1932-36-1Relevant articles and documents
Thiourea derivatives, simple in structure but efficient enzyme inhibitors and mercury sensors
Alamery, Salman,Batiha, Gaber El-Saber,Bibi, Maryam,Khan, Ezzat,Muhammad, Mian,Rahman, Faizan Ur,Shah, Abdul Bari,Shahzad, Adnan,Tahir, Muhammad Nawaz,Ullah, Farhat,Zahoor, Muhammad
supporting information, (2021/08/06)
In this study six unsymmetrical thiourea derivatives, 1-isobutyl-3-cyclohexylthiourea (1), 1-tert-butyl-3-cyclohexylthiourea (2), 1-(3-chlorophenyl)-3-cyclohexylthiourea (3), 1-(1,1-dibutyl)-3-phenylthiourea (4), 1-(2-chlorophenyl)-3-phenylthiourea (5) an
Inhibition of adipogenesis by thiourea derivatives
Siddiqui, Hina,Shafi, Sarah,Mukhtar, Farah,Ejaz, Asma,Atta-Ur-Rahman,Choudhary, M. Iqbal
, p. 508 - 515 (2018/07/25)
Background: Obesity is one of the major health problems with inherent risk of type 2 diabetes, hypertension, CVDs, etc. Adipogenesis is a major contributor in the process of obesity. Inhibition of adipocytes differentiation is one of the key approaches to treat obesity. Objective: To discover the new inhibitors of adipogenesis as the treatment for obesity. Method: We describe here, the synthesis, and anti-adipogenic activity of thiourea derivatives 1-14. These derivatives were synthesized by the reactions of phenyl and pentafluorophenyl isothiocyanate with different aromatic amines. Pure compounds 1-14 were evaluated for their in vitro antiadipogenesis activity employing 3T3-L1 cells lines. Results: Compounds 1-3, 5-9, and 11-14 significantly inhibited the pre-adipocyte differentiation into adipocytes, which was measured by staining the cells, and through morphological examination. Compound 10 (1-(4"-Chlorophenyl)-3-(pentafluorophenyl)-thiourea) showed a potent inhibition of adipocyte differentiation with IC50 = 740.00 ± 2.36 nM, which was more potent than the standards, epigallocatechin gallate (IC50 = 16.73 ± 1.34 μM), and curcumin (IC50 = 18.62 ± 0.74 μM). All other compounds showed a moderate to weak anti-adipogenesis activity. Compounds 1- 14 were also evaluated for their cytotoxicity. Compounds 3, 10, and 14 showed some toxicity to the cancer cell lines, while compounds 2, 3, 10, 12, and 14 showed a moderate to weak cytotoxicity against the normal cell lines. Conclusion: All the compounds reported in this paper are known, except compound 11. They have been identified as new inhibitors of Adipogenesis. Adipogenesis is the process of adipocytes differentiation from pre-adipocytes. This extensively studied model of cell diff differentiation. Further synthetic modifications, and optimization of anti-adipogenic activity may lead to the development of anti-obesity agents.
An "on-water" exploration of CuO nanoparticle catalysed synthesis of 2-aminobenzothiazoles
Rout, Saroj Kumar,Guin, Srimanta,Nath, Jayashree,Patel, Bhisma K.
, p. 2491 - 2498 (2013/02/21)
An "on-water" one-pot process has been engineered for the preparation of 2-aminobenzothiazole from ortho-halo (-F, -Cl, -Br and -I) substituted unsymmetrical thioureas. For ortho -I and -Br substrates the reactions afford 2-aminobenzothiazoles under metal free condition promoted by base. However, the relatively inert ortho -Cl and -F substrates undergo intramolecular arylthiolation only in the presence of CuO nanoparticles yielding 2-aminobenzothiazoles. This methodology provides easy access to aminobenzothiazoles utilising even the ortho -Cl and -F substrates. The catalyst is recyclable several times without loss of substantial activity. Other remarkable features include the wide range of functional group tolerance, absence of chromatographic purification (for ortho -I and -Br substrates) and providing moderate to excellent yield of the products under mild conditions, thus rendering the methodology as a highly eco-friendly alternative to the existing methods.