(3H)-one analogs which exhibit potent activity in in vitro assays. Among them, HEC-866 showed promising efficacy in rat IPF models. Since HEC-866 also had good oral bioavailability, a long half-life and favorable long-term safety profiles, it was selected for further clin. evaluation.3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Name: 3-Chloro-4-fluoronitrobenzene) was used in this study.

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. Many organochlorine compounds have been isolated from natural sources ranging from bacteria to humans. Name: 3-Chloro-4-fluoronitrobenzene Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics