Synthesis, antimicrobial and antiviral evaluation of certain thienopyrimidine derivatives

El‐Sherbeny, Magda A.; El‐Ashmawy, Mahmoud B.; El‐Subbagh, Hussein I.; El-Emam, Ali A.; Badria, F. A.

doi:10.1016/0223-5234(96)88255-9

Cited by 68 publications

(40 citation statements)

References 11 publications

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“…[20][21][22] Aphidicolin was used as a positive control. From the results obtained in Table 1, we can conclude that, compounds 1,2,4-triazole-5(4H)-thione 4, 2-thioxothiazole 6, thiazoles 8a, b and thiazolidin-4-one 13 showed no antiviral activity.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and Antiviral Activity of New Indole-Based Heterocycles

Abdel‐Gawad

Mohamed

Dawood

et al. 2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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Section: Resultsmentioning

confidence: 99%

Synthesis and Antiviral Activity of New Indole-Based Heterocycles

Abdel‐Gawad

Mohamed

Dawood

et al. 2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Yield 85%, mp: 115-118 ℃. 1 mmol) and morpholine(0.85 mL) were dissolved in ethanol(15 mL) and refluxed to give the desired compound (5). After the reaction completed, the product was extracted with dichloromethane(DCM) and water, the extract was washed successively with water, dried over anhydrous Na 2 SO 4 , filtered and evaporated, then to give 4-(thieno [3,2- …”

Section: Synthesis Of Compoundsmentioning

confidence: 99%

“…In addition, the research team occasionally find that the thienopyrimidine analogues didn't IKKb inhibitory activities, nevertheless it's has a effective on acute myeloid leukemia [3]. At the same times, many articles have repoted that thienopyrimidine derivatives have a antimicrobial activity [4][5][6]. One of the literature points out some 2-substituted thienopirimidin-4-one derivatives may serve as novel spasmolytic agents to treat disorders of smooth muscle function.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 4- (Thieno [3, 2-d] pyrimidin-4-yl) Morpholine

Lei¹,

Wang²,

Xiong³

et al. 2017

Proceedings of the 2016 7th International Conference on Education, Management, Computer and Medicine (EMCM 2016)

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Abstract. pyrimidin-4-yl)morpholine derivatives is an important intermediate which inhibited tumor necrosis factor alpha and nitric oxide. In this work, a rapid and green synthetic method for compound (5) was established. The compound (5) was synthesized from the commercially available methyl 3-aminothiophene-2-carboxylate and formamidine acetate through three steps including condensation reaction, chlorination, and nucleophilic substitution. The structure was confirmed by 1 H NMR and MS. Furthermore, the total yield of the three steps was 43%.

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“…The thiophene ring system is notably a structural component of the commercial imidazole antifungal agent sertaconazole [11]. In addition, the antimicrobial profile of condensed thiophenes, particularly their thieno [2,3-d]pyrimidin-4-one analogues, is also well categorized in the literature [12][13][14].…”

Section: Introductionmentioning

confidence: 99%

Regioselective synthesis and biological evaluation of some novel thiophene-containing heterocyclic scaffolds as potential chemotherapeutic agents

Gaber

Bagley

2011

Eur. J. Chem.

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KEYWORDSIn the reaction of 2-amino-3-carbethoxythiophene derivative 2b with hydrazine hydrate the respective aminocarbohydrazide 3 was isolated. Treatment of the latter product with carbon disulfide in alkaline medium caused a heterocyclization to give 1,3,4-oxadiazole-2-thione 5 rather than 3-amino-2-thioxothieno[2,3-d]pyrimidin-4-one 4, which could be obtained on treatment of carbohydrazide 3 with thiourea. The structure of products 4 and 5 was proved by spectroscopic methods and chemical transformations. Derivatization led to two novel series of condensed and uncondensed thiophenes, which were of significant interest for biological study. Since compound 4 contains two adjacent reactive functional groups, it reacted readily with different electrophilic reagents to provide a series of thieno[2,3-d]pyrimidin-4-one derivatives with annelated bridgehead nitrogen heterocycles 8-11, whereas a second series of 3-heteroaryl-substituted thiophenes 13-17 was obtained by thioamide functionalization in 1,3,4-oxadiazole derivative 5 using various chemical reagents. The new thiophene-based derivatives were evaluated for their preliminary antimicrobial activity against a representative panel of Gram-positive and Gram-negative bacteria as well as fungi strains. The compounds tested displayed different levels of inhibitory effects, with the assays carried out on two pathogenic bacteria and two pathogenic fungi. Of these compounds, the monocyclic aminothiophene derivative 15 showed the highest effect on pathogenic bacteria, while the tricyclic condensed thiophene derivative 8 was observed to have the same inhibitory effect against pathogenic mould (Aspergillus flavus) as the reference drug Amphotericin B. For those derivatives belonging to first series of condensed thiophenes with annelated bridgehead nitrogen heterocycles, it has been observed that the antibacterial effect was in general found to be significantly higher than the corresponding uncondensed analogues. Although most of the condensed and uncondensed thiophenes under investigation showed generally remarkable in vitro antibacterial activity, unfortunately, no significant antifungal activity was observed with any of the compounds tested except for 8. Surprisingly, compound 8 displayed an excellent effect on fungus (A. flavus) on the one hand, whereas the lowest effect on bacteria on the other. The attachment of a triazolothiadiazine moiety to a thiophene ring could be considered as a promising strategy for the development of new therapeutic antibacterial agents related to the aminothiophene system. Thienopyrimidinone Cyclocondensation Cyclodesulfurization Hydrazinolysis Alkylation Antimicrobial activity

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Synthesis, antimicrobial and antiviral evaluation of certain thienopyrimidine derivatives

Cited by 68 publications

References 11 publications

Synthesis and Antiviral Activity of New Indole-Based Heterocycles

Synthesis and Antiviral Activity of New Indole-Based Heterocycles

Synthesis of 4- (Thieno [3, 2-d] pyrimidin-4-yl) Morpholine

Regioselective synthesis and biological evaluation of some novel thiophene-containing heterocyclic scaffolds as potential chemotherapeutic agents

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