479533-85-2Relevant academic research and scientific papers
Synthesis and erythroid induction activity of new thiourea derivatives
Siddiqui, Hina,Shafi, Sarah,Ali, Hamad,Musharraf, Syed Ghulam
, p. 121 - 133 (2021/03/03)
Background: The use of medicinal agents to augment the fetal hemoglobin (HbF) accretion is an important approach for the treatment of sickle-cell anemia and β-thalassemia. HbF inducers have the potential to reduce the clinical symptoms and blood transfusion dependence in the patients of β-hemoglobinopathies. Objective: The current study was aimed to examine the erythroid induction potential of newly synthesized thiourea derivatives. Methods: Thiourea derivatives 1-27 were synthesized by using environmentally friendly methods. Compounds 3, 10 and 22 were found to be new. The structures of synthesized derivatives were de-duced by using various spectroscopic techniques. These derivatives were then evaluated for their erythroid induction using the human erythroleukemic K562 cell line, as a model. The benzidine-H2 O2 assay was used to evaluate erythroid induction, while HbF expression was studied through immunocyto-chemistry using the Anti-HbF antibody. Cytotoxicity of compounds 1-27 was also evaluated on mouse fibroblast 3T3 cell line and cancer Hela cell line using MTT assay. Result: All the compounds (1-27) have not been reported for their erythroid induction activity previ-ously. Compounds 1, 2, and 3 were found to be the potent erythroid inducing agents with % induction of 45± 6.9, 44± 5.9, and 41± 6.1, at 1.56, 0.78, and 0.78 μM concentrations, respectively, as compared to untreated control (12 ± 1 % induction). Furthermore, compound 1, 2, and 3 significantly induced fetal hemoglobin the expression up to 4.2-fold, 4.06-fold, and 3.52-fold, respectively, as compared to untreated control. Moreover, the compounds 1-4, 6-9, 11, 12, 15, 17, 19, 22, 23, and 25 were found to be non-cytotoxic against the 3T3 cell line. Conclusion: This study signifies that the compounds reported here may serve as the starting point for the designing and development of new fetal hemoglobin inducers for the treatment of β-hemoglobinopathies.
Catalyst-free solventless synthesis of polysubstituted urea Method for preparing thioureas and chiral ureas and thiourea compounds
-
Paragraph 0105-0111; 0126-0132, (2021/09/29)
The invention discloses a method for synthesizing polysubstituted urea, thiourea and chiral urea and thiourea compounds without catalyst without solvent, and the method comprises A contact reaction of an amine compound with a structure shown B as shown first in a non-catalyst and a solventless condition to prepare a polysubstituted urea or thiourea compound with a structure as shown C. R1 And R2 Each independently selected from a hydrocarbyl or substituted hydrocarbyl group, R3 The method is selected from H, hydrocarbyl or substituted hydrocarbyl, X is S or o. The method solves the defect that a catalyst and/or a solvent need to be used in the synthesis of urea and thiourea compounds in the prior art.
