7250-19-3Relevant articles and documents
Design, synthesis, antimicrobial evaluation, and molecular docking of novel chiral urea/thiourea derivatives bearing indole, benzimidazole, and benzothiazole scaffolds
Lafzi, Ferruh,Kilic, Deryanur,Yildiz, Melike,Saracoglu, Nurullah
, (2021/05/27)
Urea/thiourea derivatives with heteroaromatic scaffolds such as indole, benzimidazole, and benzothiazole were designed, synthesized, and evaluated for their potential antimicrobial activity in vitro assays to establish against B. cereus, S. aureus, E. coli, and P. aeruginosa. Our results indicate that compounds are only active in gram-positive bacteria. Molecular docking studies were carried out for the most efficient compounds to understand the interactions with proteins involved in peptidoglycan synthesis. ADME calculations indicate that these compounds are more likely to be taken via the oral route. In summary, these findings may contribute to the design and development of candidates for more effective therapeutics in biological systems.
First-Row Transition Metal and Lithium Pyridine-ene-amide Complexes Exhibiting N- and C-Isomers and Ligand-Based Activation of Benzylic C-H Bonds
Lindley, Brian M.,Wolczanski, Peter T.,Cundari, Thomas R.,Lobkovsky, Emil B.
supporting information, p. 4656 - 4668 (2015/10/28)
Ene-amines Z-3-(2-pyridyl)-1-aza(2,6-iPr2-Ph)propene, (pynac)H, and 2-(2-pyridyl)-1-aza(2,6-R,R′-Ph)propene, (pyEA-ArRR′)H, were synthesized by condensation procedures; corresponding lithium or potassium ene-amides were prepared via standard deprotonation protocols. Addition of 2 equiv of (pynac)H to {(Me3Si)2N}2Fe(THF) or 2 Li(pynac) to FeBr2(THF)2 afforded (pynac)2Fe (1), while treatment of CrCl2(THF)2, MnCl2, FeBr2(THF)2, and CoCl2py4 with 2 equiv of (pyEA-AriPr2)K afforded pseudotetrahedral (pyEA-AriPr2)2M (2-M, M = Cr, Mn, Fe) and (pyEA-AriPr2)2Co-py (2-Co-py). Diamagnetic (κ-C,N-pyEA-AriPr2)3Co (3) was prepared in low yield (～7%) from CoCl2, and its Co-C(sp3) linkages are unusually low in field strength. Reactivity studies yielded little clean reactivity, but thermolysis of 2-Co-py afforded the bis-indolamide derivative {κ-N,N-N(C6H3(2-iPr)CMe2C(Me)(2-py)}2Co (5-Co), and related thermolyses of 2-M (M = Cr, Mn, Fe), conducted on NMR tube scales, generated related 5-M (M = Cr, Mn, Fe) at roughly the same rates. This observation prompted thermolyses of (pyEA-ArRR′)Li, which rearrange to their corresponding indolamides in >90% yields. Rate studies, accompanied by KIE and EIE observations, revealed that an initial hydrogen transfer is reversible and is likely to correspond to an anionic rearrangement, whereas C-C bond formation is rate-determining, as suggested by accompanying calculations. X-ray structure determinations of 1, 2-Fe, 2-Co-py, 3, and 5-Co were conducted.
Three-component reaction involving metal-free heteroannulation of N-Boc-3-amido indole, aryl aldehydes, and aromatic alkynes under microwave conditions: Synthesis of highly diversified δ-carbolines
Sharma, Sudhir K.,Mandadapu, Anil K.,Saifuddin, Mohammad,Gupta, Sahaj,Agarwal, Piyush K.,Mandwal, Ashok K.,Gauniyal, Harsh M.,Kundu, Bijoy
experimental part, p. 6022 - 6024 (2010/11/18)
An efficient synthesis toward highly diversified δ-carbolines via one-pot multicomponent reaction using N-Boc-3-amido indoles, aryl aldehydes, and aromatic terminal alkynes under microwave conditions has been described.
