Synthesis and antitrypanosomal evaluation of some thiazole-containing amino acids and peptides

I. Van Bogaert; A. Haemers; W. Bollaert; N. Van Meirvenne; R. Brun; K. Smith; AH Fairlamb

doi:10.1016/0223-5234(93)90125-X

Synthesis and antitrypanosomal evaluation of some thiazole-containing amino acids and peptides

I. Van Bogaert
, A. Haemers
, W. Bollaert
, N. Van Meirvenne
, R. Brun
, K. Smith
, AH Fairlamb

Research output: Contribution to journal › Article › peer-review

12 Citations (Scopus)

Abstract

Several amino acids and peptides containing thiazole and thiazolidine residues were prepared. They were tested in vivo and in vitro as possible antitrypanosomal compounds. Some derivatives showed a slight activity. As they are structurally related to glutathione, their inhibitory properties towards glutathionylspermidine synthetase, trypanothione synthetase and trypanothione reductase were determined. No inhibitory activity was found.

Original language	English
Pages (from-to)	387-397
Number of pages	11
Journal	European Journal of Medicinal Chemistry
Volume	28
Issue number	5
DOIs	https://doi.org/10.1016/0223-5234(93)90125-X
Publication status	Published - 1993

Keywords

amino acids
antitrypanosomal activity
di- and tripeptides
thiazole
thiazolidine

ASJC Scopus subject areas

Pharmacology
Drug Discovery
Organic Chemistry

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10.1016/0223-5234(93)90125-X

Cite this

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title = "Synthesis and antitrypanosomal evaluation of some thiazole-containing amino acids and peptides",

abstract = "Several amino acids and peptides containing thiazole and thiazolidine residues were prepared. They were tested in vivo and in vitro as possible antitrypanosomal compounds. Some derivatives showed a slight activity. As they are structurally related to glutathione, their inhibitory properties towards glutathionylspermidine synthetase, trypanothione synthetase and trypanothione reductase were determined. No inhibitory activity was found.",

keywords = "amino acids, antitrypanosomal activity, di- and tripeptides, thiazole, thiazolidine",

author = "\{Van Bogaert\}, I. and A. Haemers and W. Bollaert and \{Van Meirvenne\}, N. and R. Brun and K. Smith and AH Fairlamb",

note = "Funding Information: This research was supported by grants from the Belgian Fund for Scientific Research (AH), the UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Diseases (AH) and the Wellcome Trust (AF and KS). We thank The British Council for supporting the co-operation between the University of Antwerp and the London School of Hygiene and Tropical Medicine.",

year = "1993",

doi = "10.1016/0223-5234(93)90125-X",

language = "English",

volume = "28",

pages = "387--397",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier",

number = "5",

}

TY - JOUR

T1 - Synthesis and antitrypanosomal evaluation of some thiazole-containing amino acids and peptides

AU - Van Bogaert, I.

AU - Haemers, A.

AU - Bollaert, W.

AU - Van Meirvenne, N.

AU - Brun, R.

AU - Smith, K.

AU - Fairlamb, AH

N1 - Funding Information: This research was supported by grants from the Belgian Fund for Scientific Research (AH), the UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Diseases (AH) and the Wellcome Trust (AF and KS). We thank The British Council for supporting the co-operation between the University of Antwerp and the London School of Hygiene and Tropical Medicine.

PY - 1993

Y1 - 1993

N2 - Several amino acids and peptides containing thiazole and thiazolidine residues were prepared. They were tested in vivo and in vitro as possible antitrypanosomal compounds. Some derivatives showed a slight activity. As they are structurally related to glutathione, their inhibitory properties towards glutathionylspermidine synthetase, trypanothione synthetase and trypanothione reductase were determined. No inhibitory activity was found.

AB - Several amino acids and peptides containing thiazole and thiazolidine residues were prepared. They were tested in vivo and in vitro as possible antitrypanosomal compounds. Some derivatives showed a slight activity. As they are structurally related to glutathione, their inhibitory properties towards glutathionylspermidine synthetase, trypanothione synthetase and trypanothione reductase were determined. No inhibitory activity was found.

KW - amino acids

KW - antitrypanosomal activity

KW - di- and tripeptides

KW - thiazole

KW - thiazolidine

UR - https://www.scopus.com/pages/publications/0027195053

U2 - 10.1016/0223-5234(93)90125-X

DO - 10.1016/0223-5234(93)90125-X

M3 - Article

AN - SCOPUS:0027195053

SN - 0223-5234

VL - 28

SP - 387

EP - 397

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 5

ER -

Synthesis and antitrypanosomal evaluation of some thiazole-containing amino acids and peptides

Abstract

Keywords

ASJC Scopus subject areas

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