Tag: M.W=200-250

Roecker, Anthony J.; Mercer, Swati P.; Harrell, C. Meacham; Garson, Susan L.; Fox, Steven V.; Gotter, Anthony L.; Prueksaritanont, Thomayant; Cabalu, Tamara D.; Cui, Donghui; Lemaire, Wei; Winrow, Christopher J.; Renger, John J.; Coleman, Paul J. published the artcile< Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis>, Product Details of C6H2Cl2N2S, the main research area is orexin receptor antagonist sleep acetonitrile diphosgene dichloropyrimidine; Antagonist; Bioactivation; Orexin; Pyrimidine; Sleep.

Recent clin. studies have demonstrated that dual orexin receptor antagonists (OX1R and OX2R antagonists or DORAs) represent a novel treatment option for insomnia patients. Previously we have disclosed several compounds in the diazepane amide DORA series with excellent potency and both preclin. and clin. sleep efficacy. Addnl. SAR studies in this series were enabled by the expansion of the acetonitrile-assisted, diphosgene-mediated 2,4-dichloropyrimidine synthesis to novel substrates providing an array of Western heterocycles. These heterocycles were utilized to synthesize analogs in short order with high levels of potency on orexin 1 and orexin 2 receptors as well as in vivo sleep efficacy in the rat.

Bioorganic & Medicinal Chemistry Letters published new progress about Drug bioavailability. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Product Details of C6H2Cl2N2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Zhu, Wufu; Chen, Chen; Sun, Chengyu; Xu, Shan; Wu, Chunjiang; Lei, Fei; Xia, Hui; Tu, Qidong; Zheng, Pengwu published the artcile< Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors>, Recommanded Product: 2,4-Dichlorothieno[2,3-d]pyrimidine, the main research area is thienopyrimidine preparation mTOR PI3Kalpha inhibitor treatment cancer; hydrazinylthienopyrimidine chromenecarboxaldehyde condensation; Chromone; Cytotoxicity; Docking; PI3Kα; Synthesis; Thienopyrimidine; mTOR.

Two series of thienopyrimidine derivatives, e.g, I and II, bearing chromone moiety were designed and synthesized. All the compounds were evaluated for inhibitory activity against mTOR kinase at a concentration of 10uM. Four selected compounds were further evaluated for the IC50 values against mTOR kinase, PI3Kα kinase and two cancer cell lines. One of the target compounds exhibited moderate to excellent mTOR/PI3Kα kinase inhibitory activity and cytotoxicity. The most promising compound II showed good inhibitory activity against mTOR/PI3Kα kinase and good antitumor potency for H460 and PC-3 cell lines with IC50 values of 0.16 ± 0.03 μM, 2.35 ± 0.19 μM, 1.20 ± 0.23 μM and 0.85 ± 0.04 μM, which were 8.6, >5, 7.9 and 19.1 times more active than compound I (1.37 ± 0.07 μM, >10 μM, 9.52 ± 0.29 μM, 16.27 ± 0.54 μM), resp. Structure-activity relationships (SARs) and docking studies indicated that the chromone moiety is necessary for the potent antitumor activity and cytotoxicity of these compounds Substitution of the chromone moiety at the 6-position has a significant impact to the inhibitory activity, in particular a carboxylic acid group, produced the best potency.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Recommanded Product: 2,4-Dichlorothieno[2,3-d]pyrimidine.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Heffron, Timothy P.; Wei, Bin Qing; Olivero, Alan; Staben, Steven T.; Tsui, Vickie; Do, Steven; Dotson, Jennafer; Folkes, Adrian J.; Goldsmith, Paul; Goldsmith, Richard; Gunzner, Janet; Lesnick, John; Lewis, Cristina; Mathieu, Simon; Nonomiya, Jim; Shuttleworth, Stephen; Sutherlin, Daniel P.; Wan, Nan Chi; Wang, Shumei; Wiesmann, Christian; Zhu, Bing-Yan published the artcile< Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform>, Synthetic Route of 18740-39-1, the main research area is PI3K alpha inhibitor preparation antitumor.

Of the four class I phosphoinositide 3-kinase (PI3K) isoforms, PI3Kα has justly received the most attention for its potential in cancer therapy. Herein we report our successful approaches to achieve PI3Kα vs PI3Kβ selectivity for two chem. series. In the thienopyrimidine series of inhibitors, we propose that select ligands achieve selectivity derived from a hydrogen bonding interaction with Arg770 of PI3Kα that is not attained with the corresponding Lys777 of PI3Kβ. In the benzoxepin series of inhibitors, the selectivity observed can be rationalized by the difference in electrostatic potential between the two isoforms in a given region rather than any specific interaction.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Synthetic Route of 18740-39-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Prabhakar, Virupakshi; Babu, Sangu Jagadish; Jyothi, Sangu V. N. Lalitha Siva; Lahari, Sangu V. N.; Bandi, Venkateswarlu published the artcile< Synthesis, structural elucidation and anti-bacterial evaluation of some novel heterocyclic molecules derived from thieno[2,3-d]pyrimidine as a core unit>, Formula: C6H2Cl2N2S, the main research area is pyrazolyl thienopyrimidine preparation antibacterial antifungal.

A series of novel 4-(3,5-dimethyl-1H-pyrazol-1-yl)-2-substituted phenyl/heterocyclic thieno[2,3-d]pyrimidine derivatives I (R = Ph, 4-MeOC6H4, indol-5-yl, etc.) were synthesized by a facile five-step procedure that afforded advantages of mild reaction conditions, simple protocol and good yields. The final compounds were screened for their antibacterial activity against Bacillus subtilis and Staphylococcus aureus from Gram pos. group of bacteria and Escherichia coli and Klebsiella pneumoniae from Gram neg. group of bacteria and antifungal activity against Candida albicans and Aspergillus flavus. Antibacterial and antifungal activities were evaluated and compared with the standard drugs Such as Amoxicillin and Ketoconazole. From antibacterial and antifungal activity screening results, it has been observed that compounds I (R = 2-thienyl, indol-5-yl, 4-F3CC6H4, 3-pyridyl) exhibited good activity.

Organic Chemistry: Current Research published new progress about Antibacterial agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Formula: C6H2Cl2N2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Jat, Bhagchand; Santra, Swapna; Santra, Prasanta Kumar published the artcile< Synthesis and evaluation of antimicrobial activity of pyrimidine derivatives>, Formula: C6H2Cl2N2S, the main research area is pyridinylpropylphenylamino fused pyrimidine preparation antibacterial agrochem antifungal activity.

Synthesis, characterization and evaluation of antimicrobial activity of novel pyrimidine derivatives containing O, N, and S in the ring was reported. Pyrimidine derivatives were prepared in three steps. In the first step, chalcones containing -NO2 functional group were synthesized using Claisen-Schmidt condensation of aromatic aldehydes with 2-acetyl pyridine/3-acetylpyridine in methanol in the presence of aqueous NaOH. In the second step, -NO2 group was reduced to -NH2 group. Resulting compounds containing -NH2 functional group were reacted with different dichlorothienopyrimidines and dichlorofuropyrimidines in the presence of N,N-diisopropylethylamine to obtain pyrimidine derivatives Antibacterial and antifungal activity of pyrimidine derivatives were studied in-vitro. Antibacterial and antifungal activity of the newly synthesized pyrimidine derivatives will definitely inspire future researchers for the preparation of new analogs.

Asian Journal of Pharmaceutical and Clinical Research published new progress about Agrochemical fungicides. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Formula: C6H2Cl2N2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia