Clean Grinding Technique: A Facile Synthesis and In Silico Antiviral Activity of Hydrazones, Pyrazoles, and Pyrazines Bearing Thiazole Moiety against SARS-CoV-2 Main Protease (Mpro)

Abu‐Melha, Sraa; Edrees, Mastoura M.; Riyadh, Sayed M.; Abdelaziz, Mohamad R.; Elfiky, Abdo A.; Gomha, Sobhi M.

doi:10.3390/molecules25194565

Cited by 69 publications

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References 44 publications

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“…The high medicinal significance of this scaffold has attracted considerable attention from many researchers and encouraged the design and synthesis of numerous thiazole- and bisthiazole-containing compounds with diverse pharmacological activities, such as antibacterial [ 6 ], antifungal [ 7 ], antiprotozoal [ 8 ], antiviral [ 9 , 10 ], anticancer [ 11 ], anti-inflammatory [ 12 , 13 , 14 , 15 , 16 ], antioxidant [ 17 ], analgesic [ 18 ], anticonvulsant [ 19 ], antidiabetic [ 20 ], and antihypertensive [ 21 ] activities. Furthermore, thiazole compounds exhibiting a promising biological potential for the treatment of Alzheimer’s disease [ 22 , 23 ] and metabolic syndrome [ 24 ] have been reported in the scientific literature.…”

Section: Introductionmentioning

confidence: 99%

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

et al. 2021

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Thiazole, a five-membered heteroaromatic ring, is an important scaffold of a large number of synthetic compounds. Its diverse pharmacological activity is reflected in many clinically approved thiazole-containing molecules, with an extensive range of biological activities, such as antibacterial, antifungal, antiviral, antihelmintic, antitumor, and anti-inflammatory effects. Due to its significance in the field of medicinal chemistry, numerous biologically active thiazole and bisthiazole derivatives have been reported in the scientific literature. The current review provides an overview of different methods for the synthesis of thiazole and bisthiazole derivatives and describes various compounds bearing a thiazole and bisthiazole moiety possessing antibacterial, antifungal, antiprotozoal, and antitumor activity, encouraging further research on the discovery of thiazole-containing drugs.

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Section: Introductionmentioning

confidence: 99%

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

et al. 2021

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“…Schiff base and hydrazone derivatives are well known as valuable intermediates in the synthesis of many organic compounds that are used in a multitude of applications [ 49 , 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 ]. A series of new laterally methoxy Schiff base derivatives A n were prepared according to the following Scheme 2 :…”

Section: Methodsmentioning

confidence: 99%

Optical and Thermal Investigations of New Schiff Base/Ester Systems in Pure and Mixed States

et al. 2021

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New mesomorphic series, 4-hexadecyloxy phenyl-imino-4′-(3-methoxyphenyl)-4″-alkoxybenzoates (An), were prepared and investigated with different thermal and mesomorphic techniques. The synthesized homologous series constitutes four members that differ from each other in the terminal length of flexible chain (n) attached to phenyl ester moiety, which varies between n = 6, 8, 10, and 12 carbons. A lateral CH3O group is attached to the central benzene ring in the meta position with respect to the ester moiety. Molecular structures of all newly prepared homologues were elucidated via FT-IR, 1H and 13C NMR spectroscopy. Mesomorphic and thermal properties were examined by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and the mesophases identified by polarized optical microscopy (POM). DSC and POM examinations revealed that all members of the present series (An) exhibit a purely enantiotropic nematic (N) phase. Comparative evaluations and binary phase diagrams were established between the present homologues and their corresponding shorter one (Bn). The examination revealed that, the length of the flexible alkoxy chain incorporated into the phenylimino moiety is highly effective on the temperature range and stability of the mesophase observed. With respect to the binary mixtures An/Bn, the exhibited N phase showed to cover the whole composition range with eutectic behavior.

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“…Schiff base and hydrazone derivatives are well known as valuable intermediates in synthesis of many organic compounds that exhibit many applications [39][40][41][42][43][44][45][46]. A series of new laterally methoxy Schiff base derivatives, with different terminal polar compact groups (X), namely, 4-(((4-(hexyloxy)phenyl)imino)methyl)-3-methoxyphenyl 4-substituted benzoates I6 a-e , have been prepared as shown in Scheme 1.…”

Section: Molecular Confirmation Of Synthesized Compounds I6 A-ementioning

confidence: 99%

Synthesis, Optical Characterizations and Solar Energy Applications of New Schiff Base Materials

et al. 2021

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A new set of laterally OCH3-substituted photoactive liquid crystalline analogues, 4-hexyloxy phenyl- imino-4ʹ-(3-methoxyphenyl)-4ʹ’-alkoxybenzoates, were synthesized and investigated for their mesomorphic behavior. The prepared set constitutes five analogues that differ from each other by the terminally attached compact polar group. Characterization of the synthesized derivatives is conducted using differential scanning calorimetry (DSC), polarized optical microscopy (POM), and UV-spectroscopy. Molecular structures were elucidated by elemental analyses, FT-IR and NMR spectroscopy. DSC and POM investigations indicated that all the prepared derivatives are monomorphic possessing the nematic (N) phase, except for the unsubstituted derivative that is nonmesomorphic. On the other side, the photophysical study and the optical spectra measurements confirm the photoactivity of the present compounds under UV/visible irradiation. The measured optical spectra showed impressive enhancement in the optical absorption and reduction in the optical bandgap from 3.63 to 3.0 eV depending on the terminal group. From the study of the DC electric properties, the lowest resistance, 106.5 GΩ at scan rate 0.1 V/s, was observed for the I6d film with Cl terminal, which decreased to 49.5 GΩ by increasing the scan rate to 0.5 V/s. Moreover, the electrical conductance is decreased from 9.39 pS to 1.35 pS at scan rate 0.1 V/s by changing the terminal group from Cl to F. The enhanced optical absorption and the reduced energy gap make the optimized samples suitable material for solar energy applications.

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Clean Grinding Technique: A Facile Synthesis and In Silico Antiviral Activity of Hydrazones, Pyrazoles, and Pyrazines Bearing Thiazole Moiety against SARS-CoV-2 Main Protease (Mpro)

Cited by 69 publications

References 44 publications

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

Optical and Thermal Investigations of New Schiff Base/Ester Systems in Pure and Mixed States

Synthesis, Optical Characterizations and Solar Energy Applications of New Schiff Base Materials

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