22916-26-3Relevant articles and documents
PENICILLAMINE AND ITS DERIVATIVES ARE USED IN THE TREATMENT OF COPPER TOXICITY AND NASH
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Paragraph 00061-00064, (2017/08/01)
Penicillamine and its derivatives, composition, methods of synthesizing and using the compound of formula 1 are disclosed. The compounds of formula 1 also comprises of salts, polymorphs, solvates and hydrates thereof. The compounds may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated as per oral, topical, transmucosal, inhalation, targeted delivery and sustained release formulations. Such compositions can be used for the treatment of hepatic and genetic disorders related to copper toxicity, NASH and Leigh Syndrome.
α-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases
Orrling, Kristina M.,Marzahn, Melissa R.,Gutierrez-de-Teran, Hugo,Aqvist, Johan,Dunn, Ben M.,Larhed, Mats
experimental part, p. 5933 - 5949 (2009/12/24)
The impact of moving the P1 side-chain from the β-position to the α-position in norstatine-containing plasmepsin inhibitors was investigated, generating two new classes of tertiary alcohol-comprising α-benzylnorstatines and α-phenylnorstatines. Twelve α-s
A concise synthesis of (2S,3S)-BocAHPBA and (R)-BocDMTA, chiral building blocks for peptide-mimetic HIV protease inhibitors
Ikunaka, Masaya,Matsumoto, Jun,Nishimoto, Yukifumi
, p. 1201 - 1208 (2007/10/03)
Scalable syntheses of (2S,3S)-3-N-tert-butoxycarbonylamino-2-hydroxy-4-phenylbutanoic acid (BocAHPBA) 1 and (R)-3-tert-butoxycarbonyl-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid (BocDMTA) 2 have been developed. Both 1 and 2 can serve as chiral building blocks in assembling JE-2147 (KNI-764) 3, a potent HIV protease inhibitor. The synthesis of (2S,3S)-BocAHPBA 1 is achieved in 41% overall yield from (S)-2-N,N-dibenzylamino-3-phenylpropanal 4 in five steps where Tamao's reagent [Me2(i-PrO)SiCH2MgCl] is employed for a one-carbon homologation, and Zhao's oxidation protocol (TEMPO, NaClO2, NaClO) is applied to convert a 1,2-glycol moiety into an α-hydroxy acid motif. (R)-BocDMTA 2 is synthesized with 99.4% ee in 24% yield via enantioselective hydrolysis of methyl (±)-5,5-dimethyl-1,3-thiazolidine-4-carboxylate 8b by a Klebsiella oxytoca hydrolase; the unreacted (S)-ester 8b can be recovered and racemized with NaOMe to afford (±)-8b in 46% yield for another round of the enzymatic processing.
Highly Potent and Selective Heptapeptide Antagonists of the Neurokinin NK-2 Receptor
McElroy, Andrew B.,Clegg, Stephen P.,Deal, Martyn J.,Ewan, Georg B.,Hagan, Russell M.,et al.
, p. 2582 - 2591 (2007/10/02)
Incorporation of D-Pro9 into substance P related peptides is known to enhance neurokinin NK-2 receptor agonist potency and selectivity with respect to other neurokinin receptors.We now report that replacement of D-Trp9 by D-Pro9
Amino-acid zwitterion equilibria: vibrational and nuclear magnetic resonance studies of methyl-substituted thiazolidine-4-carboxylic acids
Howard-Lock, H. E.,Lock, C. J. L.,Martins, M. L.,Smalley, P. S.,Bell, R. A.
, p. 1215 - 1219 (2007/10/02)
Infrared and Raman spectra (4000-100 cm-1) of solid samples of six different methyl substituted thiazolidine products of D-penicillamine and L-cysteine hydrochloride have been observed and assigned, Infrared spectra in D2O solutions have been obtained for comparison in order to study the amino-acid zwitterion equilibria.Proton and 13C nmr spectra for the compounds have also been measured.
2-Substituted thiazolidine-4(R)-carboxylic acids as prodrugs of L-cysteine. Protection of mice against acetaminophen hepatotoxicity
Nagasawa,Goon,Muldoon,Zera
, p. 591 - 596 (2007/10/02)
A number of 2-alkyl- and 2-aryl-substituted thiazolidine-4(R)-carboxylic acids were evaluated for their protective effect against hepatotoxic deaths produced in mice by LD90 doses of acetaminophen. 2(RS)-Methyl-(1b),2(RS)-n-propyl-, and 2(RS)-n
