Showing papers in "Bioorganic & Medicinal Chemistry in 1993"

TL;DR: Curcumin, a relatively non-toxic natural product isolated from Curcuma longa, is a modest inhibitor of the HIV-1 and HIV-2 proteases but complexes of the central dihydroxy groups of curcumin with boron lower the IC50 to a value as low as 6 microM.

TL;DR: Molecular modelling of these structures indicates that their spatial and electronic structures may make an important contribution to the biological activity.

TL;DR: 2-anthrylboronic acid complexes catechol in water with Kd 330 microM and concomitant 20-fold reduction in fluorescence intensity observe that L-DOPA and dopamine behave similarly, suggesting a mechanism for the development of real-time sensing schemes.

TL;DR: The result showed that the specificity and consequently applicability of the single primer mediated PCR for amplifying a particular DNA fragment beyond known sequence region was remarkably improved by the successive 2nd reaction.

TL;DR: This work will discuss the studies delineating the ligand binding of these enzymes and present a possible secondary structure of Fe2+ oxidase enzymes.

TL;DR: (2S,3S)-(-)-Lasiol (2,3,6-trimethyl-5-hepten-1-ol, 1) and its antipode were synthesized from cis-4,5-dimethylcyclohexene oxide by employing asymmetric cleavage of the epoxy ring with a chiral lithium amide derived from 4.

TL;DR: These compounds represent an important new class of synthetic uPA inhibitors, with carboxamidine 3 being the most potent selective inhibitor currently described in the literature.

TL;DR: A chromogenic substrate X-Neu5Ac was synthesized to facilitate the screening of bacterial colonies or plaques for the detection of either natural or mutant neuraminidase activity.

TL;DR: The application of the lipase-catalyzed C-terminal deprotection of heptyl esters for the construction of acid- and base-labile O -glycopeptides carrying the characteristic structural element of the tumor associated T N -antigen (GalNAc α→Ser/Thr) is described.

TL;DR: Several iron complexes catalytically activate O2 to oxygenate hydrocarbons and their electrochemical characterization during steady-state turnover confirm that the first-formed intermediate is a one-to-one R'OOH/FeIILx adduct.

TL;DR: Results on metabolism assays with this compound showed the generation of phenol 12 (i.e. the putative active antioxidant species); on the other hand, no metabolite resulting from dealkylation at C7 was detected, thus confirming the resistance conferred by the CF3CH2O group to the cytochrome P-450 promoted cleavage.

TL;DR: Two molecules 9 and 14, representatives of two series of electrophilic lactone derivatives, have been synthesized, and labeled with carbon 13 at their reactive sites, and the validity of the Relative Alkylation Index (RAI) as a predicative model in contact allergy is discussed.

TL;DR: K252c-related compounds were synthesized with different framework flexibilities and different functions (imide, amide and amide-alcohol) on the non-indolic heterocycle and the inhibitory activities towards protein kinase C and protein kinases A are compared.

TL;DR: Nuclear magnetic resonance data indicate that oligosaccharides 4 and 5 partially mimic the conformation of the O-specific polysaccharide of S. dys.

TL;DR: The DNA alkylation properties and in vitro cytotoxic activity of a series of analogs of CC-1065 and the duocarmycins incorporating the 9a-chloromethyl-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (C2BI) alkylated subunit are detailed.

TL;DR: Two partially constrained L-glutamate analogs known to be agonists at the metabotropic glutamate receptors (mGluRs) adenylyl cyclase coupled have been submitted to conformational analysis and the data obtained utilized to define a pharmacophore which takes into account the location of hydrogen bonding donating sites of the receptor.

TL;DR: In this paper, the design, synthesis and in vitro inhibitory activity toward human leukocyte elastase of a series of dual action saccharin derivatives are described, and the design and synthesis of such derivatives are discussed.

TL;DR: The mechanism of halide elimination from 2-haloethyl-5,8-dihydroxyquinazolin-4(3H)-ones was studied in aqueous buffer by means of a pH-rate profile, buffer dilution studies, isotopic labeling, and kinetic isotope effects, and it is apparent that a quinazolinone tautomer is formed in the rate determining step of elimination.

TL;DR: A series of 2-aryl-2,5-dihydropyridazino[4,3-b]indol-3(3H)-ones were prepared and evaluated for their ability to inhibit radioligand binding to BZR, and to prevent sound and pentylenetetrazole induced seizures in mice.

TL;DR: The conformationally restricted AdoMac analogue has been shown to act as an enzyme activated, irreversible inhibitor of the Escherichia coli form of the enzyme S-adenosylmethionine decarboxylase, and these and related analogues may be useful as conformational probes for the catalytic site of AdoMet-DC.

TL;DR: New and existing methodologies were used to prepare a series of modified CCK analogs in which each amide bond was replaced by a trans-alkene unit, indicating that every amide linkage at C-terminal tetrapeptide (CCK-4) region is crucial for biological activity.

TL;DR: This binding model rationalizes literature findings that desmethoxyverapamil can demonstrate pharmacology typical of both phenylalkylamine and benzothiazepinone (DTZ) calcium channel blockers and proposes a receptor-bound conformation for both 1 and 2.

TL;DR: P alpha-Methyl thymidine triphosphate was prepared through the pyrophosphorolysis of P alpha-methylThymidine diphosphate P beta-diphenyl ester and tested as an alternative substrate for E. coli DNA polymerase 1 (Klenow fragment).

TL;DR: P pH-dependencies of the kinetic parameters for inhibition are complex but reflect greater inhibitory potency at lower pH and suggest a mechanism for inhibition that involves the same active site groups as are involved in catalysis, which proposes that kon is rate-limited by general-acid catalyzed ligand exchange of inhibitor for the zinc-bound water molecule.

TL;DR: Three soft drug analogs and a metabolite of methatropine based on phenylsuccinic structural moiety were synthesized and tested for activity and all the soft drugs tested elicited shorter durations of mydriatic action in rabbit eyes compared to atropine.

TL;DR: The soft drugs reported in this study will likely be able to elicit a local action at the site of application but will probably be metabolized rapidly in the systemic circulation, thereby avoiding the systemic side effects with a consequent increase in the therapeutic index.

TL;DR: In this paper, N -tosyloxy-β-lactams, such as N -toyloxy4-phenyl-2-azetidinone (2b) and N-toyloxide-3-(S)-phthalimido-4-(S )-2 -azetidine (2c), are described.

TL;DR: The results conclusively proved the applicability of the new steroidal proxyl nitroxide (SPN) as a potential spin probe for spin labeling studies.

TL;DR: Several lipophilic-2',3'-dideoxynucleotide analogues have been synthesized and tested against Human Immunodeficiency Virus (HIV) and can be considered as Lipophilic nucleotide mimics.

TL;DR: This paper describes the use of the non-peptidal N-(2-adamantyloxycarbonyl)-alpha-methyl tryptophan phenylethylamide template of the "peptoid" CCK B antagonist compounds 1 as a basis to probe the functional group requirements of theCCK B receptor in order to produce an agonist response.