- COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES
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The present disclosure relates to compounds according to Formulae (I), (II) and (VIII), useful for treating diseases.
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Paragraph 00229; 00230
(2019/03/12)
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- MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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Paragraph 001255
(2018/09/12)
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- End-labeled amino terminated monotelechelic glycopolymers generated by ROMP and Cu(I)-catalyzed azide-alkyne cycloaddition
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Functionalizable monotelechelic polymers are useful materials for chemical biology and materials science. We report here the synthesis of a capping agent that can be used to terminate polymers prepared by ring-opening metathesis polymerization of norbornenes bearing an activated ester. The terminating agent is a cis-butene derivative bearing a Teoc (2-trimethylsilylethyl carba-mate) protected primary amine. Post-polymerization modification of the polymer was accomplished by amidation with an azido-amine linker followed by Cu(I)-catalyzed azide-alkyne cycloaddition with propargyl sugars. Subsequent Teoc deprotection and conjugation with pyrenyl isothiocyanates afforded well-defined end-labeled glycopolymers.
- Okoth, Ronald,Basu, Amit
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supporting information
p. 608 - 612
(2013/05/23)
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- Solid phase synthesis of benzylamine-derived sulfonamide library
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Using solid phase synthesis, a library has been constructed of benzylamine-derived sulfonamides which have strong inhibitory activity against the blood coagulant thrombin. The library compounds were obtained in good yield and high purity; four of these thrombin inhibitors showed nanomolar potency (Ki 600-10 nM).
- Kim, Sang Woong,Hong, Chang Yong,Lee, Koo,Lee, Eun Ju,Koh, Jong Sung
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p. 735 - 738
(2007/10/03)
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- Studies in the Protection of Pyrrole and Indole Derivatives
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Treatment of pyrrole (1a), 2,5-dimethylpyrrole (1b), indole (3a), 2-methylindole (3b), 3-methylindole (3c), 2,3-dimethylindole (3d), 1,2,3,4-tetrahydro-9H-carbazole (5a), 5,6,7,8,9,10-hexahydrocycloheptindole (5b), and 6,7,8,9,10,11-hexahydro-5H-cyclo-octindole (5c) with sodium hydride in tetrahydrofuran, followed by phenyl t-butyl carbonate (8) gives the corresponding N-t-butoxycarbonyl (t-BOC) derivatives in satisfactory yields.By using chlorodimethyl-t-butylsilane instead of (8), N-dimethyl-t-butylsilyl derivatives are obtained, also in satisfactory yields.The use of the 2-(trimethylsilyl)ethoxycarbonyl (TEOC) group for the N-protection of the indole system, and the pivaloyloxymethyl (POM) group for the N-protection of the pyrrole and indole systems is also described.
- Dhanak, Dashyant,Reese, Colin B.
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p. 2181 - 2186
(2007/10/02)
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