Document Detail


Renin inhibitors containing nicotinic or isonicotinic acid at the N-terminus. Part V.
MedLine Citation:
PMID:  8562014     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Four new compounds: Nic-Phe/4-OMe/-MePhe-Sta-epsilonAhx-OMe/23/,Nic-Phe/4-OMe/-MePhe- Sta-epsilonAhx-Iaa/24/,iNic-Phe/4-OMe/-MeLeu-Sta-ep silonAhx-OMe/29/ and iNic-Phe/4-OMe/-MeLeu-Sta-epsilonAhx-Iaa/30/ have been synthesized in search after renin inhibitors of improved biological properties. Their stability against chymotrypsin activity, solubility in water at pH 7.4, 6.9 and 2.0, partition coefficient and activity in vitro were determined. All synthesized inhibitors are resistant to enzymatic degradation, all are very good soluble in water at pH 2.0, poorly soluble at pH 6.9 and insoluble at pH 7.4. Partition coefficients go up together with increase of pH worth of buffer. IC50 of obtained inhibitors 23,24,29 and 30 is 3 x 10(-4),7.5 x 10(-4),4 x 10(5) and 4 x 10(-3)M/1 respectively.
Authors:
R Paruszewski; P Jaworski; J Tautt; J Dudkiewicz
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Bollettino chimico farmaceutico     Volume:  134     ISSN:  0006-6648     ISO Abbreviation:  Boll Chim Farm     Publication Date:  1995 Nov 
Date Detail:
Created Date:  1996-03-01     Completed Date:  1996-03-01     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  0372534     Medline TA:  Boll Chim Farm     Country:  ITALY    
Other Details:
Languages:  eng     Pagination:  551-6     Citation Subset:  IM    
Affiliation:
Department of Pharmaceutical Chemistry, Medical University, Warszawa, Poland.
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MeSH Terms
Descriptor/Qualifier:
Amino Acid Sequence
Chemistry, Physical
Enzyme Inhibitors / chemical synthesis,  chemistry,  pharmacology*
Isonicotinic Acids / chemical synthesis,  chemistry,  pharmacology*
Molecular Sequence Data
Nicotinic Acids / chemical synthesis,  chemistry,  pharmacology*
Peptides / chemical synthesis,  chemistry,  pharmacology
Physicochemical Phenomena
Renin / antagonists & inhibitors*
Solubility
Chemical
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Isonicotinic Acids; 0/Nicotinic Acids; 0/Peptides; EC 3.4.23.15/Renin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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