2293-07-4Relevant articles and documents
Thiazolidine-4-one clubbed pyrazoles hybrids: Potent α-amylase and α-glucosidase inhibitors with NLO properties
Duhan, Meenakshi,Kadyan, Kulbir,Kumar, Parvin,Panihar, Neeraj,Saini, Sangeeta,Sindhu, Jayant
, p. 1573 - 1587 (2020)
Molecular hybrids based on thiazolidin-4-one and pyrazolyl pharmacophore (THZP) as new antidiabetic agents were synthesized. Two sets of signals came into view in 1H NMR of THZP8-THZP14 exhibited the presence of a configurational isomeric mixture of 2E,5Z (38.24%-41.58%) and 2Z,5Z isomers (58.42%-61.76%), which was further endorsed by density functional theory (DFT) studies. All the compounds exhibit promising nonlinear optical properties (NLO). Further, the biological potential of THZPs was explored in terms of α-amylase and α-glucosidase inhibition. DFT-based descriptors were calculated to describe the reactivity, and a relationship was developed with biological activities. THZP9 and THZP14 showed remarkable inhibition of α-amylase and α-glucosidase with IC50 9.90μM and 4.84μM, respectively, as compared with standard drug acarbose.
Eco-efficient one-pot tandem synthesis of 1-aryl-1H-tetrazol-5-amine by CAN via in situ generated 1-phenylthiourea and heterocumulene
Kondhare, Dasharath D.,Bhadke, Venkat V.,Deshmukh, Sushma S.,Wakhradkar, Mahesh G.,Totawar, Balaji B.
, (2021/07/28)
A simple, cost-effective, environmentally benign, and efficient one-pot tandem approach to the synthesis of pharmaceutically important 1-aryl-1H-tetrazole-5-amines 3a-k and 4a-k has been described. The reaction utilized 1-phenyl thiourea, which was generated in situ from aqueous ammonia and isocyanates 1a-k, for the formation of heterocumenes using sodium azide, triethylamine, and ceric ammonium nitrate (CAN) to obtain various aryl-substituted 1H-tetrazole-5-amines (3a-k) in good to excellent yields.
Convenient Multicomponent One-Pot Synthesis of 2-Iminothiazolines and 2-Aminothiazoles Using Elemental Sulfur Under Aqueous Conditions
ábrányi-Balogh, Péter,Domján, Attila,Gao, Qinghe,Han, Xinya,Keser?, Gy?rgy M.,Marlok, Bence,Németh, András Gy.
supporting information, p. 3587 - 3597 (2021/07/22)
Herein, we present a novel one-pot aqueous reaction for the synthesis of 2-iminothiazolines and 2-aminothiazoles using isocyanides, amines, sulfur, and 2′-bromoacetophenones. The three-component preparation of thioureas is followed by the one-pot cyclization leading to the heterocyclic product. This efficient and mild procedure features excellent step- and atom-economy and enables the chromatography-free preparation of diversely substituted 2-iminothiazoline and 2-aminothiazole derivatives.
