1234-30-6Relevant articles and documents
Radical Anion Promoted Chemoselective Cleavage of Csp2-S Bond Enables Formal Cross-Coupling of Aryl Methyl Sulfones with Alcohols
Bai, Jixiang,Wang, Tianxin,Dai, Botao,Liu, Qingchao,Yu, Peiyuan,Jia, Tiezheng
, p. 5761 - 5765 (2021/08/16)
A novel formal cross-coupling of aryl methyl sulfones and alcohols affording alkyl aryl ethers via an SRN1 pathway is developed. Two marketed antitubercular drugs were efficiently prepared employing this approach as the key step. A dimsyl-anion initiated radical chain process was revealed as the major pathway. DFT calculations indicate that the formation of a radical anion via nucleophilic addition of alkoxide to the aryl radical is the key step in determining the observed chemoselectivity.
Novel non-peptidic small molecule inhibitors of secreted aspartic protease 2 (SAP2) for the treatment of resistant fungal infections
Dong, Guoqiang,Liu, Yang,Wu, Ying,Tu, Jie,Chen, Shuqiang,Liu, Na,Sheng, Chunquan
supporting information, p. 13535 - 13538 (2019/01/05)
Targeting secreted aspartic protease 2 (SAP2), a kind of virulence factor, represents a new strategy for antifungal drug discovery. In this report, the first-generation of small molecule SAP2 inhibitors was rationally designed and optimized using a structure-based approach. In particular, inhibitor 23h was highly potent and selective and showed good antifungal potency for the treatment of resistant Candida albicans infections.
Molecular modeling and synthesis of some new 2-imino-4-thiazolidinone derivatives with promising TNF-α inhibitory activity
Ali, Yakub,Alam, Mohammad Sarwar,Hamid, Hinna,Husain, Asif,Dhulap, Abhijeet,Hussain, Firasat,Bano, Sameena,Kharbanda, Chetna
, p. 711 - 723 (2016/01/12)
A new series of thirty two 2-imino-4-thiazolidinone derivatives were synthesized, and the synthesized compounds were docked for in silico studies against the TNF-α target. The predicted results were confirmed through an in vitro TNF-α study which revealed that compounds 3f and 3g showed better TNF-α inhibition as compared to the standard drug indomethacin without causing any cytotoxicity. Fourteen compounds exhibiting significant in vitro TNF-α activity were further tested for in vivo anti-inflammatory activity by a carrageenan induced method. Compounds 3f and 3g showed better inhibition of inflammation in vivo as compared to the standard drug without causing any damage to the stomach. Furthermore, an immunohistochemical study showed that the compounds 3f and 3g exhibited better reduction in protein expression of TNF-α as compared to indomethacin. The in silico, in vitro and in vivo studies suggested that the compounds 3f and 3g might be considered as potent anti-inflammatory agents.
A highly efficient one-pot method for the synthesis of thioureas and 2-imino-4-thiazolidinones under microwave conditions
Chau, Chi-Min,Chuan, Tzu-Jung,Liu, Kuan-Miao
, p. 1276 - 1282 (2014/01/06)
A one-pot synthesis of symmetrical and unsymmetrical substituted thioureas and 2-imino-4-thiazolidinones from simple starting materials under microwave irradiation and solventless conditions without base additives is presented. Various di- and trisubstituted thioureas are obtained in good yields in a few minutes. The sequential, three-component, one-pot synthesis of 2-imino-4-thiazolidinone derivatives is also studied, with satisfactory results obtained.
Synthesis of thioureas in ionic liquid medium
Halimehjani, Azim Ziyaei,Farahbakhsh, Fataneh
, p. 284 - 288 (2013/08/26)
A highly efficient procedure for the synthesis of symmetrical thioureas by means of simple condensation of primary amines and carbon disulfide in 1-butyl-3-methylimidazolium chloride [BMIM][Cl] as a cheap and commercially available ionic liquid is presented. This procedure works for aromatic and aliphatic primary amines and give high to excellent yields of symmetrical thioureas without need for any catalyst or tedious work-up.
