A series of piperazinyl-β-carboline-3-carboxamide derivatives were designed through a molecular hybridization approach. Designed analogues were synthesized, characterized and evaluated for anti-leishmanial activity against Leishmania infantum and Leishmania donovani. In L. infantum inhibition a...

A library of approximately 40 N1-acylated (aza)indole alkanoic esters and acids was prepared employing a microwave-assisted approach. The optimized synthetic route allows for parallel synthesis, variation of the indole substitution pattern, and high overall yield. Additionally, the procedure has...

A series of novel, heteroaryl carboxylic acid conjugates of the sesquiterpene melampomagnolide-B (MMB, 3) has been evaluated as antitumor agents against an NCI panel of 64 human hematopoetic and solid tumor cell lines. The indole-3-acrylic acid conjugate 7j and the indole-3-carboxylic acid conju...

The reaction of [18F]fluoromethyl tosylate with methyl(tert-butoxycarbonyl)-l-tryptophanate results in formation the O-alkylated ester of the tryptophan instead of alkylation of the indole nitrogen of tryptophan as initially anticipated. Treatment of protected tryptophan with NaH in dimethyl for...

Ethyl pyruvate was hydrogenated as a gas-phase reactant over 2.5% Pt/SiO2 premodified with hydroquinidine 4-chlorobenzoate at two concentrations (0.85 and 8.5 mM g−1cat). The sense of enantioselectivity changed as a function of the modifier concentration. At low modifier concentrations, the (S)-...

Fenoxaprop-P-ethyl (FE) is widely used as a post-emergence aryloxyphenoxy propionate (AOPP) herbicide in agriculture. An efficient FE-degrading strain DL-2 was isolated from the enrichment culture and identified as Acinetobacter sp. and the metabolite fenoxaprop acid (FA) was identified by HPLC/...

Herbicide resistance or tolerance in weeds mediated by cytochrome P450 monooxygenase is a considerable problem. However, cytochrome P450 mediated resistance or tolerance in weeds was less studied. Thus, in this work, the role of the cytochrome P450 monooxygenase in the different responses of Poa...

American sloughgrass is a widespread and competitive annual grass weed of wheat in Yangtze River delta of China. Whole-plant dose–response experiments were conducted with fenoxaprop-p-ethyl to confirm and characterize resistant and susceptible American sloughgrass populations. The resistant Ame...

Using adjuvants to optimize and increase the efficacy of herbicides is an acceptable manner to reduce herbicides undesirable impact on the environment. Therefore, to detect suitable adjuvants for sethoxydim or fenoxaprop-p-ethyl, two dose–response experiments were conducted separately. The trea...

Resistance to the acetyl-coenzyme A carboxylase (ACCase)- and acetolactate synthase (ALS)- inhibiting herbicides in shortawn foxtail (Alopecurus aequalis) has been reported in wheat fields of eastern China. To better understand the distribution of the resistant populations and the occurrence of ...

In this study, we evaluated effects of fenoxaprop-p-ethyl herbicide on wheat (Triticum aestivum L.). The wheat plants were grown in pots containing perlite. Fenoxaprop-p-ethyl was applied to adequately grown T. aestivum plants at determined doses (1 mM, 1.5 mM, 2.2 mM, 3.4 mM and 5.1 mM) via spr...

Chemical fixation of carbon dioxide under mild reaction conditions e.g. atmospheric pressure and low temperature depends upon the ability of catalyst. Herein, a synergistic catalytic scheme of silver sulfadiazine/nBu4NBr was described for the three-component reaction of propargylic alcohols, CO2...

In this study, the electrochromic property of vinyl benzyl viologen (VBV) was first investigated and incorporated in an electrochromic device (ECD). The polymerizable vinyl moiety of VBV enables a self-immobilization through UV-curing under potential bias. Immobilized VBV (I-VBV) was obtained on...

Lead halide perovskites, used to produce photovoltaic devices, have been the subject of a huge research effort these last years. This is due to the spectacular improvement of the conversion efficiency results within a short amount of time. However, some issues have been identified, which include...

N,N-bis((1H-pyrazol-1-yl)methyl)(cyclohexyl)methanamine (LA), N,N-bis((1H-pyrazol-1-yl)methyl)-2,6-diethylbenzenamine (LB), N,N-bis((1H-pyrazol-1-yl)methyl)-4-bromobenzenamine (LC), N,N-bis((1H-pyrazol-1-yl)methyl)cyclohexanamine (LD), N,N-bis((1H-pyrazol-1-yl)methyl)(furan-2-yl)methanamine (LE)...

The novel complexes [LnCoCl2] (Ln = LA − LH), containing the N,N-chelating ligands N,N-bis((1H-pyrazol-1-yl)methyl)aniline (LA), N,N-bis((3,5-dimethyl-1H-pyrazol-1-yl)-3,5-dimethylaniline (LB), N,N-bis((1H-pyrazol-1-yl)methyl)-3,5-dimethylaniline (LC), N,N-bis((3,5-dimethyl-1H-pyrazol-1-yl)methy...

JMV 236, a new cholecystokinin-octapeptide-sulfate (CCK 8 S) derivative (Boc-Tyr (SO3)-Nle-Gly-Trp-Nle-Asp-Phe-NH2) has been synthesized in the Centre de Pharmacologie-Endocrinologie (Montpellier). This peptide has been shown to present the same activity as CCK 8 S on pancreatic amylase secretio...

The behavioural effects of two cholecystokinin analogues Boc-Tyr(SO3H)-Nle-Gly-Trp-Nle-Asp-Phe-NH2 (JMV 236), a potent CCK agonist, and Boc-Tyr(SO3H)-Nle-Gly-DTrp-Nle-Asp-2-Phenylethylester (JMV 179), a CCK antagonist were studied. JMV 236 (3.125, 12.5 and 50 μg/kg i.p.) dose-dependently decrea...

A series of eight biologically active N, N′-disubstituted thiocarbamide compounds (1–8) have been prepared from thiophene-2-carbonyl isothiocyanate and various substituted aromatic primary amines (2,4-dichlorophenyl aniline, 4-chloro-3-nitrophenyl aniline, 4-methoxycarbonylphenyl aniline, 3-me...

We examined the in vivo mutagenicity of 2-[2-(acetylamino)-4-[bis(2-hydroxyethyl)amino]-5-methoxyphenyl]-5-amino-7-bromo-4-chloro-2H-benzotriazole (PBTA-6) and benzo[a]pyrene (BaP) by using transgenic (Tg) zebrafish carrying the mutational target gene rpsL. PBTA-6 is one of the PBTA-type compoun...