Comparative Effects of Essential Oil and Its Nanoliposomal State on Mortality of Larvae.

Background: Malaria has remained the most dreadful vector-borne disease; hence, vector control is the most affordable and achievable approach to mitigate the disease burden. Due to the emergence of resistance and environmental pollution, herbal larvicides are considered an alternative to chemical types. Also, nanotechnology has been proposed as a promising solution to improve the efficiency of plant larvicides.

Novel Benzotriazole-β-lactam Derivatives as Antimalarial Agents: Design, Synthesis, Biological Evaluation and Molecular Docking Studies.

Many people around the world suffer from malaria, especially in tropical or subtropical regions. While malaria medications have shown success in treating malaria, there is still a problem with resistance to these drugs. Herein, we designed and synthesized some structurally novel benzotriazole-β-lactams using 2-(1H-benzo[d][1,2,3]triazol-1-yl)acetic acid as a key intermediate.

Promising Larvicidal Effects of Nanoliposomes Containing Carvone and Mentha spicata and Tanacetum balsamita Essential Oils Against Anopheles stephensi.

Purpose: The use of synthetic pesticides to control the spread of mosquito-borne diseases has caused environmental pollution and insecticide resistance in mosquitoes. Developments of new green insecticides have thus received more attention to overcome these problems.

Methods: Nanoliposomes containing carvone and essential oils were first prepared.

Nanoliposomal Trachyspermum ammi (L) sprague essential oil for effective control of malaria mosquito larvae, Anopheles stephensi Liston.

Controlling mosquito vectors at immature stages using larvicides is a practical strategy to stave off mosquito-borne diseases such as malaria. Developing nanoliposomes bearing essential oil is a promising approach to improving the efficacy and stability of EOs-derived larvicides. The main aim of this investigation was to assess the efficacy of nanoliposome containing Trachyspermum ammi L.

Synthesis, docking and evaluation of in vitro anti-inflammatory activity of novel morpholine capped β-lactam derivatives.

This study reports the synthesis and biological investigation of three series of novel monocyclic β-lactam derivatives bearing a morpholine ring substituent on the nitrogen. The resulting β-lactam adducts were synthesized via Staudinger's [2 + 2]-ketene-imine cycloaddition reaction. New synthesized products were fully characterized by spectral data and elemental analyses, and then evaluated for anti-inflammatory activity toward human inducible nitric oxide synthase (iNOS) and cytotoxicity toward HepG2 cell line.

Synthesis of New -Lactams Bearing the Biologically Important Morpholine Ring and POM Analyses of Their Antimicrobial and Antimalarial Activities.

Some new lactams bearing biologically important morpholine ring have been synthesized by acylation of amino lactams in the presence of morpholine-4-carbonyl chloride. These novel -lactams were prepared under mild reaction conditions without any solvent in short reaction times. Their biological activities have been examined against microbial agents such as () (), () and fungi such as () and ().

Asymmetric Organocatalytic Synthesis of Substituted Chiral 1,4-Dihydropyridine Derivatives.

The first cinchona-alkaloid-organocatalyzed enantioselective synthesis of chiral 1,4-dihydropyridine derivatives is described. Bis-cinchona catalyst 3b activates the Michael addition reaction between malononitrile derivatives 2 and enamines 1, affording the appealing and highly substituted 1,4-dihydropyridines 4 with very good results in most cases. This is one of very few examples of the synthesis of chiral 1,4-dihydropyridines by an enantioselective catalytic procedure.

New Organocatalytic Asymmetric Synthesis of Highly Substituted Chiral 2-Oxospiro-[indole-3,4'- (1',4'-dihydropyridine)] Derivatives.

Herein, we report our preliminary results concerning the first promising asymmetric synthesis of highly functionalized 2-oxospiro-[indole-3,4'-(1',4'-dihydropyridine)] via the reaction of an enamine with isatylidene malononitrile derivatives in the presence of a chiral base organocatalyst. The moderate, but promising, enantioselectivity observed (30%-58% ee (enantiomeric excess)) opens the door to a new area of research for the asymmetric construction of these appealing spirooxindole skeletons, whose enantioselective syntheses are still very limited.

3-(2,4-Di-chloro-phen-oxy)-1-(4-meth-oxy-benz-yl)-4-(4-nitro-phen-yl)azetidin-2-one.

The β-lactam ring of the title compound, C23H18Cl2N2O5, is nearly planar [maximum deviation = 0.019 (2) Å for the N atom] and its mean plane makes dihedral angles of 56.86 (15), 68.

1-[3-(Morpholin-4-yl)prop-yl]-3-[(naph-tha-len-2-yl)oxy]-4-(3-nitro-phen-yl)azeti-din-2-one.

In the title compound, C26H27N3O5, the β-lactam (azetidin-2-one) ring is nearly planar [maximum deviation = 0.011 (3) Å]. The mean plane formed by the four C atoms of the morpholine ring, which adopts a chair conformation, the benzene ring and the naphthalene ring system form dihedral angles of 72.

(E)-4-{[(Morpholin-4-yl)imino]-meth-yl}benzo-nitrile.

In the title compound, C12H13N3O, the morpholine ring adopts a chair conformation and its mean plane is inclined to that of the benzene ring by 16.78 (12)°. The N-N=C-C bridge, which has an E conformation, has a torsion angle of 173.

1-(Morpholin-4-yl)-4-(2-nitro-phen-yl)spiro-[azetidine-3,9'-xanthen]-2-one.

In the title compound, C22H21N3O5, the β-lactam (azetidin-2-one) ring is nearly planar [maximum deviation = 0.010 (1) Å] and makes dihedral angles of 69.22 (5), 55.

1-[3-(Morpholin-4-yl)prop-yl]-4-(3-nitro-phen-yl)spiro-[azetidine-3,9'-xanthen]-2-one.

The β-lactam (azetidin-2-one) ring of the title compound, C28H27N3O5, is nearly planar [maximum deviation = 0.010 (1) Å] and makes dihedral angles of 75.77 (5), 52.

1-(4-Meth-oxy-phen-yl)-4-(3-nitro-phen-yl)-3-phen-oxy-azetidin-2-one.

In the title compound, C(22)H(18)N(2)O(5), the four-membered β-lactam ring is nearly planar, with a maximum deviation of 0.023 (2) Å for the N atom, and has long C-C distances of 1.525 (5) and 1.