Biological activity Study for some heterocyclic compounds and their impact on the gram positive and negative bacteria

Saleh, Sayran Sattar; AL-Salihi, Siham Sh.; Mohammed, Israa A.

doi:10.1016/j.egypro.2018.11.194

Cited by 28 publications

(14 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This compound was used as a comparison for a 1,3-benzodioxole ring and p-CF 3 moiety in the structure of compound 2. N and S heterocyclic compounds are well-known for their diverse biological activities and are used in several diseases treatments [26][27][28] . In our study, we synthesized such a compound using (trifluoromethyl)phenylboronic acid and 2,2′-dithiobis(benzothiazole) via S-S cleavage, resulting in a C-S bond with an N and S heterocyclic ring 10, with a 68% yield (Fig.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and initial screening of lactate dehydrogenase inhibitor activity of 1,3-benzodioxole derivatives

Annas

Cheon²,

Yusuf

et al. 2020

Sci Rep

View full text Add to dashboard Cite

Cancer is one of the main causes of mortality in the world. Many cancer cells produce ATP through high-level lactic acid fermentation catalyzed by lactate dehydrogenase (LDH), which converts pyruvic acid to lactic acid. LDH plays a dominant role in the Warburg effect, wherein aerobic glycolysis is favored over oxidative phosphorylation. Due to the high lactic acid production level in cancer cells, LDH-targeting could be a potential cancer treatment strategy. A few approaches, such as drug treatment, reportedly inhibited LDH activity. In this study, we describe new 1,3-benzodioxole derivatives that might be potential small molecule candidates for LDHA inhibition. The synthesis was carried out by trans-esterification between aryl ester and alcohol groups from piperonyl alcohol. Compounds 2 and 10 exhibited a selective LDHA IC50 value of 13.63 µM and 47.2 µM, respectively. Whereas only compound 10 showed significant cytotoxicity in several lines of cancer cells, especially in human pancreatic cancer PANC-1 cells. These synthesized compounds possess 2 aromatic rings and –CF3 moiety, which expectedly contributes to LDHA inhibition. The presented products have the potential to become a promising LDHA inhibitor drug candidate.

show abstract

Section: Resultsmentioning

confidence: 99%

Synthesis and initial screening of lactate dehydrogenase inhibitor activity of 1,3-benzodioxole derivatives

Annas

Cheon²,

Yusuf

et al. 2020

Sci Rep

View full text Add to dashboard Cite

show abstract

“…After the heating process was complete, the solution was concentrated under rarefied pressure, the remaining anhydride washed with cold methanol, and it was then dried and recrystallized from dioxane. The properties of compounds (6a-c), (7a-c) and (8a-c) shown in (Table 4) (Kelarav et al, 2003).…”

Section: Synthesis Of 13-oxazepine Compounds (6a-c) (7a-c) and (8a-c)mentioning

confidence: 99%

Synthesis, Characterization of Substituted 1,3-Oxazepine, Thiazolidine-4-one and Azetidine-2-one Using Benzimidazole as a Synthon

Muhammed¹

2023

RJS

View full text Add to dashboard Cite

Starting from benzimidazole moiety, several heterocyclic compounds (1,3-Oxazepine, thiazolidin-4one, azetidin-2-one) were synthesized, thus the Ethyl Benzimidazole acetate (1) was synthesized from the reaction of benzimidazole with ethylchloroacetate on treatment with hydrazine hydrate is giving the corresponding hydrazide (2). The reaction of this hydrazide with, 4-substituted acetophenone afforded hydrazones which on reaction with some reagents to produce synthesized compounds, (4a-c), (5a-c), (6a-c), (7a-c), (8a-c) and (9a-c). All the synthesized products were confirmed by physical and spectral methods.

show abstract

“…Several synthetic compounds (5-(3-chlorophenyl)-1-methyl-4-nitro-1 H-imidazole, synthesized inhibitors of the Hsp90 class, and many other compounds) have been reported to have potential chemotherapeutic properties against E. histolytica and G. intestinalis [8,27]. Thus, some of the compounds tested as alternatives to metronidazole have had encouraging results on intestinal tract parasites [15,28].…”

Section: Introductionmentioning

confidence: 99%

Pharmaceutical activity of a synthetic heterocyclic (C15H12N5OCl) compound on Entamoeba histolytica and Giardia lamblia

Obaid

Saleh

Boundenga

2023

Russian Journal of Infection and Immunity

View full text Add to dashboard Cite

Abstract: Background: Intestinal parasites are among the most important infectious agents with an impact on human health. Indeed, in the lack of an available treatment option, these parasites could constitute a real health problem in the population. Aim: In the present study, we investigated the effect of a synthetic heterocyclic compound on two intestinal parasites (Entamoeda histolytica and Gardia lamblia). Methods: The parasite isolates tested were collected from outpatients at the General Pediatric Hospital in Kirkuk, Iraq, between September 2019 and January 2020. Thus, we studied the in vivo and in vitro pharmaceutical activity of the ingredient on both parasites. The toxicological effects of the substance on some blood parameters and liver and kidney function tests were also studied. Results: After five days of treatment, the drug's in vivo action on G. lamblia resulted in an inhibition rate of 88.2 percent at a dose of 1 mg/kg. On the other hand, we observed that the influence of this synthetic substance on cultured E. histolytica was very close to the metronidazole effect. The maximum result was at a concentration of 1 g/ml and was obtained after 72 hours of incubation with an inhibition rate of 89.4%. The substance did not affect the blood parameters or the studied liver and kidney functions. Conclusion: It can be concluded that this substance is highly effective against both E. histolytica and G. lamblia, and that it has no toxic effects on the studied parameters. Therefore, it could be a promising pharmacophore for intestinal protozoan parasites including E. histolytica and G. lamblia and an alternative or competitor to the current medications available.

show abstract

Biological activity Study for some heterocyclic compounds and their impact on the gram positive and negative bacteria

Cited by 28 publications

References 18 publications

Synthesis and initial screening of lactate dehydrogenase inhibitor activity of 1,3-benzodioxole derivatives

Synthesis and initial screening of lactate dehydrogenase inhibitor activity of 1,3-benzodioxole derivatives

Synthesis, Characterization of Substituted 1,3-Oxazepine, Thiazolidine-4-one and Azetidine-2-one Using Benzimidazole as a Synthon

Pharmaceutical activity of a synthetic heterocyclic (C<sub>15</sub>H<sub>12</sub>N<sub>5</sub>OCl) compound on <i>Entamoeba histolytica</i> and <i>Giardia lamblia</i>

Contact Info

Product

Resources

About