Category: 89-77-0

On April 8, 2021, Zhang, Han; Yu, Peilin; Lin, Hongwei; Jin, Zefang; Zhao, Siqi; Zhang, Yi; Xu, Qingxia; Jin, Hongwei; Liu, Zhenming; Yang, Wei; Zhang, Liangren published an article.Formula: C7H6ClNO2 The title of the article was The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo. And the article contained the following:

The transient receptor potential melastatin 2 (TRPM2) channel is associated with ischemia/reperfusion injury, inflammation, cancer, and neurodegenerative diseases. However, the limit of specific inhibitors impedes the development of TRPM2-targeted therapeutic agents. To discover more potent and selective TRPM2 inhibitors, 59 N-(p-amylcinnamoyl) anthranilic acid (ACA) derivatives were synthesized and evaluated using calcium imaging and electrophysiol. approaches. Systematic structure-activity relationship studies resulted in some potent compounds inhibiting the TRPM2 channel with sub-micromolar half-maximal inhibitory concentration values. Among them, the preferred compound A23 (I) exhibited TRPM2 selectivity over TRPM8 and TRPV1 channels as well as phospholipase A2 and showed neuroprotective activity in vitro. Following pharmacokinetic studies, I was further evaluated in a transient middle cerebral artery occlusion model in vivo, which significantly reduced cerebral infarction. These data indicate that A23 might serve as a useful tool for TRPM2-related research as well as a lead compound for the development of therapeutic agents for ischemic injury. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Formula: C7H6ClNO2

The Article related to amylcinnamoyl anthranilic acid synthesis sar neuroprotectant brain ischemia, Pharmacology: Structure-Activity and other aspects.Formula: C7H6ClNO2

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

Fancellu, Gaia; Chand, Karam; Tomas, Daniel; Orlandini, Elisabetta; Piemontese, Luca; Silva, Diana F.; Cardoso, Sandra M.; Chaves, Silvia; Santos, M. Amelia published an article in 2020, the title of the article was Novel tacrine-benzofuran hybrids as potential multi-target drug candidates for the treatment of Alzheimer’s Disease.Application In Synthesis of 2-Amino-4-chlorobenzoic acid And the article contains the following content:

Pursuing the widespread interest on multi-target drugs to combat Alzheimer’s disease (AD), a new series of hybrids was designed and developed based on the repositioning of the well-known acetylcholinesterase (AChE) inhibitor, tacrine (TAC), by its coupling to benzofuran (BF) derivatives The BF framework aims to endow the conjugate mols. with ability for inhibition of AChE (bimodal way) and of amyloid-beta peptide aggregation, besides providing metal (Fe, Cu) chelating ability and concomitant extra anti-oxidant activity, for the hybrids with hydroxyl substitution. The new TAC-BF conjugates showed very good activity for AChE inhibition (sub-micromolar range) and good capacity for the inhibition of self- and Cu-mediated Aβ aggregation, with dependence on the linker size and substituent groups of each main moiety. Neuroprotective effects were also found for the compounds through viability assays of neuroblastoma cells, after Aβ1-42 induced toxicity. Structure-activity relationship anal. provides insights on the best structural parameters, to take in consideration for future studies in view of potential applications in AD therapy. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Application In Synthesis of 2-Amino-4-chlorobenzoic acid

The Article related to tacrine benzofuran hybrid preparation alzheimer’s antioxidant, ache inhibitors, alzheimer’s disease, metal chelators, multi-target drugs, tacrine-benzofuran hybrids, Pharmacology: Structure-Activity and other aspects.Application In Synthesis of 2-Amino-4-chlorobenzoic acid

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

On March 20, 2020, Liu, Jiaxin; Li, Quanzhe; Wei, Yin; Shi, Min published an article.Application In Synthesis of 2-Amino-4-chlorobenzoic acid The title of the article was Visible Light Induced Cyclization to Spirobi[indene] Skeletons from Functionalized Alkylidienecyclopropanes. And the article contained the following:

In this paper, we revealed a metal-free and visible light photoinduced method for the rapid construction of spirobi[indene] skeletons, e.g., I, providing a simple and efficient way for easy access to spirobi[indene] scaffolds under mild conditions along with a broad substrate scope and good functional group tolerance. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Application In Synthesis of 2-Amino-4-chlorobenzoic acid

The Article related to alkylidenecyclopropane nucleophile light cascade cyclization green, spiro indene preparation, Alicyclic Compounds: Spiro Compounds and other aspects.Application In Synthesis of 2-Amino-4-chlorobenzoic acid

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

On February 28, 2022, Elfeky, Sherin M.; Almehmadi, Samar J.; Tawfik, Samar S. published an article.Synthetic Route of 89-77-0 The title of the article was Synthesis, in-silico, and in-vitro study of novel chloro methylquinazolinones as PI3K-δ inhibitors, cytotoxic agents. And the article contained the following:

Through a two-step procedure, 3-amino-7-chloro-2-methylquinazolin-4(3H)-one was synthesized from 2-amino-4-chlorobenzoic acid as a starting material. The latter reacted with chloro acetylchloride, then nucleophilically substituted with various secondary amines to produce acetamide derivatives (5a-e), or underwent condensation reaction with various aldehydes to produce arylidine derivatives (6a-e). In-silico study of drug-likeness and ADME descriptors was conducted for all compounds Compounds showed good oral bioavailability, as well as good gastrointestinal absorption potential and no symptoms of liver or CNS adverse effects. In-vitro cytotoxic activity of the compounds was moderate to good when compared to staurosporine in three cell lines: HCT, MCF-7, and HepG-2. Compound 5c showed the highest cytotoxic activity against the HCT cell line (IC50 = 8.00 ± 0.33 μM), Compound 5d showed the highest cytotoxic activity against the HepG-2 cell line (IC50 = 17.78 ± 0.58 μM). Acetamide derivatives revealed higher cytotoxic activity compared to arylidine derivatives Compound 5d had the highest enzyme inhibition activity in the in-vitro PI3k-δ enzyme inhibition assay (IC50 = 1.24 ± 0.03 μM) followed by 5c (IC50 = 8.27 ± 0.19 μM). Both 5c and 5d were able to bind at the ATP binding site of the PI3k-δ enzyme in a mode similar to the native ligand where they formed H-bond interactions with the hinge region amino acid Val828 and hydrophobic interactions with other amino acids indicating an agreement between mol. docking simulation study and the biol. screening. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Synthetic Route of 89-77-0

The Article related to chloro methylquinazolinone pik inhibitor cytotoxic agent, Placeholder for records without volume info and other aspects.Synthetic Route of 89-77-0

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

Kaliraj, S.; Jeyalakshmi, R.; Kathiravan, M. K.; Madhavan, T.; Devi, Arikketh published an article in 2021, the title of the article was Design, molecular docking and biological evaluation of fused thienopyrimidines and quinazoline.Electric Literature of 89-77-0 And the article contains the following content:

The anticancer activity of the condensed pyrimidine and quinazoline moieties are pronounced with a different pathway. Thienopyrimidine is considered as ring equivalent bioisosteres of quinazolines and present in other heterocyclic compounds including thienopyrimidine. The present investigation focused on the synthesis of thienopyrimidine and quinazoline derivatives for their anticancer activity against the human oral squamous carcinoma-3 (HSC-3) cell line. The synthesized compound confirmed for their structural characteristics from spectral anal. and tested for anti-proliferative activity from MTT assay. The electron-withdrawing group in 4-chloro thienopyrimidines and amino ester derivate/facilitate the inhibition of cancer cells. Further probing by docking studies revealed that the compounds exhibit possible interactions with VEGF, FGFR and c-Met proteins, which are known to have a role in the pathogenesis of oral squamous cell carcinoma. Among the derivatives a moderate activity demonstrated by substituted 4-chloro-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]-pyrimidine (4a) and Et 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate (1a) derivatives Lack of chirality and the presence of bulky substituents in few of the compounds were found to be the cause for lower potency. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Electric Literature of 89-77-0

The Article related to fused thienopyrimidine quinazoline mol docking biol evaluation, Placeholder for records without volume info and other aspects.Electric Literature of 89-77-0

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

On March 5, 2022, Ahmad, Iqrar; Akand, Sazedur Rahman; Shaikh, Matin; Pawara, Rahul; Manjula, S. N.; Patel, Harun published an article.COA of Formula: C7H6ClNO2 The title of the article was Synthesis, molecular modelling study of the methaqualone analogues as anti-convulsant agent with improved cognition activity and minimized neurotoxicity. And the article contained the following:

In the current research, methaqualone derivatives were synthesized and assessed for their anti-convulsant activity. Among them, compounds 3, 4, 6, 7 and 11 exhibited significant anti-convulsant activities with ED50 values of 132.23 mg/kg, 120.34 mg/kg, 100.78 mg/kg, 145.89 mg/kg, and 148.46 mg/kg, resp. The toxicity profiling (TD50) of these compounds (3, 4, 6, 7 and 11) demonstrated that these drugs caused only a minor neurol. impairment. The PI scores of these compounds (3, 4, 6, 7 and 11) were higher than the reference drug (methaqualone PI: 1.99). The acetylcholinesterase enzyme level is significantly reduced in these compounds, indicating the enhancement of cognition activity. Pharmacophoric modeling and mol. docking studies against the human GABA-A receptor are in close agreement with each other. Mol. dynamic simulation of compound 6 indicates that it remains stable with the human GABA-A receptor for a 100 ns time span. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).COA of Formula: C7H6ClNO2

The Article related to methaqualone anticonvulsant cognition neurotoxicity mol docking, Placeholder for records without volume info and other aspects.COA of Formula: C7H6ClNO2

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

On March 15, 2021, Abdulwahab, Muhammad Kumayl; Tan, Ke Han; Dzulkeflee, Rashidi; Leong, Kok Hoong; Heh, Choon Han; Ariffin, Azhar published an article.Safety of 2-Amino-4-chlorobenzoic acid The title of the article was In-silico Studies of the Antiproliferative Activity of New Anilinoquinazoline Derivatives Against NSCLC Cells.. And the article contained the following:

The current reversible epidermal growth factor (EGFR) tyrosine kinase inhibitors of non-small cell lung cancer (NSCLC) have been resisted by T790M mutation, while the irreversible inhibitors introduced to overcome the mutation have faced resistance from C979S mutation. In the effort to discover potentially improved reversible EGFR inhibitors, a series of new anilinoquinazoline derivatives with modification on the 2nd carbon on the aniline ring was synthesized. The derivatives were tested for their antiproliferative activity against NSCLC cell lines with wild-type (A549), exon 19 deletion mutated (H1650) and L858R+T790M (H1975) mutated EGFR kinases. Three derivatives (4-6) performed better than the standard drug, gefitinib, in all cell lines. Derivative 5 recorded the lowest IC50 values in all cell lines (A549: 24.60 ± 0.75 μM, H1650: 14.83 ± 0.54 μM, H1975: 21.72 ± 1.21 μM). A mol. docking study followed by mol. dynamics simulations was performed on derivative 5 and gefitinib using wild-type EGFR kinase (WT-EGFR) and L858R+T790M mutated kinase (LRTM-EGFR) to provide an understanding of their binding mechanisms. In WT-EGFR kinase, derivative 5 recorded better hydrogen bonding occupancy with MET793 (94.16%) and binding energy profile (-35.287 kcal/mol) as compared to gefitinib (91.80%, -26.071 kcal/mol). In LRTM-EGFR kinase, derivative 5 recorded better hydrogen bonding occupancy with MET793 (93.68%) as compared to gefitinib (91.48%). Derivative 5 also recorded addnl. hydrogen bonding interactions with ASP855, with a total of 60.61% occupancy as well as a better energy profile (-42.867 kcal/mol) as compared to gefitinib (-41.778 kcal/mol). The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Safety of 2-Amino-4-chlorobenzoic acid

The Article related to anilinoquinazolin antiproliferative activity kinase inhibitor mol docking, Placeholder for records without volume info and other aspects.Safety of 2-Amino-4-chlorobenzoic acid

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

On May 19, 2022, Sabbah, Dima A.; Samarat, Hla H.; Al-Shalabi, Eveen; Bardaweel, Sanaa K.; Hajjo, Rima; Sweidan, Kamal; Khalaf, Reema Abu; Al-Zuheiri, Aya M.; Abushaikha, Ghassan published an article.Name: 2-Amino-4-chlorobenzoic acid The title of the article was Design, Synthesis, and Biological Examination of N-Phenyl-6-fluoro-4-hydroxy-2-quinolone-3-carboxamides as Anticancer Agents. And the article contained the following:

Cancer is one of the leading causes of death worldwide, and it has a major impact on public health. Phosphatidylinositol 3-kinase (PI3Kα) has been recognized as a promising drug target for developing anticancer agents. Herein, a series of N-phenyl-6-fluoro-4-hydroxy-2-quinolone-3-carboxamides was developed to target PI3Kα. All synthesized compounds were characterized using FT-IR, NMR (1H and 13C) and elemental anal. All synthesized chem. analogs exerted distinctive anticancer activity. They inhibited the growth of human epithelial colorectal adenocarcinoma (Caco-2) with IC50 values between 48.63-378 μM, and human colon cancer (HCT-116) cell lines with IC50 values between 44-664 μM. Computational modeling studies provided important biol. insight. Induced-fit docking (IFD) studies showed that the synthesized chem. analogs fit the kinase catalytic domains and form a significant H-bond interaction network with key amino acids at the biding site. Furthermore, cheminformatics analyses indicated that all synthesized compounds were drug-like permitting further animal testing or clin. development. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Name: 2-Amino-4-chlorobenzoic acid

The Article related to phenylfluoro hydroxyquinolone carboxamide anticancer agent clin development, Placeholder for records without volume info and other aspects.Name: 2-Amino-4-chlorobenzoic acid

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

Auti, Prashant S.; Nandi, Arijit; Kumari, Vijeta; Paul, Atish T. published an article in 2022, the title of the article was Design, synthesis, biological evaluation and molecular modelling studies of oxoacetamide warhead containing indole-quinazolinone based novel hybrid analogues as potential pancreatic lipase inhibitors.Related Products of 89-77-0 And the article contains the following content:

A novel series of indolyl oxoacetamide-quinazolinone hybrid analogs (9aa-9df) were designed, synthesized, and evaluated for their in vitro pancreatic lipase (PL) inhibitory potential which may lead to efficient anti-obesity agents. All the synthesized hybrid analogs exhibited moderate to potent PL inhibitory activity (IC50 = 32.51 to 4.86 μM). Among all the analogs, 9ak, 9af, 9aj, and 9ah were found to have the most potent PL inhibitory activity (IC50 = 4.86, 5.73, 5.83, and 5.94 μM resp.), as compared to orlistat (IC50 = 0.86 μM). The most potent analogs 9af and 9ak were found to inhibit PL competitively with an inhibition constant (Ki) of 2.136, 1.648 μM. Furthermore, the docking study confirmed the binding of analogs 9ak and 9af (MolDock score of -161.25, -133.67 kcal mol-1) that exhibited docking interactions with important active site amino acids, namely Phe 77, Tyr 114, Ser 152, Arg 256, His 263, etc. Also, the anal. of analog 9ak and 9af in SeeSAR revealed the covalent inhibition of PL. In mol. dynamics simulations of 100 ns, the complex between each analog (9ak & 9af) and PL was found to be stable (RMSD < 1.5 Å). The present work highlights the importance of a hybrid drug design approach for the development of indole and quinazolinone containing hybrids as potential PL inhibitors. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Related Products of 89-77-0

The Article related to obesity indole quinazolinone mol modeling pancreatic lipase inhibitor antiobesity, Placeholder for records without volume info and other aspects.Related Products of 89-77-0

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

On December 15, 2021, Ip, Fanny C. F.; Fu, Guangmiao; Yang, Fengzhi; Kang, Fangyuan; Sun, Peiran; Ling, Choi Ying; Cheung, Kit; Xie, Fangzhou; Hu, Yueqing; Fu, Lei; Ip, Nancy Y. published an article.Category: chlorides-buliding-blocks The title of the article was A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. And the article contained the following:

Cholinergic neurons are ubiquitous and involved in various higher brain functions including learning and memory. Patients with Alzheimer′s disease exhibit significant dysfunction and loss of cholinergic neurons. Meanwhile, such cholinergic deficits can be potentially relieved pharmacol. by increasing acetylcholine. Acetylcholinesterase (AChE) inhibitors have been used to improve cholinergic transmission in the brain for two decades and have proven effective for alleviating symptoms in the early stages of Alzheimer′s disease. Therefore, the search for AChE inhibitors for drug development is ongoing. The enzymic pocket of AChE has long been the target of several drug designs over the last two decades. The peripheral and catalytic sites of AChE are simultaneously bound by several dimeric mols., enabling more-efficient inhibition. Here, we used 6-chlorotacrine and the tetrahydroquinolone moiety of huperzine A to design and synthesize a series of heterodimers that inhibit AChE at nanomolar potency. Specifically, 6-[3-(6-chloro-1,2,3,4-tetrahydro-acridin-9-ylamino)propylamino]-5,6,7,8-tetrahydro-1H-quinolin-2-one inhibits AChE with an IC50 < 1 nM and spares butyrylcholinesterase. Administration of 6-[3-(6-chloro-1,2,3,4-tetrahydro-acridin-9-ylamino)propylamino]-5,6,7,8-tetrahydro-1H-quinolin-2-one to mouse brain slices restores synaptic activity impaired by pirenzepine, a muscarinic M1-selective antagonist. Moreover, oral administration of 6-[3-(6-chloro-1,2,3,4-tetrahydro-acridin-9-ylamino)propylamino]-5,6,7,8-tetrahydro-1H-quinolin-2-one to C57BL/6 mice enhances hippocampal long-term potentiation in a dose-dependent manner and is detectable in the brain tissue. All these data supported that 6-[3-(6-chloro-1,2,3,4-tetrahydro-acridin-9-ylamino)propylamino]-5,6,7,8-tetrahydro-1H-quinolin-2-one is a potential cognitive enhancer and is worth for further exploration. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Category: chlorides-buliding-blocks

The Article related to tacrine tetrahydroquinoline heterodimer acetylcholinesterase inhibitor, cognitive function, dementia, electrophysiological recordings, hybrid, synaptic plasticity, Placeholder for records without volume info and other aspects.Category: chlorides-buliding-blocks

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