Organic molecule functionalized lead sulfide hybrid system for energy storage and field dependent polarization performances.

A wet chemical route is reported for synthesising organic molecule stabilized lead sulfide nanoparticles. The dielectric capacitance, energy storage performances and field-driven polarization of the organic-inorganic hybrid system are investigated in the form of a device under varying temperature and frequency conditions. The structural analysis confirmed the formation of the monoclinic phase of lead sulfide within the organic network. The band structure of lead sulfide was obtained by density functional theory calculation that supported the semiconductor nature of the material with a direct band gap of 2.27 eV. The dielectric performance of the lead sulfide originated due to the dipolar and the space charge polarization. The energy storage ability of the material was investigated under DC-bias conditions, and the device exhibited the power density values 30 W/g and 340 W/g at 100 Hz and 10 kHz, respectively. The electric field-induced polarization study exhibited a fatigue-free behaviour of the device for 103 cycles with a stable dielectric strength. The study revealed that the lead sulfide-based system has potential in energy storage applications.

Removal of toxic dye from dye-laden wastewater using a new nanocomposite material: Isotherm, kinetics and adsorption mechanism.

In this study, (hemi)cellulosic biochar-based environment-friendly non-toxic nanocomposite (nAg-AC) was fabricated for an inordinate overlook of toxic dye-laden wastewater depollution. This hybrid nanocomposite grafted with silver nanoparticles, numerous hydroxyl and π-bond containing functional groups exhibited outstanding physicochemical properties. FESEM images indicated the heterogeneous porous structure of nAg-AC, while BET analysis revealed mesoporous property with a significant increment of overall surface area (132%). Imbedding of silver nanoparticles and the presence of multiple hydroxyl groups was evident from the XRD and XPS spectrum. Further, the TGA result indicated excellent thermal stability, and FTIR analysis suggested the involvement of surface functional groups like -OH, =C = O, =NH, =C = C = , and -CH in Rhodamine B (RhB) adsorption. The adsorbent matrix provided the overall mechanical strength and facilitated recycling, while the functional matrix (biochar) provided the adsorptive locus for augmented RhB adsorption efficiency (92.77%). Experiments pertaining to adsorption isotherms and kinetics modeling suggested that RhB was removed through multilayer chemisorption on the heterogeneous nAg-AC surface. The main RhB adsorption mechanism included cumulative efforts of H-bindings, π-π stacking interaction, pore-filling, and electrostatic interactions. The nAg-AC maintained mechanical robustness with significant RhB adsorption even after three consecutive regeneration cycles signifying facile recycling. The nAg-AC displayed an outstanding efficacy for the real industrial wastewater depollution, indicating high effectiveness for practical environmental applications. Finally, the cost analysis (incorporating economic, environmental, and social dimensions) suggested a significant role of the nAg-AC in promoting and establishing sustainable development with the circular economy.

LDL associates with pro-inflammatory monocyte subset differentiation and increases in chemokine receptor profile expression in African Americans.

BACKGROUND: In the United States, African Americans (AAs) have greater risk for Class III obesity and cardiovascular disease (CVD). Previous reports suggest that AAs have a different immune cell profile when compared to Caucasians. METHODS: The immune cell profile of AAs was characterized by flow cytometry using two experimental setups: ex vivo (N = 40) and in vitro (N = 10). For ex vivo experiments, PBMC were treated with participant serum to understand how lipid contents may contribute to monocyte phenotypic differences. For in vitro experiments, monocytes were low-density lipoprotein (LDL)- or vehicle-treated for four hours and subsequently analyzed by flow cytometry and RT-qPCR. RESULTS: When PBMCs were treated with participant sera, subsequent multivariable regression analysis revealed that serum triglycerides and LDL levels were associated with monocyte subset differences. In vitro LDL treatment of monocytes induced a phenotypic switch in monocytes away from classical monocytes accompanied by subset-specific chemokine receptor CCR2 and CCR5 expression changes. These observed changes are partially translation-dependent as determined by co-incubation with cycloheximide. CONCLUSIONS: LDL treatment of monocytes induces a change in monocyte subsets and increases CCR2/CCR5 expression in a subset-specific manner. Understanding the molecular mechanisms could prove to have CVD-related therapeutic benefits, especially in high-risk populations with hyperlipidemia and increased risk for CVD.

Fabrication of biochar-based hybrid Ag nanocomposite from algal biomass waste for toxic dye-laden wastewater treatment.

Dual functional innovative approaches were developed to tackle the algal scum problem in water by utilizing the algal (Spirogyra sp.) biomass waste for organic dye-laden industrial wastewater treatment, a global problem, and challenge. Therefore, an algal biochar-based nanocomposite (nAgBC) was synthesized and employed as a low-cost adsorbent for Congo red (CR) removal. Surface morphology, physicochemical characteristics, elemental composition, phase, and stability of the nanocomposite was analyzed using BET, FESEM-EDX, FTIR, XRD, XPS, and TGA. The nanocomposite was found to be thermostable, mesoporous with large and heterogeneous surface area, containing nAg as doped material, where -OH, NH, CO, CC, SO, and CH are the surface binding active functional groups. Maximum adsorption efficiency of 95.92% (18 mg L-1 CR) was achieved (qe = 34.53 mg g-1) with 0.5 g L-1 of nanocomposite after 60 min, at room temperature (300 K) at pH 6. Isotherm and kinetic model suggested multilayer chemisorption, where adsorption thermodynamics indicated spontaneous reaction. Fluorescens spectral analysis of CR confirmed the formation of CR supramolecule, supporting enhanced adsorption. Furthermore, the result suggested a 5th cycle reusability and considerable efficacy towards real textile industrial effluents. Synergistic effects of the active surface functional groups of the biochar and nAg, along with the overall surface charge of the composite lead to chemisorption, electrostatic attraction, H-bonding, and surface complexation with CR molecules. Thus, synthesized nAgBC can be applicable to mitigate the wastewater for cleaner production and environment.

Biochar-based nanocomposite from waste tea leaf for toxic dye removal: From facile fabrication to functional fitness.

The present study utilized discarded tea leaf waste to produce 'Tea leaf biochar' (TLB) as the functional matrix for the fabrication of hybrid nanocomposite (nAg-TC), with colloidal deposition of silver nanoparticles (nAg) via modified chemical co-precipitation, for treatment of dye-laden wastewater. The chemical composition, physicochemical properties, and morphology of nAg-TC, and active surface functional groups involved in adsorption were identified using BET, FESEM-EDX, FTIR, TGA, XPS, and XRD. The nAg-TC matrix was found to be heterogeneous, mesoporous, thermostable, with rich in active surface functional groups (-OH, =NH, =CH, CC, CO, CN, and CC), and nAg as a dopant material. The dye adsorption results indicated the maximum removal efficiency (RhB = 95.89%, CR = 94.10%) at 300 K for rhodamine B (RhB) and Congo red (CR) concentrations of 25 mg L-1 and 22.5 mg L-1, respectively. The present investigation agreed with Freundlich isotherm (R2CR:0.991; R2RhB:0.993) and pseudo-second order kinetic (R2CR:0.999; R2RhB:0.999) model, indicating overall adsorption of RhB and CR through spontaneous and exothermic chemisorption on the heterogeneous surface of nAg-TC. The mechanism of RhB and CR adsorption was complex where nAg-TC, possessing the synergistic effects of TLB and nAg, showed surface complexation, electrostatic attraction, and H-bonding, leading to chemisorption. Study showed excellent reusability of spent nAg-TC, and commendable treatment efficiency for dye-laden real industrial effluents. The study exhibits substantial techno-economic feasibility of adsorbent and translates the principles of circular economy into synthesis of value-added products through sustainable management of biowaste and bioresource.

A review of the phytochemical mediated synthesis of AgNP (silver nanoparticle): the wonder particle of the past decade.

Silver nanoparticle (AgNP) has been one of the most commonly used nanoparticles since the past decade for a wide range of applications, including environmental, agricultural, and medical fields, due to their unique physicochemical properties and ease of synthesis. Though chemical and physical methods of fabricating AgNPs have been quite popular, they posed various environmental problems. As a result, the bioinspired route of AgNP synthesis emerged as the preferred pathway for synthesis. This review focuses extensively on the biosynthesis of AgNP-mediated through different plant species worldwide in the past 10 years. The most popularly utilized application areas have been highlighted with their in-depth mechanistic approach in this review, along with the discussion on the different phytochemicals playing an important role in the bio-reduction of silver ions. In addition to this, the environmental factors which govern their synthesis and stability have been reviewed. The paper systematically analyses the trend of research on AgNP biosynthesis throughout the world through bibliometric analysis. Apart from this, the feasibility analysis of the plant-mediated synthesis of nanoparticles and their applications have been intrigued considering the perspectives of engineering, economic, and environmental limitations. Thus, the review is not only a comprehensive summary of the achievements and current status of plant-mediated biosynthesis but also provides insight into emerging future research frontier. Supplementary Information: The online version contains supplementary material available at 10.1007/s13204-021-02135-5.

Multilevel mobile health approach to improve cardiovascular health in resource-limited communities with Step It Up: a randomised controlled trial protocol targeting physical activity.

INTRODUCTION: Although physical activity (PA) reduces cardiovascular disease (CVD) risk, physical inactivity remains a pressing public health concern, especially among African American (AA) women in the USA. PA interventions focused on AA women living in resource-limited communities with scarce PA infrastructure are needed. Mobile health (mHealth) technology can increase access to PA interventions. We describe the development of a clinical protocol for a multilevel, community-based, mHealth PA intervention for AA women. METHODS AND ANALYSIS: An mHealth intervention targeting AA women living in resource-limited Washington, DC communities was developed based on the socioecological framework for PA. Over 6 months, we will use a Sequential Multi-Assignment, Randomized Trial approach to compare the effects on PA of location-based remote messaging (named 'tailored-to-place') to standard remote messaging in an mHealth intervention. Participants will be randomised to a remote messaging intervention for 3 months, at which point the intervention strategy will adapt based on individuals' PA levels. Those who do not meet the PA goal will be rerandomised to more intensive treatment. Participants will be followed for another 3 months to determine the contribution of each mHealth intervention to PA level. This protocol will use novel statistical approaches to account for the adaptive strategy. Finally, effects of PA changes on CVD risk biomarkers will be characterised. ETHICS AND DISSEMINATION: This protocol has been developed in partnership with a Washington, DC-area community advisory board to ensure feasibility and acceptability to community members. The National Institutes of Health Intramural IRB approved this research and the National Heart, Lung, and Blood Institute provided funding. Once published, results of this work will be disseminated to community members through presentations at community advisory board meetings and our quarterly newsletter. TRIAL REGISTRATION NUMBER: NCT03288207.

Incorporation of α-methylated amino acids into Apolipoprotein A-I mimetic peptides improves their helicity and cholesterol efflux potential.

Apolipoprotein A-I (ApoA-I) mimetic peptides are potential therapeutic agents for promoting the efflux of excess cellular cholesterol, which is dependent upon the presence of an amphipathic helix. Since α-methylated Ala enhances peptide helicity, we hypothesized that incorporating other types of α-methylated amino acids into ApoA-I mimetic peptides may also increase their helicity and cholesterol efflux potential. The last helix of apoA-I, peptide 'A' (VLESFKVSFLSALEEYTKKLNT), was used to design peptides containing a single type of α-methylated amino acid substitution (Ala/Aα, Glu/Dα, Lys/Kα, Leu/Lα), as well as a peptide containing both α-methylated Lys and Leu (6α). Depending on the specific residue, the α-helical content as measured by CD-spectroscopy and calculated hydrophobic moments were sometimes higher for peptides containing other types of α-methylated amino acids than those with α-methylated Ala. In ABCA1-transfected cells, cholesterol efflux to the peptides showed the following order of potency: 6α>Kα≈Lα≈Aα≫Dα≈A. In general, α-methylated peptides were resistant to proteolysis, but this varied depending on the type of protease and specific amino acid substitution. In summary, increased helicity and amphilicity due to α-methylated amino acid substitutions in ApoA-I mimetic peptides resulted in improved cholesterol efflux capacity and resistance to proteolysis, indicating that this modification may be useful in the future design of therapeutic ApoA-I mimetic peptides.

Select ß- and γ-branched 1-alkylpyrazol-4-yl methylcarbamates exhibit high selectivity for inhibition of Anopheles gambiae versus human acetylcholinesterase.

The widespread emergence of pyrethroid-resistant Anopheles gambiae has intensified the need to find new contact mosquitocides for indoor residual spraying and insecticide treated nets. With the goal of developing new species-selective and resistance-breaking acetylcholinesterase (AChE)-inhibiting mosquitocides, in this report we revisit the effects of carbamate substitution on aryl carbamates, and variation of the 1-alkyl group on pyrazol-4-yl methylcarbamates. Compared to aryl methylcarbamates, aryl dimethylcarbamates were found to have lower selectivity for An. gambiae AChE (AgAChE) over human AChE (hAChE), but improved tarsal contact toxicity to G3 strain An. gambiae. Molecular modeling studies suggest the lower species-selectivity of the aryl dimethylcarbamates can be attributed to a less flexible acyl pocket in AgAChE relative to hAChE. The improved tarsal contact toxicity of the aryl dimethylcarbamates relative to the corresponding methylcarbamates is attributed to a range of complementary phenomena. With respect to the pyrazol-4-yl methylcarbamates, the previously observed low An. gambiae-selectivity of compounds bearing α-branched 1-alkyl groups was improved by employing ß- and γ-branched 1-alkyl groups. Compounds 22a (cyclopentylmethyl), 21a (cyclobutylmethyl), and 26a (3-methylbutyl) offer 250-fold, 120-fold, and 96-fold selectivity, respectively, for inhibition of AgAChE vs. hAChE. Molecular modeling studies suggests the high species-selectivity of these compounds can be attributed to the greater mobility of the W84 side chain in the choline-binding site of AgAChE, compared to that of W86 in hAChE. Compound 26a has reasonable contact toxicity to G3 strain An. gambiae (LC50 = 269 µg/mL) and low cross-resistance to Akron strain (LC50 = 948 µg/mL), which bears the G119S resistance mutation.

Structural properties of apolipoprotein A-I mimetic peptides that promote ABCA1-dependent cholesterol efflux.

Peptides mimicking the major protein of highdensity lipoprotein (HDL), apolipoprotein A-I (apoA-I), are promising therapeutics for cardiovascular diseases. Similar to apoA-I, their atheroprotective property is attributed to their ability to form discoidal HDL-like particles by extracting cellular cholesterol and phospholipids from lipid microdomains created by the ABCA1 transporter in a process called cholesterol efflux. The structural features of peptides that enable cholesterol efflux are not well understood. Herein, four synthetic amphipathic peptides denoted ELK, which only contain Glu, Leu, Lys, and sometimes Ala, and which have a wide range of net charges and hydrophobicities, were examined for cholesterol efflux. Experiments show that ELKs with a net neutral charge and a hydrophobic face that subtends an angle of at least 140° are optimal for cholesterol efflux. All-atom molecular dynamics simulations show that peptides that are effective in promoting cholesterol efflux stabilize HDL nanodiscs formed by these peptides by the orderly covering of the hydrophobic acyl chains on the edge of the disc. In contrast to apoA-I, which forms an anti-parallel double belt around the HDL, active peptides assemble in a mostly anti-parallel "picket fence" arrangement. These results shed light on the efflux ability of apoA-I mimetics and inform the future design of such therapeutics.

N'-mono- and N, N'-diacyl derivatives of benzyl and arylhydrazines as contact insecticides against adult Anopheles gambiae.

New public health insecticides are urgently required to prevent the spread of vector-borne disease. With the goal of identifying new K+-channel-directed mosquitocides, analogs of the RH-5849 family of diacyl t-butylhydrazines were synthesized and tested for topical toxicity against adult Anopheles gambiae, the African vector of malaria. In total, 80N'-monoacyl and N, N'-diacyl derivatives of benzyl- and arylhydrazines were prepared. Three compounds (2bo, 2kb, 3ab) were identified that were more toxic than RH-5849 and RH-1266. The potencies of these compounds to block K+ currents in An. gambiae and human Kv2.1 channels were assessed to address their possible mechanism of mosquitocidal action. Selectivity for inhibition of An. gambiae Kv2.1 vs human Kv2.1 did not exceed 3-fold. Furthermore, no correlation was seen between the potency of insecticidal action and K+ channel blocking potency. These observations, combined with the minimal knockdown seen with 2bo near its LD50 value, suggests a mode of action outside of the nervous system.

Identification of a novel lipid binding motif in apolipoprotein B by the analysis of hydrophobic cluster domains.

Apolipoprotein B (apoB) is a large amphipathic protein that is the structural scaffold for the formation of several classes of lipoproteins involved in lipid transport throughout the body. The goal of the present study was to identify specific domains in the apoB sequence that contribute to its lipid binding properties. A sequence analysis algorithm was developed to identify stretches of hydrophobic amino acids devoid of charged amino acids, which are referred to as hydrophobic cluster domains (HCDs). This analysis identified 78 HCDs in apoB with hydrophobic stretches ranging from 6 to 26 residues. Each HCD was analyzed in silico for secondary structure and lipid binding properties, and a subset was synthesized for experimental evaluation. One HCD peptide, B38, showed high affinity binding to both isolated HDL and LDL, and could exchange between lipoproteins. All-atom molecular dynamics simulations indicate that B38 inserts 3.7Å below the phosphate plane of the bilayer. B38 forms an unusual α-helix with a broad hydrophobic face and polar serine and threonine residues on the opposite face. Based on this structure, we hypothesized that B38 could efflux cholesterol from cells. B38 showed a 12-fold greater activity than the 5A peptide, a bihelical Class A amphipathic helix (EC50 of 0.2658 vs. 3.188µM; p<0.0001), in promoting cholesterol efflux from ABCA1 expressing BHK-1 cells. In conclusion, we have identified novel domains within apoB that contribute to its lipid biding properties. Additionally, we have discovered a unique amphipathic helix design for efficient ABCA1-specific cholesterol efflux.

Toxicity and Synergistic Activities of Chalcones Against Aedes aegypti (Diptera: Culicidae) and Drosophila melanogaster (Diptera: Drosophilidae).

Mosquito-borne illnesses are of great concern throughout the world, and chemical insecticides are commonly employed to decrease mosquito populations. However, the developmental insecticide pipeline for vector control has primarily been filled by repurposed agricultural products, and is hampered by their widespread use and insecticide resistance. The present study was performed in the search for new chemical insecticides or insecticide synergists. Screening of 31 chalcone analogs was performed using Aedes aegypti (Linnaeus) first-instar larval toxicity assay, and oral feeding to Drosophila melanogaster's proper authority should be (Meigen). Synergism studies were performed by topically applying chalcones to adult female Ae. aegypti mosquitoes to examine its impact on activity of carbaryl, which was compared to piperonyl butoxide alone. Fourteen chalcone analogs had LC50 values in the range of 0.4-38 ppm against first-instar Ae. aegypti larvae, and three chalcones displayed toxicity against D. melanogaster via feeding (LC50 values ranged from 146-214 µg/ml). Two chalcones synergized carbaryl toxicity against adult Ae. aegypti with efficacy similar to piperonyl butoxide. As a result, it is concluded that chalcones may serve as novel insecticides and synergists after further structural optimization.

Toxicology of potassium channel-directed compounds in mosquitoes.

Potential targets for new vector control insecticides are nerve and muscle potassium channels. In this study, the activities of known potassium channel blockers (4-aminopyridine, quinidine, and tetraethylammonium) and the insecticide propoxur were compared to three experimental catechols and several other compounds against Anopheles gambiae and Aedes aegypti mosquitoes. Experimental catechol 1 was the most toxic experimental compound in all of the mortality assays conducted, but was at least 100-fold and 39-fold less toxic than propoxur against Ae. aegypti and An. gambiae, respectively. Injection treatment and synergist (piperonyl butoxide) bioassays found that catechol toxicity was not unduly impacted by cuticular transport or oxidative metabolism. Electrophysiological studies showed a decrease in amplitude of evoked muscle contractions, along with an increase in twitch duration at concentrations that increased basal muscle tension (mM). High concentration effects on basal muscle tension were matched by complete depolarization of the muscle membrane potential. Effects on muscle physiology and blockage of Kv2.1 potassium channels in patch clamp experiments were generally consistent with in vivo toxicity, except for 4-aminopyridine, which suggest the involvement of other potassium channel subtypes. Extensive melanization of Anopheles larvae, but not Aedes larvae, occurred from exposure to catechol compounds. Interaction with the phenol oxidase system within insects may be the cause of this melanization, but any contribution to toxicity requires further investigation.

Carbon nitride supported copper nanoparticles: light-induced electronic effect of the support for triazole synthesis.

The composite framework of graphitic carbon nitride (gCN) supported copper nanoparticle can act as a high-performance photoreactor for the synthesis of 1,2,3-triazole derivatives under light irradiation in the absence of alkaline condition. The photoactivity of gCN originates from an electron transition from the valence band to the conduction band, in the presence of photon energy, and the hot electron acts as a scavenger of the terminal proton of the alkyne molecule to facilitate the formation of copper acetanilide complex. In this study, we have performed the experiment under a different photonic environment, including dark condition, and in the presence and absence of base. A comparative study was also executed using Cu-TiO2 system, as a reference material, in the support of our proposed mechanism. The recycling performance and the photocorrosion effect of the catalyst have also been reported in this study.

Light effect on Click reaction: Role of photonic quantum dot catalyst.

Due to the light excitation, the valence band electron of the copper (I) sulfide quantum dot transfer to the conduction band and act as a scavenger of the terminal proton of the alkyne in the presence of organic azide with the formation of 1,4-disubstituted 1,2,3-triazoles, where the copper(I) species of Cu2S act as a catalyst for the reaction. The above cycloaddition reaction between alkyne and azide is commonly known as the Click reaction. In this study, experiments were carried out under the exposure of ultra-violate and daylight and also dark environment. According to the original recommendation for the Click reaction, the role of the base was also considered for this experiment. We found that the effect of conduction band electron is more efficient than the recommended conventional base mediated reaction procedure.

Difluoromethyl ketones: Potent inhibitors of wild type and carbamate-insensitive G119S mutant Anopheles gambiae acetylcholinesterase.

Malaria is a devastating disease in sub-Saharan Africa, and current vector control measures are threatened by emerging resistance mechanisms. With the goal of developing new, selective, resistance-breaking insecticides we explored α-fluorinated methyl ketones as reversible covalent inhibitors of Anopheles gambiae acetylcholinesterase (AgAChE). Trifluoromethyl ketones 5 demonstrated remarkable volatility in microtiter plate assays, but 5c,e-h exhibited potent (1-100 nM) inhibition of wild type (WT) AgAChE and weak inhibition of resistant mutant G119S mutant AgAChE. Fluoromethyl ketones 10c-i exhibited submicromolar to micromolar inhibition of WT AgAChE, but again only weakly inhibited G119S AgAChE. Interestingly, difluoromethyl ketone inhibitors 9c and 9g had single digit nanomolar inhibition of WT AgAChE, and 9g had excellent potency against G119S AgAChE. Approach to steady-state inhibition was quite slow, but after 23 h incubation an IC50 value of 25.1 ± 1.2 nM was measured. We attribute the slow, tight-binding G119S AgAChE inhibition of 9g to a balance of steric size and electrophilicity. However, toxicities of 5g, 9g, and 10g to adult A. gambiae in tarsal contact, fumigation, and injection assays were lower than expected based on WT AgAChE inhibition potency and volatility. Potential toxicity-limiting factors are discussed.

Polymer immobilized Cu(I) formation and azide-alkyne cycloaddition: A one pot reaction.

During the polymerization of aniline using copper sulphate, act as an oxidizing agent, the in-situ synthesized Cu(I) ion catalyzed the cyclo-addition between azides and alkynes. This work represents the merging of two steps, synthesis of the catalyst and application of the catalyst, in a one pot reaction. The elimination of the separate catalyst synthesis step is economic in terms of cost and time. As aniline was used as one of the reactant components so there is no requirement to use additional base for this reaction that further eliminates the cost of the process. Again, the catalyst can be readily recovered by filtration and efficiently used for the several sets of reactions without any significant loss of catalytic activity.

3-Oxoisoxazole-2(3H)-carboxamides and isoxazol-3-yl carbamates: Resistance-breaking acetylcholinesterase inhibitors targeting the malaria mosquito, Anopheles gambiae.

To identify potential selective and resistance-breaking mosquitocides against the African malaria vector Anopheles gambiae, we investigated the acetylcholinesterase (AChE) inhibitory and mosquitocidal properties of isoxazol-3-yl dimethylcarbamates (15), and the corresponding 3-oxoisoxazole-2(3H)-dimethylcarboxamide isomers (14). In both series, compounds were found with excellent contact toxicity to wild-type susceptible (G3) strain and multiply resistant (Akron) strain mosquitoes that carry the G119S resistance mutation of AChE. Compounds possessing good to excellent toxicity to Akron strain mosquitoes inhibit the G119S mutant of An. gambiae AChE (AgAChE) with ki values at least 10- to 600-fold higher than that of propoxur, a compound that does not kill Akron mosquitoes at the highest concentration tested. On average, inactivation of WT AgAChE by dimethylcarboxamides 14 was 10-20 fold faster than that of the corresponding isoxazol-3-yl dimethylcarbamates 15. X-ray crystallography of dimethylcarboxamide 14d provided insight into that reactivity, a finding that may explain the inhibitory power of structurally-related inhibitors of hormone-sensitive lipase. Finally, human/An. gambiae AChE inhibition selectivities of these compounds were low, suggesting the need for additional structural modification.