Abstract:
:A new series of N'-(pyridinioacetyl)alkanoic and -benzoic acid hydrazides, as chloride salts, and some cyclic analogues produced ring closure have been synthesize and tested in a search for more effective germicides. Physicochemical parameters, such as surface tension, critical micelle concentration, and thermodynamic activity. (Ferguson values), were also determined. Staphylococcus aureus and Streptococcus pyogenes were the most susceptible of the organisms tested. N'-(Pyridinoacetyl)hexadecanoic acid hydrazide exhibited the highest toxicity to Staph. aureus and fungi. The mean surface tension of the equitoxic solutions is 59.8 +/- 0.3 dyn/cm for bacteria and 51.65 +/- 0.1 dyn/cm for fungi. N'-(Pyridinoacetyl)octadecanoic acid hydrazide and N'-(pyridinoacetyl)-9-ocadecenoic acid hydrazide exhibit the highest toxicity to S. pyogenes (1.1 x 10(-6) M). The surface tension of their equitoxic solutions and their Ferguson values indicate that these compounds may act through a different mechanism.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Sicardi SM,Vega CM,Cimijotti EBdoi
10.1021/jm00184a016subject
Has Abstractpub_date
1980-10-01 00:00:00pages
1139-42issue
10eissn
0022-2623issn
1520-4804journal_volume
23pub_type
杂志文章abstract::Recruitment of suppressive CD4+ FOXP3+ regulatory T cells (Treg) to the tumor microenvironment (TME) has the potential to weaken the antitumor response in patients receiving treatment with immuno-oncology (IO) agents. Human Treg express CCR4 and can be recruited to the TME through the CC chemokine ligands CCL17 and CC...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/acs.jmedchem.9b00506
更新日期:2019-07-11 00:00:00
abstract::A series of 4- aminobenzamides of some simple primary and secondary amines were prepared and evaluated for anticonvulsant effects. The compounds were tested in mice against seizures induced by electroshock and pentylenetetrazole ( metrazole ) and in the rotorod assay for neurologic deficit. For those N-alkyl amides te...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00372a013
更新日期:1984-06-01 00:00:00
abstract::The title compounds were prepared to investigate their potential as thromboxane synthetase inhibitors as well as antihypertensive agents. Imidazoles VIII and triazoles X were prepared to examine the effects of aromatic substitution, chain length, and heterocycle substitution upon biological activity. Imidazoles VIII a...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00154a017
更新日期:1986-04-01 00:00:00
abstract::Significant efforts have been reported on the development of influenza antivirals including inhibitors of the RNA-dependent RNA polymerase PA N-terminal (PAN) endonuclease. Based on recently identified, highly active metal-binding pharmacophores (MBPs) for PAN endonuclease inhibition, a fragment-based drug development...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/acs.jmedchem.9b00747
更新日期:2019-11-14 00:00:00
abstract::A close analogue of the antileukemic agent 5,8-dideaza-N10 propargylfolic acid (2) was synthesized by replacing the propargyl moiety of 2 with a cyanomethyl group. This compound, N10-(cyanomethyl)-5,8-dideazafolic acid (3), was evaluated for its antifolate and antitumor activities in several biological test systems. A...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00358a030
更新日期:1983-04-01 00:00:00
abstract::New ruthenium(II) and iron(II) organometallic compounds of general formula [(η(5)-C5H5)M(PP)Lc][PF6], bearing carbohydrate derivative ligands (Lc), were prepared and fully characterized and the crystal structures of five of those compounds were determined by X-ray diffraction studies. Cell viability of colon cancer HC...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/acs.jmedchem.5b00403
更新日期:2015-05-28 00:00:00
abstract::We report herein the identification of the rhodium(III) complex [Rh(phq)2(MOPIP)]+ (1) as a potent and selective ATP-competitive neural precursor cell expressed, developmentally down-regulated 8 (NEDD8)-activating enzyme (NAE) inhibitor. Structure-activity relationship analysis indicated that the overall organometalli...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/acs.jmedchem.6b00250
更新日期:2017-01-12 00:00:00
abstract::Various lines of evidence, including molecular modeling studies, imply that the endoethylenic bridge of 3,8-diazabicyclo[3.2. 1]octanes (DBO, 1) plays an essential role in modulating affinity toward mu opioid receptors. This hypothesis, together with the remarkable analgesic properties observed for N(3) propionyl, N(8...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm991140q
更新日期:2000-06-01 00:00:00
abstract::Gamma9delta2T cells represent the most abundant population of human blood gammadeltaT lymphocytes. They produce and promote strong cytotoxic activity against many pathogens that are implicated in several human infectious diseases. Their activation requires their exposure to small phosphorus-containing antigens in the ...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm049861z
更新日期:2004-08-26 00:00:00
abstract::Novel bisbenzimidazole inhibitors of bacterial type IA topoisomerase are of interest for the development of new antibacterial agents that are impacted by target-mediated cross resistance with fluoroquinolones. The present study demonstrates the successful synthesis and evaluation of bisbenzimidazole analogues as Esche...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm5003028
更新日期:2014-06-26 00:00:00
abstract::Selective inhibitors of protein tyrosine phosphatases (PTPs) and dual-specificity phosphatases (DSPs) are expected to be useful tools for clarifying the biological functions of the PTPs themselves and also to be candidates for novel therapeutics. We planned a library approach for the identification of PTP/DSP inhibito...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm0100741
更新日期:2001-09-27 00:00:00
abstract::Inhibitors of checkpoint kinase 1 (CHK1) are of current interest as potential antitumor agents, but the most advanced inhibitor series reported to date are not orally bioavailable. A novel series of potent and orally bioavailable 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitrile CHK1 inhibitors was generated ...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm3012933
更新日期:2012-11-26 00:00:00
abstract::In this article we introduce a molecular docking algorithm called MolDock. MolDock is based on a new heuristic search algorithm that combines differential evolution with a cavity prediction algorithm. The docking scoring function of MolDock is an extension of the piecewise linear potential (PLP) including new hydrogen...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm051197e
更新日期:2006-06-01 00:00:00
abstract::A facile procedure is described for the conversion of morphine, via the diphosphate ester derivative 1 followed by catalytic reduction and treatment with Li/NH3, to 3-deoxy-7,8-dihydromorphine (3). Oxidation with benzophenone tert-butoxide converted 3 to the ketone 4, which on treatment with Zn/NH4Cl formed (-)-4-hydr...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00144a013
更新日期:1981-12-01 00:00:00
abstract::Analogues of 9-(2-fluorobenzyl)-6-(methylamino)-9H-purine (1) containing isosteric replacements of the imidazole ring atoms were synthesized and tested for anticonvulsant activity. The pyrrolo[2,3-d]-, pyrazolo[3,4-d]-, and triazolo[4,5-d]pyrimidines were less active than 1 against maximal electroshock-induced seizure...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00019a019
更新日期:1995-09-15 00:00:00
abstract::The pharmaceutical industry has recognized that many drug-like molecules can self-aggregate in aqueous media and have physicochemical properties that skew experimental results and decisions. Herein, we introduce the use of a simple NMR strategy for detecting the formation of aggregates using dilution experiments that ...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm400535b
更新日期:2013-06-27 00:00:00
abstract::Two series of indenoisoquinoline topoisomerase I inhibitors have been prepared to investigate optimal substituents on the indenone ring at the 9-position. The more exhaustive series was prepared using a nitrated isoquinoline ring that has been previously demonstrated to enhance biological activity. After preliminary b...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm070307+
更新日期:2007-09-06 00:00:00
abstract::A series of 3-thioindolamidines (and 3-indolamidines) related to mixidine (1) was studied for cardiac-slowing properties, following the discovery of activity for prototype thioindole 2. Structure-activity relationships were explored, leading to many potent antitachycardiac agents (6-9, 12, 13, 15-17, 20, 23, 24, 30, 3...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00356a021
更新日期:1983-02-01 00:00:00
abstract::In our search for potent and receptor-selective agonists and antagonists, we report here the results of D-amino acid substitution at each position of the short peptide gamma-melanocyte-stimulating hormone (gamma-MSH). The native gamma-MSH shows weak binding at all three receptors (i.e., the human MC3, MC4, and MC5) an...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm000211e
更新日期:2000-12-28 00:00:00
abstract::To enhance the ability of indirubin derivatives to inhibit CDK2/cyclin E, a target of anticancer agents, we designed and synthesized a new series of indirubin-3'-oxime derivatives with combined substitutions at the 5 and 5' positions. A molecular docking study predicted the binding of derivatives with OH or halogen su...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm100080z
更新日期:2010-05-13 00:00:00
abstract::The preparation of a series of indole N-acyl and N-carbamic esters of (+/-)-alpha-5-[1-(indol-3-yl)ethyl]-2-methylamino-delta2-thiazolin-4-one (1) is reported. These derivatives were synthesized as potential water-soluble precursors of the antiviral thiazolinone 1, for evaluation by intranasal administration against i...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00188a013
更新日期:1979-02-01 00:00:00
abstract::A series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives, substituted at the 7-position with functionalized side chains, was synthesized and evaluated as inhibitors of human blood platelet cAMP phosphodiesterase (PDE) as well as ADP- and collagen-induced platelet aggregation, in vitro. Structural modificati...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00092a019
更新日期:1992-07-10 00:00:00
abstract::Optimization of a new series of small molecule human glucagon receptor (hGluR) antagonists is described. In the process of optimizing glucagon receptor antagonists, we counter-screened against the closely related human gastric inhibitory polypeptide receptor (hGIPR), and through structure activity analysis, we obtaine...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm7015599
更新日期:2008-09-11 00:00:00
abstract::We have reported the preparation and anticancer evaluation of certain 4-anilinofuro[2,3-b]quinolines. However, drawbacks such as lack of selective cytotoxicity, poor oral bioavailability, and poor water solubility exhibited by these compounds prompted us to search for newer derivatives. Among them, (E)-1-(4-(furo[2,3-...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm200046z
更新日期:2011-07-14 00:00:00
abstract::Rebeccamycin analogues containing uncommon sugars and substitutions on the imide nitrogen have been synthesized. Their cytotoxicities were tested in colon cancer and leukemia cells. Their ability to target topoisomerase I was examined using the in vivo complex of the topoisomerase bioassay in Hela cells. Compared with...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm0493764
更新日期:2005-04-07 00:00:00
abstract::A diverse range of chromen-2-one, chromen-4-one and pyrimidoisoquinolin-4-one derivatives was synthesized and evaluated for inhibitory activity against the DNA repair enzyme DNA-dependent protein kinase (DNA-PK), with a view to elucidating structure-activity relationships for potency and kinase selectivity. DNA-PK inh...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm049526a
更新日期:2005-01-27 00:00:00
abstract::The enantiomers of two isosteric phosphonate analogs of the ether-linked antitumor agent 1-O-octadecyl-2-O-methyl-sn-glycero-3-phosphocholine (ET-18-OMe) were synthesized and evaluated for their cytotoxicity against various mouse leukemic cell lines in vitro and in vivo. The key step in the synthesis of the alkyloxy a...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00029a016
更新日期:1994-02-04 00:00:00
abstract::A dihydropyridine-pyridine type redox pro-drug system was developed for delivering quaternary pyridinium salts through biological membranes. As a first application, the dihydropyridine derivative of N-methylpyridinium-2-carbaldoxime chloride (2-PAM) was synthesized using a reduction-addition-elimination sequence. The ...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00223a017
更新日期:1976-01-01 00:00:00
abstract::The preparation and activity against Plasmodium berghei of derivatives of 1-(4-methoxycinnamoyl)-4-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine are described. Replacement of the cinnamoyl group was accomplished by acylation or alkylation of 1-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine. Modifications of the 5-phenyl grou...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00246a009
更新日期:1975-12-01 00:00:00
abstract::A series of 3-fluoromethyl-1,2,3,4-tetrahydroisoquinolines (3-fluoromethyl-THIQs) was proposed, and their phenylethanolamine N-methyltransferase (PNMT) and alpha(2)-adrenoceptor affinities were predicted through the use of comparative molecular field analysis (CoMFA) models. These compounds were synthesized and evalua...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm990045e
更新日期:1999-09-09 00:00:00