Acyl Hydrazides as Insecticides: Synthesis, Biochemical, Structure-Activity Relationship Studies and Insecticidal Activity of some IGRs Analogues Against Spodoptera littorallis (Boisd.).

The exponential rise in pesticide resistance to conventional chemical pesticides is another major factor driving the development of novel insecticidal active agents. One approach to solving this problem is to investigate novel classes and environmentally safe insecticidal chemicals with a variety of modes of action. Among these techniques is the creation of novel tebufenozide derivatives.

Pyridine Derivatives as Insecticides: Part 6. Design, Synthesis, Molecular Docking, and Insecticidal Activity of 3-(Substituted)methylthio-5,6,7,8-tetrahydroisoquinoline-4-carbonitriles Toward (, 1887).

Three new series of 3-(substituted)methylthio-4-cyano-5,6,7,8-tetrahydroisoquinolines were designed and synthesized starting from readily available materials, 7-acetyl-4-cyano-1,6-dimethyl-6-hydroxy-8-(4-pyridyl, 3-pyridyl, phenyl, 4-methoxyphenyl, or 4-chlorophenyl)-5,6,7,8-tetrahydrosoquinoline-3(2)-thiones - in high yields and very pure states. Thus, compounds - were reacted with some chloro reagents, namely, -aryl-2-chloroacetamides - and -(naphthalen-2-yl)-2-chloroacetamide () under mild basic conditions to give the first two series of the target compounds, 3-(-aryl)carbamoylmethylthio-5,6,7,8-tetrahydroisoquinoline-4-carbonitriles - and -, respectively. Reaction of compounds , with ethyl chloroacetate under the same conditions gave the other series, 3-ethoxycarbonyl-methylthio-5,6,7,8-tetrahydroisoquinoline-4-carbonitriles ,.

Pyridine Derivatives as Insecticides. Part 5. New Thieno[2,3-]pyridines and Pyrazolo[3,4-]pyridines Containing Mainly Ethyl Nicotinate Scaffold and Their Insecticidal Activity toward (Glover,1887).

Ethyl 5-cyano-1,6-dihydro-2-methyl-4-(2'-thienyl)-6-thioxonicotinate () was synthesized and reacted with ethyl chloroacetate in the presence of sodium acetate or sodium carbonate to give ethyl 5-cyano-6-((2-ethoxy-2-oxoethyl)thio)-2-methyl-4-(2'-thienyl)nicotinate () or its isomeric thieno[2,3-]pyridine . 3-Aminothieno[2,3-]pyridine-2-carboxamide was also synthesized by the reaction of with 2-chloroacetamide. The reaction of with hydrazine hydrate in boiling ethanol gave acethydrazide .

New Prospective Insecticidal Agents Based on N-(arylcarbamothioyl)arylmide Derivatives Against Spodoptera frugiperda: Design, Synthesis, Toxicological, Biological, Biomedical Studies and Antibacterial Activity.

In this work, a novel series of N-(arylcarbamothioyl)arylmide) 2-11 were synthesized by treating One-Pot three-multicomponent of Aroyl chloride, ammonium isothiocyanate and amine compounds under refluxing conditions. Using spectroscopic methods, the chemical structure of the novelty developed compounds were investigated. After five days, the proposed derivatives' insecticidal bioassay was assessed using the median lethal concentration (LC) against the second & fourth larvae of Spodoptera frugiperda as toxicity agents.

Synthesis, Insecticide Evaluation & Molecular Docking Studies of Some New Functionalized Pyrazole Derivatives Against the Cotton Leafworm, Spodoptera littoralis.

5-(Cyanomethyl)-3-((5,5-dimethyl-3-oxocyclohex-1-en-1-yl)amino)-1H-pyrazole-4-carbonitrile (3) is used as a key for the synthesis of arylidenes 5 a-fvia its reaction with some aldehydes 4 a-f. 5-[(5,5-Dimethyl-3-oxocyclohex-1-en-1-yl)amino]-3-(2-imino-2H-chromen-3-yl)-1H-pyrazole-4-carbonitrile (7) was synthesized via the reaction of compound (3) with 2-Hydroxybenzaldehyde in EtOH/piperidine. The target compounds were tested against cotton leafworm larvae in their second and fourth instar.

Synthesis and Biological Evaluation of Benzamide Compounds as Insecticides Agents Against Spodoptera Frugiperda (Lepidoptera: Noctuidae).

Due to its severe damage, Spodoptera frugiperda is receiving attention as one of the biggest dangers to world food security. Although there are numerous insecticides that are widely and successfully used to control S. frugiperda, they do not have an immediate effect.

Thiadiazole/Thiadiazine Derivatives as Insecticidal Agent: Design, Synthesis, and Biological Assessment of 1,3,4-(Thiadiazine/Thiadiazole)-Benzenesulfonamide Derivatives as IGRs Analogues against .

In keeping with our investigation, a simple and practical synthesis of novel heterocyclic compounds with a sulfamoyl moiety that can be employed as insecticidal agents was reported. The compound 2-hydrazinyl--(4-sulfamoylphenyl)-2-thioxoacetamide was coupled smoothly with triethylorthoformate or a variety of halo compounds, namely phenacyl chloride, chloroacetyl chloride, chloroacetaldehyde, chloroacetone, 1,3-dichloropropane, 1,2-dichloroethane, ethyl chloroformate, 2,3-dichloro-1,4-naphthoquinone, and chloroanil respectively, which afforded the 1,3,4-thiadiazole and 1,3,4-thiadiazine derivatives. The new products structure was determined using elemental and spectral analysis.

Exploration of Some Heterocyclic Compounds Containing Trifluoromethylpyridine Scaffold as Insecticides Toward Aphis gossypii Insects.

Five types of heterocyclic compounds containing trifloromethylpyridine scaffold namely; 3-cyano-2-(N-phenyl)carbamoylmethylthio-6-(thiophen-2-yl)-4-trifluoromethyl-pyridine (6a), thieno[2,3-b]pyridines 3-5 and 7a-c, pyrido[3',2':4,5]thieno[3,2-d] pyrimidines 8-13 and 15a-c, pyrido[3',2':4,5]thieno[3,2-d][1,2,3]triazines 16a,b, and 9-(thiophen-2-yl)-7-(trifluoromethyl) pyrido [3',2':4,5]thieno[2,3-e][1,2,4]triazolo[1,5-c]pyrimidine (14) were synthesized in excellent yields and very pure state. The structures of these compounds were confirmed by elemental and spectral analyses. Most of the synthesized compounds were evaluated as insecticidal agents toward Aphis gossypii insects and promising results obtained.

A tolerant hydrologic technique for real-time selection of optimum QPFs from NWPMs for flood warning applications.

The most important information required to successfully issue a flood warning is the quantitative precipitation forecasts (QPFs). This is important to run subsequent rainfall-runoff simulations. A rainfall-runoff simulation derives its accuracy mainly from the accuracy of the input QPFs.

Synthesis and Insecticidal Evaluation of 3,5-Dicyanopyridines Against Cotton Aphids via Microwave-Assisted Multicomponent Reactions.

Certain 2-amino-6-alkoxy-4-arylpyridine-3,5-dicyanide 1a-e were prepared via a straightforward process using microwave technology rather than conventional methods. This involved reaction of arylidenemalononitrile thru propanedinitrile in the occurrence of sodium alkoxide under MW. While, their positional isomer 4-amino-6-alkoxy-2-arylpyridine-3,5-dicyanide 3a-j have been separated from the reaction of aryl aldehydes with 2-aminoprop-1-ene-1,1,3-tricarbonitrile 2 in the presence of sodium alkoxide using microwave technic.

Green synthesis and bioefficacy screening of new insect growth regulators as eco-friendly insecticides against the cotton mealybug Phenacoccus solenopsis.

Overcoming or reducing the majority of difficulties caused by the use of common pesticides requires the use of developed, secure, unique and selective organic compounds. Due to their clear mechanism of action on pests and lower poisonousness towards vertebrates than conventional insecticides, juvenile hormone analogues as an example of insect growth regulators appear promising. Thus, a unique set of pure insect growth regulators has been synthesized.

Design, Characterization and SAR Studies of Novel Bioactive Benzylideneacetophenone Derivatives as Insecticidal Agents against Spodoptera frugiperda (Lepidoptera: Noctuidae).

Unintentional environmental effects brought on by insecticides encourage the creation of safer substitutes. A very polyphagous migrating lepidopteran pest species in Africa called S. Frugiperda causes terrible damage.

Pyridine Derivatives as Insecticides─Part 4: Synthesis, Crystal Structure, and Insecticidal Activity of Some New Thienylpyridines, Thienylthieno[2,3-]pyridines, and Related Heterocyclic Derivatives.

The reaction of ethyl 5-cyano-2-methyl-4-(thiophen-2-yl)-6-thioxo-1,6-dihydropyridine-3-carboxylate () with 2-chloroacetamide or its -aryl derivatives gave ethyl 6-((2-amino-2-oxoethyl)thio)-5-cyano-2-methyl-4-(thiophen-2-yl) nicotinate () or its -aryl derivatives -, respectively. Cyclization of - into their isomers - was carried out by heating in absolute ethanol in the presence of a catalytic amount of sodium ethoxide. The -aminoamide was reacted with some aryl aldehydes in refluxing ethanol containing a few drops of conc.

Green synthesis, biological and molecular docking of some novel sulfonamide thiadiazole derivatives as potential insecticidal against Spodoptera littoralis.

Although crop plants provide the majority of human food, pests and insects frequently cause huge economic losses. In order to develop innovative insecticidal compounds with low toxicity and a positive environmental impact, we developed new N-(4-sulfamoylphenyl)-1,3,4-thiadiazole-2-carboxamide derivatives (2-12). With the use of spectroscopic techniques and elemental data, the chemical structure of these new compounds was meticulously clarified.

Functionalized Pyridines: Synthesis and Toxicity Evaluation of Potential Insecticidal Agents against .

Using ultrasound technology instead of traditional methods, some pyridine derivatives were prepared by a simple procedure via a four-component reaction of different aromatic aldehydes, acetyl aryl, sodium alkoxide, and malononitrile, and additionally, all prepared compounds were monitored for insecticidal activities toward nymphs and adults of cowpea aphid. Though a lot of insecticides are discovered as a novelty on the other hand, neonicotinoid compounds are reflected as the most affected insecticides against aphids and many other pests. Thus, some of the pyridine derivatives were chemically prepared as analogues to a large group of insecticides called neonicotinoids.

Synthesis and insecticide evaluation of some new oxopropylthiourea compounds as insect growth regulators against the cotton leafworm, Spodoptera littoralis.

In this project we aim to share in increasing the production of the most important non-food agricultural product i.e. cotton via protection of it is plant.

Design and Synthesis of Pyridine and Thiazole Derivatives as Eco-friendly Insecticidal to Control Olive Pests.

Treatment of p-tosyloxybenzaldehyde (1) with ethyl cyanoacetate afforded ethyl 2-cyano-3-(4-{[(4-methylphenyl)sulfonyl]oxy}phenyl)acrylate (2) which reacted with some active methylene derivatives under microwave irradiation in presence of ammonium acetate yielded pyridine derivatives 3-7. On the other hand, when treatment of compound 1 with thiosemicarbazide gave 4-tosyloxybenzylidenethiosemicarbazone (8), which allowed to react with some active methylene compounds, such as: ethyl bromoacetate, chloroacetonitrile or phenacyl bromide derivatives gave thiazole derivatives 9-13. The structure of all products were confirmed by elemental and spectroscopic analyses such as IR, H-NMR, CNMR and mass spectra.

Design, Synthesis, and Toxicological Activities of Novel Insect Growth Regulators as Insecticidal Agents against (Boisd.).

As a result of some major problems that come from using insecticides, the use of safe alternatives to these pesticides has become very necessary. Thus, a novel series of predicted toxicologically active urea, thiourea, thiosemicarbazide, oxadiazole, pyrazole, and triazine derivatives have been synthesized in a pure form to be lufenuron analogues as insect growth regulators which were screened and examined against (Boisd). The structure of synthesized compounds was established by means of spectroscopic and elemental analyses.

Novel Antidiabetic Medications in Polycystic Ovary Syndrome.

Polycystic ovary syndrome is a very common endocrine disorder prevalent in premenopausal women. Patients with polycystic ovary syndrome present with abnormal menstruation, ovulation disorders, and hyperandrogenemia. They are often accompanied by insulin resistance, metabolic disorders, and other cardiovascular abnormalities.

Design, Synthesis, and SAR Studies of Some Novel Chalcone Derivatives for Potential Insecticidal Bioefficacy Screening on (Lepidoptera: Noctuidae).

is a species of the order Lepidoptera. It is one of the species of fall armyworm moths distinguished by its larval life stage, is found in different regions of Africa, and can cause incredible damage. This is the first report produced by the preparation of an indexed combinatorial library of novel chalcone derivatives treatment of 4-formylphenyl4-methylbenzenesulfonate () with some acetyl compounds in the presence of NaOH.

Pyridine Derivatives as Insecticides. Part 3. Synthesis, Crystal Structure, and Toxicological Evaluation of Some New Partially Hydrogenated Isoquinolines against (, 1887).

Three new series of isoquinolines, that is, 7-acetyl-3-acetonylsulfanyl-8-aryl-1,6-dimethyl-6-hydroxy-5,6,7,8-tetrahydroisoquinoline-4-carbonitriles (-); 3-acetonylsulfanyl-8-aryl-1,6-dimethyl-7,8-dihydroisoquinoline-4-carbonitriles (-); and 7-acetyl-8-aryl-1,6-dimethyl-3-ethylsulfanyl-7,8-dihydroisoquinoline-4-carbo-nitriles (,) were carefully synthesized. Also, pyrazoloisoquinoline was used as a precursor for synthesis of 7-ethylsulfanyl-4-phenyl-1-thiocarbamoyl-3,5,9a-trimethyl-3a,4,9,9a-tetrahydro-1-pyrazolo[3,4-g]isoquinoline-8-carbonitrile (); 7-benzyl-sulfanyl-4-phenyl-1-thiocarbamoyl-3,5,9a-trimethyl-3a,4,9,9a-tetrahydro-1-pyrazolo[3,4-]isoquinoline-8-carbonitrile (); and 7-ethylsulfanyl-1-(4-oxo-4,5-dihydrothiazol-2-yl)-4-phenyl-3,5,9a-trimethyl-3a,4,9,9a-tetrahydro-1-pyrazolo[3,4-]isoquinoline-8-carbonitrile (). Moreover, the crystal structures of two representative compounds were determined.

Bile Cast Nephropathy: A Comprehensive Review.

Bile cast nephropathy (BCN) or cholemic nephropathy (CN) is an acute renal dysfunction, including acute kidney injury (AKI) in the setting of liver injury. It is a common phenomenon in patients with liver disease and is associated with significant morbidity and mortality. CN is characterized by hemodynamic changes in the liver, kidney, systemic circulation, intratubular cast formation, and tubular epithelial cell injury.

Synthesis and Toxicological Effect of Some New Pyrrole Derivatives as Prospective Insecticidal Agents against the Cotton Leafworm, (Boisduval).

Herein, a series of biologically active pyrrole derivatives, namely 2-[(3-cyano-5-aryl-1-pyrrol-2-yl)thio]acetic acids , 2-[(2-hydroxyethyl)-thio]-5-aryl-1-pyrrole-3-carbonitriles , and 2-[(2-amino-ethyl)thio]-5-aryl-1-pyrrole-3-carbonitriles , 2,2'-disulfanediylbis(5-aryl-1-pyrrole-3-carbonitriles) , 2-((3-cyano-5-aryl-1-pyrrol-2-yl)thio)acetates , 2-[(3-cyano-5-phenyl-1-pyrrol-2-yl)thio]acetohydrazides , and 2-{2-[(3-cyano-5-aryl-1-pyrrol-2-yl)thio]acetyl}--phenyl-hydrazinecarbothioamides , as insecticidal agents, were synthesized via adaptable, smoothly accessible 2-(2-oxo-2-arylylethyl)malononitriles . The structures were proved using infrared (IR), nuclear magnetic resonance (NMR), and mass spectrum (MS) techniques. Under laboratory conditions, the toxicological characteristics were tested towards , cotton leafworm insect type.

Chemical design and bioefficacy screening of new insect growth regulators as potential insecticidal agents against (Boisd.).

The new compounds were chemically synthesized and their spectroscopic analysis was done to determine their chemical structure. All the compounds were screened for their insecticidal potential against (Boisd.).

Strategies for stabilizing formulation and QbD assisted development of robust stability indicating method of azilsartan medoxomil/chlorthalidone.

Reasons for formulation instability were investigated either encountered during production or analytical processes of azilsartan medoxomil (AZM)/chlorthalidone hydrochloride (CLT) tablets. Through the identification of the most feasible degradation pathways, several strategies were proposed to enhance the stability of AZM/CLT formulation. Furthermore, a robust HPLC-UV method was developed and validated for the determination of AZM, CLT in the presence of their possible degradation products.