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Mohamed F. El Shehry

Bio: Mohamed F. El Shehry is an academic researcher. The author has contributed to research in topics: Pyrazole & Thiazole. The author has an hindex of 5, co-authored 5 publications receiving 131 citations.

Papers
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Journal ArticleDOI
TL;DR: The synthesized quinoline derivatives bearing pyrazole moiety are interesting scaffolds for the development of novel antibacterial and antifungal agents according to the tested strains of bacteria and fungi.

133 citations

Journal ArticleDOI
TL;DR: One of the best ways to design new biocidal agents is synthesizing hybrid molecules by combining two or more bioactive moieties in a single molecular scaffold, so quinolines bearing a thiazole moiety can be suggested as interesting scaffolds for the development both of the novel antibacterial and antifungal agents.

57 citations

Journal ArticleDOI
TL;DR: In this article, a series of novel pyrazoles containing benzofuran and trifluoromethyl moieties were synthesized via two routes starting from 5-(3-(trifluorsyl)phenyl azo) salicylaldehyde.
Abstract: Abstract Searching for new anti-inflammatory and analgesic agents, we have prepared a series of novel pyrazoles containing benzofuran and trifluoromethyl moieties. The pyrazole derivatives have been synthesized via two routes starting from 5-(3-(trifluoromethyl)phenyl azo) salicylaldehyde. The first route involved the synthesis of 2-acetylbenzofuran and then treatment with aldehydes to afford the corresponding chalcones. The cyclization of the latter chalcones with hydrazine hydrate led to the formation of new pyrazoline derivatives. The second route involved the synthesis of benzofuran-2-carbohydrazide and then treatment with formylpyrazoles, chalcones and ketene dithioacetal derivatives to afford the corresponding pyrazole derivatives. Some of the synthesized compounds exhibited anti-inflammatory and analgesic activities.

21 citations

Journal ArticleDOI
TL;DR: It is suggested that quinaxoline derivatives bearing a pyrazole moiety are interesting scaffolds for the development of novel antibacterial and antifungal agents.
Abstract: Novel series of quinaxoline derivatives incorporating N-propionic and O-propionic hydrazide moieties were synthesized. Alkylation of 3-methylquinoxalin-2(1H)-one with ethyl 2-bromopropanoate afforded a mixture of O-alkylated and N-alkylated 3-methylquinoxaline. Hydrazide derivatives were afforded by reaction of O-alkylated and N-alkylated 3-methylquinoxaline with hydrazine hydrate. Condensation of hydrazide derivatives with different aromatic aldehydes and formylpyrazoles afforded the corresponding hydrazone derivatives. The synthesized quinaxoline derivatives were evaluated for their expected antimicrobial activity; where, the majority of these compounds showed potent antibacterial and antifungal activities against the tested strains of bacteria and fungi. Hydrazone derivative which contain 3-p-tolyl-pyrazolyl moiety showed fourfold potency of amphotericin B in inhibiting the growth of Aspergillus fumigatus, twofold potency of gentamycin in inhibiting the growth of Neisseria gonorrhoeae, equipotent potency of ampicillin in inhibiting the growth of Streptococcus pyogenes, equipotent potency of gentamycin in inhibiting the growth of Proteus vulgaris and Shigella flexneri, equipotent potency of amphotericin B in inhibiting the growth of Aspergillus clavatus, Geotrichum candidum and Penicillium marneffei. Thus, these studies suggested that quinaxoline derivatives bearing a pyrazole moiety are interesting scaffolds for the development of novel antibacterial and antifungal agents.

14 citations

Journal ArticleDOI
TL;DR: Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives showed a significant decrease of the elevated glucose in comparison with the anti‐diabetic standard drug, metformin.
Abstract: New 1-arylamidebiguanide hydrochloride salts were synthesized via reaction of hydrazide derivatives with dicyandiamide in acidic medium. The structure of the obtained derivatives was characterized by spectroscopic and elemental analysis tools. The anti-diabetic properties of the synthesized compounds were determined. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives showed a significant decrease of the elevated glucose in comparison with the anti-diabetic standard drug, metformin. The effects of the synthesized biguanide derivatives on the diabetic properties regarding liver function enzyme activities (AST, ALT, and ALP), lipid profiles (TC, TG, and TL), lipid peroxide, and nitrous oxide as well as histopathological characteristics were investigated and discussed.

7 citations


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Journal ArticleDOI
TL;DR: The different synthesis methods and the pharmacological properties of pyrazole derivatives developed by many scientists around the globe are highlighted.
Abstract: Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

520 citations

Journal ArticleDOI
TL;DR: A review of quinoline-based marketed drugs can be found in this paper, where the authors provide information about the biological activities of these drugs, such as antibacterial, antifungal, antimycobacterial, antiviral, antimalarial, anticancer, cardiovascular, CNS effects, antioxidant, anticonvulsant, analgesic, anti-inflammatory, anthelmintic and miscellaneous activities.

161 citations

Journal ArticleDOI
TL;DR: A comprehensive review of recent studies on the various aspects of benzofuran derivatives including their important natural product sources, biological activities and drug prospects, and chemical synthesis, as well as the relationship between the bioactivities and structures can be found in this paper.
Abstract: Benzofuran compounds are a class of compounds that are ubiquitous in nature. Numerous studies have shown that most benzofuran compounds have strong biological activities such as anti-tumor, antibacterial, anti-oxidative, and anti-viral activities. Owing to these biological activities and potential applications in many aspects, benzofuran compounds have attracted more and more attention of chemical and pharmaceutical researchers worldwide, making these substances potential natural drug lead compounds. For example, the recently discovered novel macrocyclic benzofuran compound has anti-hepatitis C virus activity and is expected to be an effective therapeutic drug for hepatitis C disease; novel scaffold compounds of benzothiophene and benzofuran have been developed and utilized as anticancer agents. Novel methods for constructing benzofuran rings have been discovered in recent years. A complex benzofuran derivative is constructed by a unique free radical cyclization cascade, which is an excellent method for the synthesis of a series of difficult-to-prepare polycyclic benzofuran compounds. Another benzofuran ring constructed by proton quantum tunneling has not only fewer side reactions, but also high yield, which is conducive to the construction of complex benzofuran ring systems. This review summarizes the recent studies on the various aspects of benzofuran derivatives including their important natural product sources, biological activities and drug prospects, and chemical synthesis, as well as the relationship between the bioactivities and structures.

119 citations

Journal ArticleDOI
TL;DR: Various selected quinolines and derivatives with potential biological and pharmaceutical activities will be presented and synthesis protocols used up to now for the construction of the principal quinoline scaffold are highlighted.
Abstract: Recently, quinoline has become an essential heterocyclic compound due to its versatile applications in the fields of industrial and synthetic organic chemistry. It is a vital scaffold for leads in drug discovery and plays a major role in the field of medicinal chemistry. Nowadays there are plenty of articles reporting syntheses of the main scaffold and its functionalization for biological and pharmaceutical activities. So far, a wide range of synthesis protocols have been reported in the literature for the construction of this scaffold. For example, Gould–Jacob, Friedlander, Pfitzinger, Skraup, Doebner–von Miller and Conrad–Limpach are well-known classical synthesis protocols used up to now for the construction of the principal quinoline scaffold. Transition metal catalysed reactions, metal-free ionic liquid mediated reactions, ultrasound irradiation reactions and green reaction protocols are also useful for the construction and functionalization of this compound. The main part of this review focuses on and highlights the above-mentioned synthesis procedures and findings to tackle the drawbacks of the syntheses and side effects on the environment. Furthermore, various selected quinolines and derivatives with potential biological and pharmaceutical activities will be presented.

105 citations

Journal ArticleDOI
TL;DR: Molecular docking studies were conducted to investigate the binding mode, amino acid interactions and free binding energy of these potent derivatives, and compounds 4b, 7a and 9 showed more potent activity against EGFR than Lapatinib.

72 citations