Category: 115843-99-7

Hansa, Raj KC.; Khan, M. M. K.; Frangie, M. M.; Gilmore, D. F.; Shelton, R. S.; Savenka, A. V.; Basnakian, A. G.; Shuttleworth, S. L.; Smeltzer, M. S.; Alam, M. A. published the artcile< 4-4-(Anilinomethyl)-3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-ylbenzoic acid derivatives as potent anti-gram-positive bacterial agents>, Application of C6H4BrClFN, the main research area is anilinomethyl phenyl pyrazolyl benzoic acid preparation antibacterial cytotoxicity SAR; Antibiotics; Antimicrobial; Enterococcus; MRSA; Pyrazole; Staphylococcus aureus; Toxicity.

A collection of potent antimicrobials consisting of novel 1,3-bis-benzoic acid and trifluoromethyl Ph derived pyrazoles I [R = HO(O)C, F3C; R1 = Ph, 3-bromophenyl, 5-iodopyridin-2-yl, etc.] was synthesized and tested for antibacterial activity. The majority of trifluoromethyl Ph derivatives are highly potent growth inhibitors of Gram-pos. bacteria and showed low toxicity to human cultured cells. In particular, two compounds I [R = F3C; R1 = 3-fluoro-5-(trifluoromethyl)phenyl, 3,5-dichloro-4-fluorophenyl] were selected for addnl. studies. These compounds were highly effective against Staphylococcus aureus as shown by a low min. inhibitory concentration (MIC), a bactericidal effect in time-kill assays, moderate inhibition of biofilm formation as well as biofilm destruction and a bactericidal effect against stationary phase cells representing non-growing persister cells. Multistep resistance assays showed a very low tendency for S. aureus and Enterococcus faecalis to develop resistance through mutation. Addnl., in vivo mouse model studies showed no harmful effects at doses up to 50 mg/kg using 14 blood plasma organ toxicity markers or TUNEL assay in liver and kidney. Investigations into the mode of action by performing macromol. synthesis inhibition studies showed a broad range of inhibitory effects, suggesting targets that have a global effect on bacterial cell function.

European Journal of Medicinal Chemistry published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 115843-99-7 belongs to class bromides-buliding-blocks, and the molecular formula is C6H4BrClFN, Application of C6H4BrClFN.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Cha, Mi Young; Lee, Kwang-Ok; Kim, Jong Woo; Lee, Chang Gon; Song, Ji Yeon; Kim, Young Hoon; Lee, Gwan Sun; Park, Seung Bum; Kim, Maeng Sup published the artcile< Discovery of A Novel Her-1/Her-2 Dual Tyrosine Kinase Inhibitor for the Treatment of Her-1 Selective Inhibitor-Resistant Non-Small Cell Lung Cancer>, SDS of cas: 115843-99-7, the main research area is tyrosine kinase inhibitor quinazolinyl pyrrolidine preparation SAR.

A novel series of (S)-1-acryloyl-N-[4-(arylamino)-7-(alkoxy)quinazolin-6-yl]pyrrolidine-2-carboxamides were synthesized and evaluated as Her-1/Her-2 dual inhibitors. In contrast to the Her-1 selective inhibitors, our novel compounds are irreversible inhibitors of Her-1 and Her-2 tyrosine kinases with the potential to overcome clin. relevant, mutation-induced drug resistance. The selected compounds, 19c and 19d (I), showed excellent EGFR inhibition activity even toward the T790M mutation of Her-1 tyrosine kinase with excellent selectivity. The excellent pharmacokinetic profiles of these compounds in rats and their robust in vivo efficacy in an A431 xenograft model clearly demonstrate that they merit further investigation as novel therapeutic agents for EGFR-targeting treatment of solid tumors, especially Her-1 selective inhibitor-resistant non-small cell lung cancer.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 115843-99-7 belongs to class bromides-buliding-blocks, and the molecular formula is C6H4BrClFN, SDS of cas: 115843-99-7.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Katkova, Svetlana A.; Mikherdov, Alexander S.; Sokolova, Elina V.; Novikov, Alexander S.; Starova, Galina L.; Kinzhalov, Mikhail A. published the artcile< Intermolecular (Isocyano group)···PtII interactions involving coordinated isocyanides in cyclometalated PtII complexes>, Application of C6H4BrClFN, the main research area is platinum isocyanide cyclometalated complex preparation crystal structure DFT luminescence.

A series of platinum(II) isocyanide complexes [Pt(ppy)Cl(CNR)] (ppy = 2-phenylpyridinato-C2,N; R = Mes 1, C6H2-2,6-Me2-4-Br 2, C6H2-2-F-3-Cl-4-Br 3, naphthalen-2-yl 4) were prepared and characterized by high resolution ESI-MS, 1D and 2D NMR, IR, UV-visible absorption, and photoluminescence spectroscopies, as well as single-crystal x-ray diffraction. Anal. of x-ray diffraction data allowed the authors to identify (isocyano group)···PtII interactions where the nitrogen atom of the isocyano group acts as a π-hole donor toward a d2z-orbital of PtII. The presence of these noncovalent interactions was confirmed by DFT calculations followed by NCI anal. and topol. anal. of the electron d. distribution within the framework of Bader’s theory (QTAIM method). Processing of CSD data allowed verification of the contacts between coordinated isocyano moieties and various d9 and d8- metal-centers (AuI, AuIII, AgI, PtII, PdII, NiII, RhI) to be performed.

Journal of Molecular Structure published new progress about Crystal structure. 115843-99-7 belongs to class bromides-buliding-blocks, and the molecular formula is C6H4BrClFN, Application of C6H4BrClFN.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Alkhaibari, Ibrahim S.; Kc, Hansa Raj; Roy, Subrata; Abu-gazleh, Mohd. K.; Gilmore, David F.; Alam, Mohammad A. published the artcile< Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant Bacteria>, Recommanded Product: 4-Bromo-3-chloro-2-fluoroaniline, the main research area is trifluoromethyl phenyl pyrazole preparation antibacterial activity cytotoxicity SAR; Enterococcus faecalis; Enterococcus faecium; MRSA; Staphylococcus aureus; VRE; aniline; pyrazole.

The design, synthesis, and antimicrobial studies of 30 novel pyrazole derivatives I (R = C6H5, 3-FC6H4, 3,4-(F2)C6H3, etc.) have been described. Most of the synthesized compounds I are potent growth inhibitors of planktonic Gram-pos. bacteria with min. inhibitory concertation (MIC) values as low as 0.25μg/mL. Further studies led to the discovery of several lead compounds, which are bactericidal and potent against MRSA persisters. Compounds I (R = 4-BrC6H4, 3,5-(Cl)2-4-FC6H2, 4-Br-3-Cl-2-FC6H2) are potent against S. aureus biofilms with min. biofilm eradication concentration (MBEC) values as low as 1μg/mL.

Molecules published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 115843-99-7 belongs to class bromides-buliding-blocks, and the molecular formula is C6H4BrClFN, Recommanded Product: 4-Bromo-3-chloro-2-fluoroaniline.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary