Azole antimicrobial pharmacophore-based tetrazoles: Synthesis and biological evaluation as potential antimicrobial and anticonvulsant agents

Rostom, Sherif A. F.; Ashour, Hayam M. A.; Razik, Heba A. Abd El; Fattah, Abd El Fattah H. Abd El; El-Din, Nagwa N.

doi:10.1016/j.bmc.2009.02.004

Cited by 127 publications

(50 citation statements)

References 40 publications

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“…Data collection: APEX2 (Bruker, 2005); cell refinement: SAINT (Bruker, 2005); data reduction: SAINT; program(s) used to solve structure: SHELXS97 (Sheldrick, 2008); program(s) used to refine structure: SHELXL97 (Sheldrick, 2008); molecular graphics: PLATON (Spek, 2009) and ORTEP-3 for Windows (Farrugia, 1997); software used to prepare material for publication: publCIF (Westrip, 2010). Tetrazoles derivatives are an important class of compounds, which can be used in the fields of bioorganic and medicinal chemistry as antibacterials, anti-cancer, heart disease, neurodegenerative disease, and antifungal activity (Smissman et al,1976;McGuire et al, 1990;Lunn et al, 1992;Itoh et al, 1995;Upadhayaya et al, 2004;Wu et al, 2008;Rostom et al, 2009. The tetrazole moiety has long been established as a bioisostere of a carboxyl unit (Burger, 1991). A major advantage of tetrazoles over carboxylic acids is that they are resistant to many biological metabolic degradation pathways (Singh et al, 1980).…”

Section: Methodsmentioning

confidence: 99%

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N-(Cyanomethyl)benzamide

et al. 2010

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Key indicators: single-crystal X-ray study; T = 296 K, P = 0.0 kPa; mean (C-C) = 0.002 Å; R factor = 0.038; wR factor = 0.109; data-to-parameter ratio = 13.6.In the structure of the title compound, C 9 H 8 N 2 O, the amide group is twisted by a dihedral angle of 21.86 (7) with respect to the benzene ring, while the planes of the benzene ring and cyanomethyl group form a dihedral angle of 53.13 (11) . In the crystal structure, molecules are linked via N-HÁ Á ÁO hydrogen bonds, forming a chain running parallel to the a axis. Related literature ExperimentalCrystal data Data collectionBruker X8 APEXII CCD areadetector diffractometer 11132 measured reflections 1920 independent reflections 1433 reflections with I > 2 (I) R int = 0.027

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Section: Methodsmentioning

confidence: 99%

“…For the biological activity and medicinal properties of tetrazole derivatives, see : Smissman et al (1976); McGuire et al (1990); Lunn et al (1992); Itoh et al (1995); Upadhayaya et al (2004); Wu et al (2008); Rostom et al (2009);Burger (1991); Singh et al (1980). For the synthetic procedure, see: Adams & Langley (1941a,b).…”

Section: Related Literaturementioning

confidence: 99%

N-(Cyanomethyl)benzamide

et al. 2010

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“…The results revealed that five compounds 17,18 were able to display noticeable anticonvulsant activity in both tests at 100 mg/kg dose level [6] (Figure 6). …”

Section: Hybridsmentioning

confidence: 96%

Latest Update on Pharmacological Activities of 1,3,4-Oxadiazole Derivatives

Kumar¹,

Kumar²

2016

J Cell Sci Ther

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Heterocyclic compounds have been an interesting area for the study of synthesis and biological activity of novel oxadiazole derivatives for a long time. Heterocyclic compounds possess diverse biological properties that have led to intense study and research of these compounds. One of these compounds 1,3,4-Oxadiazole is a versatile heterocyclic nucleus is a novel molecule which attract the medicinal chemist to search a new therapeutic molecule. 1,3,4-oxadizole exhibited a wide range of biological activities which includes antimicrobial activity, anti-tubercular, anticonvulsant, antidiabetic, anti-allergic, enzyme inhibitors, anti-HIV activity, antipyretic activity, Immunosuppressive activity, Spasmolytic Activity, antioxidant activity, Anti-Alzheimer's activity cardiovascular acivity, anti-inflammatory, anti-tumor activity, insecticidal activity, CGRP receptor antagonists, anti-anthelmintic activities. Results of various derivatives of different oxadiazole and their substitutions with diverse biological activities are reviewed in present article.

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“…Therefore, in continuation of our ongoing interest in the synthesis novel heterocycles with chemotherapeutic activities [21][22][23][24][25][26][27][28][29][30] , it was considered of interest to prepare some new tetrahydro-and hexahydroindazole derivatives, bearing functionalities that are reported to contribute to potential chemotherapeutic activities such as the sulfonamide, sulfonylurea and thiourea groups. Besides incorporating an electron withdrawing group at position-3 we have also introduced a methyl substituent in position-7.…”

Section: Research Articlementioning

confidence: 99%