Evaluation of Pyrazolyl-Indolizine Derivatives as Antimicrobial Agents: Synthesis, In vitro, In silico ADMET and Molecular Docking Studies.

Herein, we report analogues of s-indacene by the synthesis of novel indolizine derivatives. Using chloroform as an appropriate solvent, sixteen derivatives of pyrazolyl-indolizine (4--19) were prepared by the reaction of 3-(dimethylamino)-1-(1H-pyrrol-2-yl)prop-2-en-1-one (1) with hydrazonoyl chloride derivatives (2) in the presence of triethylamine in good to excellent yields. We used NMR spectra, IR, mass spectrometry, as well as elemental analyses to prove the chemical structures and the purity of the synthesized compounds 4-19.

Production of natural flavor compounds using fermented soybean meal extract and their biological potential: a comprehensive study.

This study aims to investigate the production of natural flavor compounds through the utilization of -fermented soybean meal extract and evaluate their biological potential. The experiment involved a comprehensive investigation to assess the capabilities and effects of the produced flavor compounds. The resulting flavor compounds were subjected to various tests to assess their properties, including cytotoxicity, antioxidant activity, anticancer potential, antiviral activity, and antimicrobial activity.

Toxicity and Repellency Efficacy of Benzyl Alcohol and Benzyl Benzoate as Eco-Friendly Choices to Control the Red Flour Beetle (Herbst. 1797).

is a damaging pest of stored grains, causing significant losses and secreting lethal quinones, which render the grains unfit for human consumption. Chemical insecticides are the most commonly used approach for control; however, they create insecticide resistance and affect the health of humans, animals, and the environment. As a result, it is critical to find an environmentally friendly pest-management strategy.

A protocol for evaluating the entomological impact of larval source reduction on mosquito vectors at hotel compounds in Zanzibar.

There is an increasing awareness of the association between tourism activity and risks of emerging mosquito-borne diseases (MBDs) worldwide. In previous studies we showed that hotels in Zanzibar may play an important role in maintaining residual foci of mosquito vectors populations of public health concern. These findings indicated larval sources removal (LSR) interventions may have a significant negative impact on vector communities.

Newly Synthesized Arylazo Derivatives Induce Apoptosis and G2/M Cell Cycle Arrest With Molecular Docking Validation in Human Cancer Cell Lines.

Objective: We reported herein the synthesis of novel arylazo derivatives 3a-e incorporating isoquinoline moiety.

Methods: A coupling reaction of 2-(6,7-dimethoxy-3,4-dihydroisoquinolin-1-yl)acetonitrile 1 with diazotized heterocyclic amines 2 in ethanol in the presence of sodium acetate to give arylazo derivatives 3a-e.

Results: Cytotoxic effect of five arylazo derivatives on breast carcinoma MCF7 and hepatocellular carcinoma HepG2 was carried out, followed by molecular and functional-based assays, to estimate the anticancer effect of these compounds.

Application of Gurma Melon Pulp-Based Gel Fat Replacer in Mayonnaise.

Gurma melon pulp-based gel (GMPG) was examined as a fat replacement in mayonnaise. GMPG was used to partially replace fat in quantities of 25, 50, and 70%, abbreviated as GMPG-25, GMPG-50, and GMPG-70, respectively. Mayonnaise's physicochemical and sensory properties were studied.

Ethosomal gel for rectal transmucosal delivery of domperidone: design of experiment, and evaluation.

Despite high efficiency of domperidone (DOM) in prophylaxis of emesis accompanied with radiotherapy and chemotherapy, it still can bother cancer patients by its powerful side effects and difficulty of its oral administration. The study was designed to develop and optimize DOM loaded ethosomal gel for rectal transmucosal delivery. Ethosomal formulations were prepared using a 2, 5 full-factorial design where the impact of lecithin concentration and additives were investigated.

Hydrazonoyl chlorides possess promising antitumor properties.

Aims: the main purpose of this study was to identify new selective antitumor agents.

Main Methods: several hydrazonoyl chlorides (HCs) were synthesized and human tumor cell line viability was determined using the MTT assay. Tumor development was assessed using Ehrlich ascites carcinoma (EAC)-bearing mice.

Anticancer activity of novel 3-(furan-2-yl)pyrazolyl and 3-(thiophen-2-yl)pyrazolyl hybrid chalcones: Synthesis and in vitro studies.

Twelve novel chalcone derivatives were prepared using the Claisen-Schmidt condensation reaction. The reaction of 4-acetyl-5-furan/thiophene-pyrazole derivatives 5 with the corresponding aldehydes 6 afforded the targeted chalcone derivatives 7a-l in good yields. The newly synthesized chalcones were fully characterized by spectrometric and elemental analyses.

Risk factors for occurrence and abundance of Aedes aegypti and Aedes bromeliae at hotel compounds in Zanzibar.

Background: A field survey was performed to investigate local environmental factors promoting occurrence and abundance of Aedes aegypti and Ae. bromeliae mosquitoes at hotel compounds in the south-east coastal region of Zanzibar Island.

Methods: The potential risk factors were determined using generalized linear mixed models.

Survey of Dental Implant and Restoration Selection by Prosthodontists in Dubai.

Background: With various surgical and prosthetic component designs being introduced in dental implants, decisions have to be made when choosing a system and a certain prosthodontic protocol. A survey of implant prosthodontic specialists has not been previously performed in the Middle East.

Aim: This study aimed to determine selection criteria and choice of dental implants and restorations by prosthodontic specialists in the Emirate of Dubai, United Arab Emirates.

Emerging epidemics: is the Zanzibar healthcare system ready to detect and respond to mosquito-borne viral diseases?

Background: Effective control of emerging mosquito-borne viral diseases such as dengue, chikungunya, and Zika requires, amongst other things, a functional healthcare system, ready and capable of timely detection and prompt response to incipient epidemics. We assessed the readiness of Zanzibar health facilities and districts for early detection and management of mosquito-borne viral disease outbreaks.

Methods: A cross-sectional study involving all 10 District Health Management Teams and 45 randomly selected public and private health facilities in Zanzibar was conducted using a mixed-methods approach including observations, document review, and structured interviews with health facility in-charges and District Health Management Team members.

Assessment of the core and support functions of the integrated disease surveillance and response system in Zanzibar, Tanzania.

Background: Disease surveillance is a cornerstone of outbreak detection and control. Evaluation of a disease surveillance system is important to ensure its performance over time. The aim of this study was to assess the performance of the core and support functions of the Zanzibar integrated disease surveillance and response (IDSR) system to determine its capacity for early detection of and response to infectious disease outbreaks.

Epidemic risk of arboviral diseases: Determining the habitats, spatial-temporal distribution, and abundance of immature Aedes aegypti in the Urban and Rural areas of Zanzibar, Tanzania.

Background: In Zanzibar, little is known about the arboviral disease vector Aedes aegypti in terms of abundance, spatio-temporal distribution of its larval habitats or factors associated with its proliferation. Effective control of the vector requires knowledge on ecology and habitat characteristics and is currently the only available option for reducing the risk of arboviral epidemics in the island nation of Zanzibar.

Methodology: We conducted entomological surveys in households and surrounding compounds from February to May 2018 in the urban (Mwembemakumbi and Chumbuni) and rural (Chuini and Kama) Shehias (lowest government administrative unit) situated in the Urban-West region of Unguja island, Zanzibar.

Novel [l,2,4]triazolo[3,4-a]isoquinoline chalcones as new chemotherapeutic agents: Block IAP tyrosine kinase domain and induce both intrinsic and extrinsic pathways of apoptosis.

Two novel chemotherapeutic chalcones were synthesized and their structures were confirmed by different spectral tools. Theoretical studies such as molecular modeling were done to detect the mechanism of action of these compounds. In vitro cytotoxicity showed a strong effect against all tested cell lines (MCF7, A459, HepG2, and HCT116), and low toxic effect against normal human melanocytes (HFB4).

Synthesis, Cytotoxicity and Docking Simulation of Novel Annulated Dihydroisoquinoline Heterocycles.

Objective: Coupling of ethyl 2-(6,7-dimethoxy-3,4-dihydroisoquinolin-1-yl)acetate 2 with diazotized anilines in ethanol in the presence of sodium acetate yielded 2-(2-arylhydrazono)-2-(6,7- dimethoxy-3,4-dihydroisoquinolin-1-yl)acetate (4a-f).

Methods: Treatment of 2 with α-bromoketones 6a-f in dry benzene at reflux gave the corresponding isoquinolinium bromides 7a-f. Refluxing of each of the salts 7a-f in dry benzene and in the presence of triethylamine yielded 2-arylpyrrolo-[2,1-a]isoquinoline structures 8a-f, that converted to ethyl (E)-8,9- dimethoxy-3-(phenyldiazen-yl)-2-(aryl)-5,6-dihydropyrrolo[2,1-a]isoquinoline-1-carboxylate (9a-f) upon treatment with diazotized anilines 3 in ethanol in the presence of sodium acetate.

Molecular Docking Study, Cytotoxicity, Cell Cycle Arrest and Apoptotic Induction of Novel Chalcones Incorporating Thiadiazolyl Isoquinoline in Cervical Cancer.

Background: Chalcones are naturally occurring compounds found in various plant species which are widely used for the traditional popular treatments. Chalcones are distinguished secondary metabolites reported to display diverse biological activities such as antiviral, antiplatelet, anti-inflammatory, anticancer, antibacterial and antioxidant agents. The presence of a,ß-unsaturated carbonyl group in chalcones is assumed to be responsible for their bioactivity.

Temporal Pattern of Mutations in the Knockdown Resistance () Gene of Mosquitoes Sampled from Southern Taiwan.

mosquitoes are the principal dengue vector in Taiwan, where the use of insecticides is a key element in the national control strategy. However, control efforts are constrained by the development of resistance to most insecticides, including pyrethroids. In this study, mutations in the voltage-gated sodium channel (VGSC) gene resulting in knockdown resistance () were examined in .

Biological Activity, Apoptotic Induction and Cell Cycle Arrest of New Hydrazonoyl Halides Derivatives.

Background: The hydrazonoyl halides are presently an important target in the field of medicinal chemistry. The interest in the chemistry of hydrazonoyl halides is a consequence of the fact that they undergo a wide variety of reactions which provide routes to a myriad of both heterocyclic and acyclic compounds. In addition, they have diverse biological activities such as antiviral, anthelmintic, antiarthropodal, fungicidal, herbicidal, insecticidal, pesticidal, acaricidal and miticidal Activity correlated to the presence of hydrazonoyl halides.

Synthesis, Cytotoxicity, Antimicrobial and Docking Simulation of Novel Pyrazolo[3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[3,4-c] pyrimidine Derivatives.

Background: Isobutyrohydrazonoyl bromide 1 was used as a precursor for the synthesis of 4-imino-3-isopropyl-1-(4-nitrophenyl)-1,4-dihydro-5H-pyrazolo[3,4-d]pyrimidin-5-amine 4, which was converted into hydrazino derivative 5 by heating with hydrazine hydrate at reflux. Hydrazino, as well as imino-amino derivatives, underwent condensation and cyclization reactions to give pyrazolo[ 3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[3,4-c]pyrimidine derivatives, respectively.

Method: Antimicrobial studies are performed using two-gram positive bacteria and two-gram negative bacteria.

Q-switched Nd: YAG laser alone or with modified Jessner chemical peeling for treatment of mixed melasma in dark skin types: A comparative clinical, histopathological, and immunohistochemical study.

Backgrounds: Treatment of mixed melasma remains challenging. Promising results have been achieved with low-fluence 1064-nm Q-switched Nd-YAG laser; however, multiple sessions are necessary with occurrence of complications especially in dark skin types. So, combination methods may be recommended.

Epithelial expression of cytokeratins 15 and 19 in vitiligo.

Background: Cytokeratins (CK) belong to the family of intermediate filament proteins, and among them specific epithelial keratins are considered markers for stem cells activation.

Objectives: This study aims to investigate the expression of CK15 and CK19 as possible stem cell markers in vitiligo during phototherapy.

Methods: The study was conducted on vitiligo patients receiving narrow-band ultraviolet therapy.