4-氰基吡啶置于ammonium Persulfate,硫酸,Silver Nitrate,Magnesium Chloride体系中,用 水,N,N-二甲基甲酰胺 用作溶剂,化学反应 2.41H,反应生成丙硫异烟胺 参考文献:Diarylthiazole: An Antimycobacterial Scaffold Potentially Targeting Prrb-Prra Two-Component System 标题:Diarylthiazole: An Antimycobacterial Scaffold Potentially Targeting Prrb-Prra Two-Component System 摘要:Diarylthiazole (Dat),A Hit From Diversity Screening,Was Found To Have Potent Antimycobacterial Activity Against Mycobacterium Tuberculosis (Mtb). In A Systematic Medicinal Chemistry Exploration,We Demonstrated Chemical Opportunities To Optimize The Potency And Physicochemical Properties. The Effort Led To More Than 10 Compounds With Submicromolar Mics And Desirable Physicochemical Properties. The Potent Antimycobacterial Activity,In Conjunction With Low Molecular Weight,Made The Series An Attractive Lead (Antibacterial Ligand Efficiency (Ale)>0.4). The Series Exhibited Excellent Bactericidal Activity And Was Active Against Drug-Sensitive And Resistant Mtb. Mutational Analysis Showed That Mutations In Prrb Impart Resistance To Dat Compounds But Not To Reference Drugs Tested. The Sensor Kinase Prrb Belongs To The Prrba Two Component System And Is Potentially The Target For Dat. Prrba Is A Conserved,Essential Regulatory Mechanism In Mtb And Has Been Shown To Have A Role In Virulence And Metabolic Adaptation To Stress. Hence,Dats Provide An Opportunity To Understand A Completely New Target System For Antimycobacterial Drug Discovery. Doi:10.1021/jm500833F
专利号:US-9873689-B2 优先权日:2014-11-07 标题:Synthesis of fatostatin based polycyclic compounds 发明人:CANTRELL JR WILLIAM R 权利人:FGH BIOTECH INC 摘要:The present invention relates to methods and strategies for large-scale synthesis of compounds having the chemical structure: n nThe R substituents are H, methyl, isopropyl, benzyl, cyclohexyl, cyclopropylmethyl, methoxy, tert-butyloxycarbonyl, methanesulfonyl, p-toluenesulfonyl, quinolinesulfonyl, or thiophenesulfonyl groups. The method comprises condensing prothionamide with a halo nitroacetophenone to form a nitrophenyl substituted thiazole, reducing the nitro group to form an amine and derivatizing the amine to produce the compound.
专利号:US-10487099-B2 优先权日:2017-06-30 标 题:Synthesis of hypervalent iodine reagents with dioxygen 发明人:POWERS DAVID CHARLES; MAITY ASIM; HYUN SUNG-MIN 权利人:TEXAS A & M UNIV SYS 摘要:Methods of synthesis of hypervalent iodine reagents and methods for oxidation of organic compounds are disclosed.
专利号:US-6126740-A 优先权日:1995-09-29 标 题:Solution synthesis of mixed-metal chalcogenide nanoparticles and spray deposition of precursor films 发明人:SCHULZ DOUGLAS L; CURTIS CALVIN J; GINLEY DAVID S 权利人:MIDWEST RESEARCH INST 摘要:A colloidal suspension comprising metal chalcogenide nanoparticles and a volatile capping agent. The colloidal suspension is made by reacting a metal salt with a chalcogenide salt in an organic solvent to precipitate a metal chalcogenide, recovering the metal chalcogenide, and admixing the metal chalcogenide with a volatile capping agent. The colloidal suspension is spray deposited onto a substrate to produce a semiconductor precursor film which is substantially free of impurities.
专利号:US-9890126-B2 优先权日:2012-04-24 标 题:Synthesis of novel inhibitors of isoprenoid biosynthesis (ISPF) 发明人:HAGEN TIMOTHY J; ZHANG ZHENG; LAZOWSKI ZACHARY; CLARE MICHAEL; BEGLEY DARREN W 权利人:UNIV NORTHERN ILLINOIS BOARD OF TRUSTEES; BERYLLIUM DISCOVERY CORP 摘要:Antibacterial and antimalarial IspF inhibitor compounds and compositions are described. Methods include administering described compounds and compositions to treat bacterial or parasitic infections and to inhibit parasite or bacterial growth.
专利号:US-2002068798-A1 优先权日:2000-10-13 标题:Synthesis of tin/silicon coupled rubbery polymers 发明人:HALASA ADEL FARHAN; HSU WEN-LIANG 摘要:Rubbery polymers made by anionic polymerization can be coupled with tin halides or silicon halides to improve the characteristics of the rubber for use in some applications, such as tire treads. In cases where the rubbery polymer is synthesized by anionic polymerization utilizing a polar modifier it is difficult to attain a high level of coupling. This invention is based upon the unexpected finding that the coupling efficiency of rubbery polymers made with polar modifiers can be significantly improved by initiating the anionic polymerization with an alkylsilyloxy protected functional lithium initiator having a structural formula selected from the group consisting of: (a): n n n wherein X represents a group IVa element selected from the group consisting of carbon, silicon, germanium, and tin, wherein Y represents phosphorous or nitrogen, wherein R represents alkyl groups that can be the same or different, wherein the alkyl groups contain from 1 to about 8 carbon atoms, and wherein A represents an alkylene group containing from 1 to about 12 carbon atoms.
专利号:US-4388235-A 优先权日:1982-02-12 标 题:Synthesis of peptides 发明人:ORLOWSKI RONALD C; SEYLER JAY K 权利人:ARMOUR PHARMA 摘要:New peptides are disclosed which have biological activity of the same type as known calcitonins and which have a shorter amino acid chain than natural calcitonins. Also resin peptides are disclosed which may be converted to peptides having such biological activity; and processes for producing said resin peptides and said calcitonin peptides.
1: Prothionamide. Tuberculosis (Edinb). 2008 Mar;88(2):139-40. doi: 10.1016/S1472-9792(08)70020-9. 48(3):946-52. doi: 10.1183/13993003.00438-2016. Epub 2016 Jun 10. 108(9):3106-3111. doi: 10.1016/j.xphs.2019.04.009. Epub 2019 Apr 13. 25(8):1041.e1-1041.e7. doi: 10.1016/j.cmi.2018.12.008. Epub 2018 Dec 22. 97:126-36. doi: 10.1016/j.tube.2015.09.007. Epub 2015 Oct 19. 5(2):185-200. doi: 10.4155/bio.12.301. 13(1):e0190976. doi: 10.1371/journal.pone.0190976. 8: Hicks ND, Carey AF, Yang J, Zhao Y, Fortune SM. Bacterial Genome-Wide Association Identifies Novel Factors That Contribute to Ethionamide and Prothionamide Susceptibility in Mycobacterium tuberculosis. mBio. 2019 Apr 23;10(2):e00616-19. doi: 10.1128/mBio.00616-19.
合成参考文献
摘要:Farmakologiya i Toksikologiya, 38(471), 1975 [] 摘要:Drugs in Japan, 6(726), 1982 摘要:Leiker DL. [Chemotherapy of leprosy. II. Sulfones and sulfonamides]. Ned Tijdschr Geneeskd. 1980 Jan 12;124(2):46–8. 参考文献:10.1186/s40793-015-0071-4 摘要:Han SJ, Song T, Cho Y, Kim J, Choi SY, Bang H, Chun J, Bai G, Cho S, Shin SJ. Complete genome sequence of Mycobacterium tuberculosis K from a Korean high school outbreak, belonging to the Beijing family. Environmental Microbiome. 2015 Oct 14;10(1):78. doi: 10.1186/s40793-015-0071-4.