专利号:US-2021214303-A1 优先权日:2018-05-30 标 题:Scorpion venom benzoquinone derivatives and uses thereof 发明人:ZARE RICHARD NEIL; VEYTIA-BUCHELI JOSE IGNACIO; NORIEGA EDSON NORBERTO CARCAMO; ELUMALAI GNANAMANI; SATHYAMOORTHI SHYAM; POSSANI POSTAY LOURIVAL DOMINGOS; BANERJEE SHIBDAS; HERNANDEZ PANDO ROGELIO ENRIQUE 权利人:UNIV LELAND STANFORD JUNIOR; UNIV MEXICO NAC AUTONOMA; INSTITUTO NAC DE CIENCIAS MEDICAS Y NUTRICION SALVADOR ZUBIRAN 摘要:Provided are colored 1,4-benzoquinone compounds obtained by oxidation of precursor molecules from the venom of the scorpion Diplocentrus melici (Diplocentridae family). Schemes for the chemical synthesis of these compounds using reagents commercially available are also provided. Biological assays show that the red compound (3,5-dimethoxy-2-(methylthio)cyclohexa-2,5-diene-1,4-dione) is very effective at killing Staphylococcus aureus and that the blue compound (5-methoxy-2,3-bis(methylthio)cyclohexa-2,5-diene-1,4-dione) has remarkable activity against Mycobacterium tuberculosis. The blue compound is effective against multi-drug-resistant tuberculosis (MDR-TB) and is not detrimental to lung epithelium. Both compounds were found to be cytotoxic to human neoplastic cell lines and to mononuclear cells (PBMCs).
参考标题:Efficient And Complementary Methods Offering Access To Synthetically Valuable 1,2-Dibromobenzenes 作者:Vincent Diemer,Frédéric R. Leroux,Françoise Colobert |发布日期:2011.1 摘要:In Particular, Reactions Based On The Intermediate Formation Of Benzynes. This Report Describes Short Sequences For The Synthesis Of Various Derivatives Based On Regioselective Bromination, Ortho-Metalation, And Halogen/metal Permutations. 1,2-Dibromo-3-Iodobenzene (2F), 1,2-Dibromo-4-Iodobenzene (4C), And 2,3-Di-Bromo-1,4-Diiodobenzene (5E) Act As Intermediates In These Syntheses.
合成参考文献
参考文献:10.1038/s41429-025-00809-8 摘要:Gallegos-Monterrosa R, Cid-Uribe JI, Delgado-Prudencio G, Pérez-Morales D, Banda MM, Téllez-Galván A, Carcamo-Noriega EN, Garza-Ramos U, Zare RN, Possani LD, Bustamante VH. Blue benzoquinone from scorpion venom shows bactericidal activity against drug-resistant strains of the priority pathogen Acinetobacter baumannii. J Antibiot (Tokyo). 2025 Mar;78(4):235–45.