1615-02-7Relevant articles and documents
Structural elucidation and bioassays of newly synthesized pentavalent antimony complexes
Iftikhar, Tuba,Rauf, Muhammad Khawar,Sarwar, Sidra,Badshah, Amin,Waseem, Durdana,Tahir, Muhammad Nawaz,Khan, Amjad,Khan, Khalid Mohammad,Khan, Gul Majid
, p. 89 - 96 (2017)
Antimony (V) organometallics (1–5) have been synthesized with general formula [SbR′3(O2CR)2], where R' = phenyl, p-tolyl and O2CR are substituted cinnamates. These complexes have been characterized by FT-IR analysis, multinuclear (1H, 13C) NMR spectroscopy and single crystal X-ray diffraction analysis. The crystal structures of [Sb(phenyl)3(4-ClC6H4C2H2O2C)2] (1) and [Sb(p-tol)3(4-OCH3C6H4C2H2O2C)2].CHCl3 (5) displayed distorted geometry between trigonal bipyramidal and square pyramidal with monomeric structure at a five coordinated Sb center. Starting reagents and complexes were evaluated for anticancer, antileishmanial, antibacterial and alpha amylase inhibition potentials. It was observed that complexes 3, 4 and 5 showed significant (p 0.05) antileishmanial and anticancer activities against Leishmania tropica KWH23 promastigotes and HepG2 cell lines respectively. Antibacterial activity of compound 3 was also significant against E. coli (MIC: 5.55 μg/mL), K. pneumoniae (MIC: 16.66 μg/mL), S. aureus (MIC: 5.55 μg/mL) and P. aeruginosa (MIC: 50 μg/mL). Hence, these new antimony complexes can act as good drug candidates.
Design, synthesis, and evaluation of different scaffold derivatives against NS2B-NS3 protease of dengue virus
Ganji, Lata R.,Gandhi, Lekha,Musturi, Venkataramana,Kanyalkar, Meena A.
, p. 285 - 301 (2020/11/19)
The number of deaths or critical health issues is a threat in the infection caused by Dengue virus, which complicates the situation, as only symptomatic treatment is the current solution. In this regard we have targeted the dengue protease NS2B-NS3 that is responsible for the replication. The series was designed with the help of molecular modeling approach using docking protocols. The series comprised of different scaffolds viz. cinnamic acid analogs (CA1–CA11), chalcone (C1–C10) and their molecular hybrids (Lik1–Lik10), analogs of benzimidazole (BZ1-BZ5), mercaptobenzimidazole (BS1-BS4), and phenylsulfanylmethylbenzimidazole (PS1-PS4). Virtual screening of various natural phytoconstituents was employed to determine the interactions of designed analogs with the residues of catalytic triad in the active site of NS2B-NS3. We have further synthesized the selected leads. The synthesized analogs were evaluated for the cytotoxicity and NS2B-NS3 protease inhibition activity and compared with known anti-dengue natural phytoconstituent quercetin as the standard. CA2, BZ1, and BS2 were found to be more potent and efficacious than the standard quercetin as evident from the protease inhibition assay.
Chlorination Reaction of Aromatic Compounds and Unsaturated Carbon-Carbon Bonds with Chlorine on Demand
Liu, Feng,Wu, Na,Cheng, Xu
supporting information, p. 3015 - 3020 (2021/05/05)
Chlorination with chlorine is straightforward, highly reactive, and versatile, but it has significant limitations. In this Letter, we introduce a protocol that could combine the efficiency of electrochemical transformation and the high reactivity of chlorine. By utilizing Cl3CCN as the chloride source, donating up to all three chloride atom, the reaction could generate and consume the chlorine in situ on demand to achieve the chlorination of aromatic compounds and electrodeficient alkenes.
Dual Nickel/Ruthenium Strategy for Photoinduced Decarboxylative Cross-Coupling of α,β-Unsaturated Carboxylic Acids with Cycloketone Oxime Esters
Gao, Ang,Jiang, Run-Chuang,Liu, Chuang-Chuang,Liu, Qi-Le,Lu, Xiao-Yu,Xia, Ze-Jie
supporting information, p. 8829 - 8842 (2021/06/30)
Herein, a dual nickel/ruthenium strategy is developed for photoinduced decarboxylative cross-coupling between α,β-unsaturated carboxylic acids and cycloketone oxime esters. The reaction mechanism is distinct from previous photoinduced decarboxylation of α,β-unsaturated carboxylic acids. This reaction might proceed through a nickelacyclopropane intermediate. The C(sp2)-C(sp3) bond constructed by the aforementioned reaction provides an efficient approach to obtaining various cyanoalkyl alkenes, which are synthetically valuable organic skeletons in organic and medicinal chemistry, under mild reaction conditions. The protocol tolerates many critical functional groups and provides a route for the modification of complex organic molecules.