Showing papers in "Bioorganic & Medicinal Chemistry Letters in 1991"

TL;DR: Analogs of MTT, 3-(4,5-dimethylthiazolyl)-2,5diphenyltetrazolium bromide, designed to yield water-soluble formazans upon reduction, have been synthesized and evaluated as cell-viability indicators as mentioned in this paper.

TL;DR: The enantiomers of natural dideoxynucleoside analogues with known potent HIV activity were prepared as potential anti-HIV agents and showed promise in terms of antiviral activity and specificity.

TL;DR: In this article, a pyrazole ring can effectively mimic the combined effect of N3-substituent (R 3 ) and C2-hetero atom (X) of monocyclic dihydropyrimidines.

TL;DR: Simple dipeptides incorporating phosphonamidate and phosph onamidate ester isosteres for the scissile peptide bond are modest inhibitors of the HIV-1 protease.

TL;DR: A series of pyridine-containing stilbene and amide derivatives based on the structure of piceatamol, a naturally occurring protein-tyrosine kinase inhibitor, has been prepared and tested for inhibition of p56lck as discussed by the authors.

TL;DR: Conversion of prodrug to drug is mediated by an immunoconjugate consisting of a β-lactamase enzyme covalently attached to a monoclonal antibody Fab′ fragment which is pre-localized at the tumor.

TL;DR: In this article, the synthesis and preliminary evaluation of (+)-CBI-indole2 (3) are detailed in efforts that further demonstrate a direct relationship between the chemical stability of the agents and their biological potency/DNA alkylation intensity.

TL;DR: A recombinant human Lewis α(1,3/1,4)fucosyltranferase has been studied for its acceptor substrate specificity and used in the synthesis of sialyl Lex and derivatives.

TL;DR: One of these benzofurans, the bromobenzofuran 11b, is a potent and specific antagonist of angiotensin II which, after oral administration, causes marked and long-lasting falls in blood pressure in renal hypertensive rats.

TL;DR: In this paper, a new heparin-like pentasaccharide fragment was synthesized in which the reducing end glucosamine unit was replaced by a glucose residue.

TL;DR: Facile stereocontrolled syntheses of the potent HIV-a protease inhibitors 1 and 2 are described, employing a unified synthetic route from carbohydrate precursors.

TL;DR: The synthesis of two series of constrained mimetics of the dipeptide phenylalanylglycine oriented in the “anti” conformation (X1 = 180°) are described, which differ about the geometry of the internal amide bond (ω1=0° or 180°).

TL;DR: The 12-(3'hydroxy-n-propyl)-deoxoartmisinin was synthesized from artemisinic acid via photooxidative cyclization as a key step.

TL;DR: A simple semicarbazide derivative of CBI, an analog of the authentic CPI alkylation subunit of CC-1065, exhibits enhanced in vitro cytotoxic potency and DNA alinesslation properties ( ca. 100x) derived from noncovalent electrostatic DNA binding as mentioned in this paper.

TL;DR: Both enantiomers of unnatural 4,4-difluorinated threonine were readily prepared via enzymatic optical resolution and only the corresponding (2 S, 3 S ) isomer was found to possess comparable or even stronger in vitro antitumor activity than the currently used 5-fluorouracil (5-FU).

TL;DR: A chiral synthesis of the antifungal agent Sch 42427 starting from S-chloropropionic acid was described in this paper, where the synthesis was carried out in a chiral manner.

TL;DR: Analogs of monocyclic ET-1 (Ala3,11, Nl7) containing substitutions were prepared and assayed for vasoconstrictor and receptor binding activity.

TL;DR: Difluoromethylenebisphosphonic acid was prepared by acetyl hypofluorite-mediated fluorination of tetraisopropyl methylene bisphosphonate and ester hydrolysis as discussed by the authors.

TL;DR: In this paper, an efficient synthesis of the C 11 -C 16 subunit of ionomycin from cis -3,5-dimethyl cyclohexanone using as the enzymatic Baeyer-Villiger oxidation to establish the correct absolute stereochemistry at C 12 and C 14 is reported.

TL;DR: In this paper, the first glimpse of phosphorus-containing metabolites generated during cleavage of organophosphonate carbon to phosphorus (CP) bonds was provided by Escherichia coli.

TL;DR: F fluorinated analogs of several of the intermediates of the methionine salvage pathway were synthesized and tested as inhibitors of the malarial parasite Plasmodium falciparum, showing good activity against this chloroquine resistant strain.

TL;DR: A new synthesis of optically active 2-phenyl benzothiazepin-4-(5H)-one i.e. Thiazesim has been described in this paper.

TL;DR: A phosphorylated disaccharide from the inner core region of Neisseria meningitidis immunotype lipopolysaccharide 6 could be conjugated via an artificial spacer to an elongated peptide sequence of a meningococcal outer membrane protein.

TL;DR: The binding of aryl boronic acids to α-chymotrypsin and subtilisin has been studied by 11B NMR spectroscopy; evidence is provided for the direct spectroscopic observation of a tetrahedral enzyme/boromate complex as discussed by the authors.

TL;DR: In this paper, a method for the preparation of highly pure optically active (R)- and (S)-3-chloro-1,2-propanediol (99.5% ee and 99.4%) was established based on stereospecific dehalogenation and assimilation with bacteria.

TL;DR: A pentasaccharide containing a N-acetyl-glucosamine unit and corresponding to the major natural sequence required in heparin for binding to antithrombin III is reported for the first time.

TL;DR: In this paper, the synthesis of the antihypertensive potassium channel activator WAY-120,491 (1) is described, and a large scale classical resolution of racemic 9 was facilitated using authentic seed crystals, whose preparation was accomplished via a novel coupling of raceemic azidoalcohol 17 with the putative acyltriflate 20.

TL;DR: In this article, the conformationally restricted β-ketophosphonic acid, 3(S )-phosphonoacetyl-2( R )-piperidinecarboxylic acid (4 ) is described.

TL;DR: Modification of simple monocyclic β-lactams has led to development of substituted 4-azetidinones that both inhibit HLE in a time dependent manner and prevent HLE-induced lung damage in hamsters.

TL;DR: The esterification of 2-(4-chlorophenoxy) propionic acid and n-butanol by the lipase from Candida cylindracea in different reaction media showed reverse enantioselectivity.