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In an attempt to find novel, potent α-glucosidase inhibitors, a library of poly-substituted 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2- a ]pyrimidines 3a–ag have been synthesized through heating a mixture of 2-aminobenzimidazoles 1 and α -azidochalcone 2 under the mild conditions. This efficient, facile protocol has been resulted into the desirable compounds with a wide substrate scope in good to excellent yields. Afterwards, their inhibitory activities against yeast α-glucosidase enzyme were investigated. Showing IC 50 values ranging from 16.4 ± 0.36 µM to 297.0 ± 1.2 µM confirmed their excellent potency to inhibit α-glucosidase which encouraged us to perform further studies on α-glucosidase enzymes obtained from rat as a mammal source. Among various synthesized 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2- a ]pyrimidines, compound 3k exhibited the highest potency against both Saccharomyces cerevisiae α -glucosidase (IC 50  = 16.4 ± 0.36 μM) and rat small intestine α -glucosidase (IC 50  = 45.0 ± 8.2 μM). Moreover, the role of amine moiety on the observed activity was studied through substituting with chlorine and hydrogen resulted into a considerable deterioration on the inhibitory activity. Kinetic study and molecular docking study have confirmed the in-vitro results.

Fourteen novel 4,5-diphenyl-imidazol-1,2,3-triazole hybrids 8a–n were synthesized with good yields by performing click reaction between the 4,5-diphenyl-2-(prop-2-yn-1-ylthio)-1H-imidazole and various benzyl azides. The synthesized compounds 8a–n were evaluated against yeast α-glucosidase, and all these compounds exhibited excellent inhibitory activity (IC50 values in the range of 85.6 ± 0.4–231.4 ± 1.0 μM), even much more potent than standard drug acarbose (IC50 = 750.0 μM). Among them, 4,5-diphenyl-imidazol-1,2,3-triazoles possessing 2-chloro and 2-bromo-benzyl moieties (compounds 8g and 8i) demonstrated the most potent inhibitory activities toward α-glucosidase. The kinetic study of the compound 8g revealed that this compound inhibited α-glucosidase in a competitive mode. Furthermore, docking calculations of these compounds were performed to predict the interaction mode of the synthesized compounds in the active site of α-glucosidase.Graphic abstract A novel series of 4,5-diphenyl-imidazol-1,2,3-triazole hybrids 8a–n was synthesized with good yields by performing click reaction between the 4,5-diphenyl-2-(prop-2-yn-1-ylthio)-1Himidazole and various benzyl azides. The synthesized compounds 8a–n were evaluated against yeast α-glucosidase and all these compounds exhibited excellent inhibitory activity (IC50 values in the range of 85.6 ± 0.4-231.4 ± 1.0 μM), even much more potent than standard drug acarbose (IC50 = 750.0 μM).

In this study, a novel series of mercapto-phenyl-1,2,4-triazole-bearing thio-quinoline moieties was designed, synthesized, and evaluated for their anti-tyrosinase activities. All compounds were tested for inhibitory activity against tyrosinase, compound 12j was found to be the most potent with IC 50  = 10.49 ± 1.02 µM. Structure–activity relationship (SAR) analysis indicated that the introduction of electron-donating and electron-withdrawing groups at specific positions influenced the inhibitory efficacy. The antioxidant activity of all derivatives were also performed, and 12j showed IC 50  = 102.36 ± 3.33 µM. In silico molecular docking studies showed that compound 12j had the strongest binding affinity (binding energy = − 8.04 kcal/mol) and formed stable hydrogen bonds with key active site residues (e.g., His85, His259, and His296) of tyrosinase. Molecular dynamics simulations have further exhibited the high stability and compactness of the 12j –tyrosinase complex, with minimum RMSD fluctuations and stable hydrogen bonding patterns. These results suggest the potency of these derivatives as promising tyrosinase inhibitors with useful information into their mechanism, establishing a foundation for future therapeutic applications in hyperpigmentation and related disorders.

Berberine (Ber) as a natural isoquinoline alkaloid, with a wide range of biological activities, mainly suffers from low bioavailability, decreasing its therapeutic efficacy. In this study, two novel conjugates of Ber with self-assembly property, Ber–polyethylene glycol (B–PEG) and Ber–diethylene glycol monomethyl ether (B–DG), were synthesized to investigate the effect of the anchoring part on the CMC, morphology as well as antioxidant and neuroprotective properties of the nanomicelles. The CMC increased from 1.2 μmol in B–DG to 3.0 μmol in B–PEG, measured by pendant drop. The anchored part affected greatly the shape and CMC of the self-assembled nanomicelles. A mixture of semi-spherical and cubic nanomicelles in the average hydrodynamic size of 93 nm was achieved for B–PEG, while B–DG nanomicelles were just in semispherical morphology with the hydrodynamic size of 64 nm. The antioxidant property of the nanomicelles was studied by DPPH scavenging and ferric reducing antioxidant power assays, exhibiting improved antioxidant activity of B–PEG and B–DG conjugates compared to free Ber. The neuroprotection potency of Ber was improved significantly after conjugation compared to free Ber against H 2 O 2 -induced cell death and B–PEG showed activity as level as that of the standard drug, Quercetin. Owing to the self-assembly property and interesting biological activities of the introduced amphiphilic Ber–PEG conjugate, we propose application of this nanomicelle alone, or as a promising bioactive carrier of the poorly water-soluble drugs, against neurodegenerative diseases.

A novel approach to design and synthesis a pH-responsive nanocarrier for targeted drug delivery (TDD) is developed. The synthesized Zn-HKUST-1 metal–organic frameworks (MOFs) was calcined at 500 °C as an optimum temperature to synthesize highly pure and hexagonal crystalline mesoporous ZnO nanoparticles (m-ZnO NPs) having high surface area of ZnO (137 m 2 /g) larger than many reported porous ZnO nanostructures, characterized by PXRD, FT-IR, UV–Vis, FE-SEM and, BET methods. The rice-seed-like m-ZnO NPs were decorated by polyethylene glycol (PEG) and loaded with doxorubicin (DOX). The nanocomposite thus obtained was evaluated for doxorubicin TDD in a simulated tumor microenvironment (TMU), which showed the release of ~ 48% of DOX at a pH of 5.4 after 72 h. The effect of biocompatible nanocomposite on breast cancer cell lines (MCF-7) was evaluated which showed that the use of DOX loaded m-ZnO decorated PEG nanocomposite has a good drug performance. Mesoporous ZnO nanoparticle with mean diameter of 30 nm and very high surface area of 137 m 2 /g is synthesized and loaded by PEG and DOX for efficient drug delivery.

A facile and efficient synthetic procedure for effecting the pinacol rearrangement catalyzed by AlCl3 in the absence of solvent is developed. The rearrangement product is obtained at room temperature in a few minutes and in almost quantitative yield. Benzylic pinacols rearrange under these conditions, while aliphatic pinacols do not react.

Pd(II) catalyzed the exchange reaction of vinyl acetate with aromatic acids to produce the corresponding vinyl esters in good yields.

In an attempt to find novel, potent α-glucosidase inhibitors, a library of poly-substituted 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines 3a-ag have been synthesized through heating a mixture of 2-aminobenzimidazoles 1 and α-azidochalcone 2 under the mild conditions. This efficient, facile protocol has been resulted into the desirable compounds with a wide substrate scope in good to excellent yields. Afterwards, their inhibitory activities against yeast α-glucosidase enzyme were investigated. Showing IC50 values ranging from 16.4 ± 0.36 µM to 297.0 ± 1.2 µM confirmed their excellent potency to inhibit α-glucosidase which encouraged us to perform further studies on α-glucosidase enzymes obtained from rat as a mammal source. Among various synthesized 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines, compound 3k exhibited the highest potency against both Saccharomyces cerevisiae α-glucosidase (IC50 = 16.4 ± 0.36 μM) and rat small intestine α-glucosidase (IC50 = 45.0 ± 8.2 μM). Moreover, the role of amine moiety on the observed activity was studied through substituting with chlorine and hydrogen resulted into a considerable deterioration on the inhibitory activity. Kinetic study and molecular docking study have confirmed the in-vitro results.In an attempt to find novel, potent α-glucosidase inhibitors, a library of poly-substituted 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines 3a-ag have been synthesized through heating a mixture of 2-aminobenzimidazoles 1 and α-azidochalcone 2 under the mild conditions. This efficient, facile protocol has been resulted into the desirable compounds with a wide substrate scope in good to excellent yields. Afterwards, their inhibitory activities against yeast α-glucosidase enzyme were investigated. Showing IC50 values ranging from 16.4 ± 0.36 µM to 297.0 ± 1.2 µM confirmed their excellent potency to inhibit α-glucosidase which encouraged us to perform further studies on α-glucosidase enzymes obtained from rat as a mammal source. Among various synthesized 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines, compound 3k exhibited the highest potency against both Saccharomyces cerevisiae α-glucosidase (IC50 = 16.4 ± 0.36 μM) and rat small intestine α-glucosidase (IC50 = 45.0 ± 8.2 μM). Moreover, the role of amine moiety on the observed activity was studied through substituting with chlorine and hydrogen resulted into a considerable deterioration on the inhibitory activity. Kinetic study and molecular docking study have confirmed the in-vitro results.

An improved selective ipso-nitration of the tripropoxy derivative of tertbutylcalix[4]arene at the upper rim is described. The synthesized products are key intermediates for construction of molecular receptors based on calixarenes.

A novel series of 1,2,3-triazolo-benzodiazepine derivatives 6a–o has been synthesized and evaluated in vivo for their anticonvulsant activities using by pentylenetetrazole (PTZ)- and maximal electroshock (MES)-induced seizures in mice. The synthetic approach started with diazotizing 2-aminobenzoic acids 1 to produce 2-azidobenzoic acids 2. Next, reaction of the latter compounds with propargylamine 3, benzaldehyde 4, and isocyanides 5 led to the formation of the title compounds 6a–o, in good yields. All the synthesized compounds exhibited high anticonvulsant activity in the PTZ test, comparable to or better than the standard drug diazepam. Among the tested compounds, N-(tert-butyl)-2-(9-chloro-6-oxo-4H-[1,2,3]triazolo[1,5-a][1,4]benzodiazepin-5(6H)-yl)-2-(3-bromophenyl)acetamide 6h was the most potent compound in this assay. Moreover, compounds 6i and 6k showed excellent activity in MES test. Loss of the anticonvulsant effect of compound 6h in the presence of flumazenil in the PTZ test and appropriate interaction of this compound in the active site of benzodiazepine (BZD)-binding site of GABAA receptor confirm involvement of BZD receptors in the anticonvulsant activity of compound 6h.A novel series of 1,2,3-triazolo-benzodiazepine derivatives 6a–o have been synthesized and evaluated in vivo for their anticonvulsant activities using by pentylenetetrazole (PTZ)- and maximal electroshock (MES)-induced seizures in mice. All the synthesized compounds exhibited high anticonvulsant activity, comparable to or better than the standard drug diazepam in the PTZ test and compounds 6i and 6k showed excellent activity in MES test. Flumazenil test and in silico docking study confirm involvement of benzodiazepine receptors in the anticonvulsant activity of these compounds.