- SMALL MOLECULES AGAINST CEREBLON TO ENHANCE EFFECTOR T CELL FUNCTION
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Disclosed are small molecules against cereblon to enhance effector T cell function. Methodos of making thes molecules and methods of using them to treat various disease states are also disclosed.
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- Synthesis and screening of cyclooxygenase inhibitory activity of some 1,3-dioxoisoindoline derivatives
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In this study, 15 compounds bearing N,Nphthaloylacetamide structure designed by the molecular simplification approach based on thalidomide structure were synthesized and evaluated for inhibitory potencies against cyclooxgenase (COX) isoenzymes, namely COX-1 and COX-2. The results suggested that the N,Nphthaloylacetamide structure, as a primary amide, has inhibitory activity against cyclooxygenase isoenzymes with a higher COX-1 selectivity. The conversion of the primary amide to secondary or tertiary derivatives lowered the potency but favored the COX-2 selectivity thus yielding the compounds with stronger COX-2 inhibiting activity. ECV · Editio Cantor Verlag.
- Cizmecioglu, Murat,Pabuccuoglu, Varol,Ballar, Petek,Pabuccuoglu, Aysun,Soyer, Zeynep
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p. 186 - 190
(2011/10/10)
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- Synthesis and anticonvulsant activity of N,N-phthaloyl derivatives of central nervous system inhibitory amino acids
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In order to study the influence of the length of the amino acid chain of N,N-phthaloyl-amino acid amides as analogues of the former anticonvulsant taltrimide on the seizure-antagonizing activity glycine, β-alanine and γ-aminobutyric acid (GABA) derivatives were synthesized. The corresponding taurine derivatives were also included. Generally, the glycine-derived amides showed a higher activity than the β-alanine and GABA derivatives in the maximal electroshock seizure (MES) test in mice upon intraperitoneal administration. The activity was comparable to the respective taurine derivatives. The N,N-phthaloyl-glycine amides were also active in the MES test upon oral administration to rats. No significant activity was noted in the seizure threshold test with subcutaneous pentylene-tetrazole. The ED50 of N,N-phthaloyl-glycine ethyl amide (4b) in the MES test upon intraperitoneal administration to mice was 19.1 mg/kg. On a molar basis this activity is comparable to the activity of phenytoin with little toxicity in the rotorod test. In conclusion, N,N-phthaloyl-glycine amides might represent promising antiepileptic drugs.
- Usifoh, Cyril O.,Lambert, Didier M.,Wouters, Johan,Scriba, Gerhard K.E.
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p. 323 - 331
(2007/10/03)
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- Ultrasound and ZnCl2 promoted synthesis of phthaloyl derivatives of α-amino carboxamides
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A new, one-step and racemization-free synthesis of phthaloyl derivatives of α-amino carboxamides is described. Under ultrasound, α-amino carboxamides and dipeptide derivatives react with monomethyl phthalate in the presence of BOP, ZnCl2 and i-
- Casimir,Guichard,Briand
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- Efficient synthesis of primary amides using 2-mercaptopyridone-1-oxide-based uronium salts
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S-(1-Oxido-2-pyridinyl)-1,1,3,3-tetramethylthiouronium tetrafluoroborate (TOTT) and hexafluorophosphate (HOTT) are cheap and convenient reagents for the rapid and high-yielding preparation of primary amides when reacted with carboxylic acids and ammonium chloride in the presence of diisopropylethylamine. The reaction is chemoselective and undesired ammonolysis of other sensitive functional groups is not observed. (C) 2000 Elsevier Science Ltd.
- Bailen,Chinchilla,Dodsworth,Najera
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p. 9809 - 9813
(2007/10/03)
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- A selective method for the preparation of primary amides: Synthesis of Fmoc-L-4 carboxamidophenylalanine and other compounds
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A new method for the synthesis of primary amides was developed in which carboxylic acids were treated with ammonium chloride in the presence of peptide synthesis coupling agents and base at room temperature. These mild conditions allow the conversion of carboxyl groups to primary amides on substrates possessing sensitive functional groups such as esters and the base-labile Fmoc protecting group.
- Wang, Wei,McMurray, John S.
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p. 2501 - 2504
(2007/10/03)
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- Scope of phthalimido chemistry I. Extension of utility by conversion to the opcb protecting group
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The scope of the phthalimido protecting group (PhthN-) is extended by reaction with pyrrolidine. The resulting o-pyrrolidinocarbonylbenzamide ("OPCB-") represents a base/nucleophile stable derivative of the parent, which reverts to the imide form upon treatment with acid. This methodology allows utilization of this protecting group (as the OPCB form in synthetic sequences requiring basic/nucleophilic reaction conditions.
- Astleford, Bret,Weigel, Leland O.
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p. 3301 - 3304
(2007/10/02)
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- 4-Hydroxy-1(2H)-isoquinolone-3-carboxamides. Synthesis and Properties
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Reaction of some α-phthalimidoacetamides 1a-i with sodium ethoxide was carried out under drastic conditions.Compounds 1b-g afforded 4-hydroxy-1(2H)-isoquinolone-3-carboxamides 2b-g, while 1h-i afforded the acids 3a-b together with the expected isoquinolon
- Schapira, Celia B.,Abasolo, Maria I.,Perillo, Isabel A.
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p. 577 - 581
(2007/10/02)
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