Metronidazole aryloxy, carboxy and azole derivatives: Synthesis, anti-tumor activity, QSAR, molecular docking and dynamics studies

Faghih-Mirzaei, Ehsan; Sabouri, Salehe; Zeidabadinejad, Leila; AbdolahRamazani, Salman; Abaszadeh, Mehdi; Khodadadi, Arash; Shamsadini-pour, M.; Jafari, Mandana; Pirhadi, Somayeh

doi:10.1016/j.bmc.2018.12.003

“…Trichomonas vaginitis, as a common gynecological disease, is the female vaginal infection on account of Trichomonas vaginalis, wherein clinical symptoms will appear such as mucosal redness, swelling, pruritus vulvae, and painful intercourse [1][2][3]. Unsafe sexual practices and long-term use of antibiotics are thought to be closely associated with the causative factors of this disease [4,5]. According to relevant data, there are 1.8 billion cases of trichomoniasis worldwide each year, most of which are among people with low immunity and poor lifestyle habits.…”

Section: Introductionmentioning

confidence: 99%

The Clinical Effects of Metronidazole Vaginal Effervescent Tablets Combined with Kushen Suppository in the Treatment of Trichomonas Vaginitis

Zhang

¹

,

Zeng

²

,

Li

³

et al. 2022

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

Objective. The aim of this study was to explore the clinical effects of metronidazole vaginal effervescent tablets combined with Kushen suppository in the treatment of Trichomonas vaginitis. Methods. Ninety patients with trichomoniasis admitted to our hospital from January 2019 to January 2020 were prospectively analyzed and randomly divided into a control group (n = 45) treated with metronidazole vaginal effervescent tablets and an experimental group (n = 45) treated with Kushen suppository on top of the control group using the random number table method. The clinical effects, inflammatory factors, and microcirculation indexes were compared. We assessed patient’s vaginal health by Vaginal Health Score Scale (VHS) before and after treatment and estimated their quality of life according to Generic Quality of Life Inventory-74 (GQOLI-74). A follow-up visit was conducted to compare patient’s recurrence 3 months after treatment. Results. Distinctly higher total clinical effective of the experimental group compared with that of the control group was obtained ( P < 0.05 ); the serum level of inflammatory factors of the experimental group was dramatically lower than that of the control group after treatment ( P < 0.001 ); the experimental group experienced a favorable microcirculation index in comparison with the control group ( P < 0.001 ); superior VHS ( P < 0.001 ) and GQOLI-74 ( P < 0.05 ) scores of the experimental group after treatment compared to those of the control group were observed; the recurrence rate of the experimental group 3 months after treatment was significantly decreased in comparison with that of the control group ( P < 0.05 ). Conclusion. Metronidazole vaginal effervescent tablets combined with Kushen suppository can effectively improve the clinical symptoms of patients with trichomonas vaginitis, abate patient’s inflammatory reaction, and raise their quality of life, which is worthy of promotion.

show abstract

“…17 The incorporation of 1H-1,2,3-triazolyl rings into the molecular framework is an attractive strategy, since they are readily recognized by target proteins such as enzymes or receptors in the cells. [18][19][20][21][22][23][24][25] Fish scales are inedible and are hence thrown away as industrial waste; also, the fish scales possess large amounts of hydroxyapatite (HA), which is utilized as a template for stabilizing the mineral phases. 26 HA is easily obtained from various natural resources, such as fish scale waste or bovine bone.…”

Section: Introductionmentioning

confidence: 99%

“…17 The incorporation of 1 H -1,2,3-triazolyl rings into the molecular framework is an attractive strategy, since they are readily recognized by target proteins such as enzymes or receptors in the cells. 18–25…”

Section: Introductionmentioning

confidence: 99%

Synthesis, biological evaluation andin silicostudies of 1,2,3-triazolyl-metronidazole derivatives againstLeishmania major

Ghanbariasad

¹

,

Emami

²

,

Zarenezhad

³

et al. 2022

View full text Add to dashboard Cite

show abstract

“…A particularly interesting imidazole-like compound is the metronidazole ( II , Figure 1 ). This molecule provides a broad spectrum of useful properties for the treatment of infections [ 33 , 34 ], inflammations [ 35 ] and cancer [ 36 ].…”

Section: Introductionmentioning

confidence: 99%

New Metallophthalocyanines Bearing 2-Methylimidazole Moieties—Potential Photosensitizers against Staphylococcus aureus

Wierzchowski

¹

,

Ziental

²

,

Łażewski

³

et al. 2022

IJMS

1

0

View full text Add to dashboard Cite

Newly developed tetra- and octasubstituted methimazole-phthalocyanine conjugates as potential photosensitizers have been obtained. Synthesized intermediates and final products were characterized by the MALD-TOF technique and various NMR techniques, including 2D methods. Single-crystal X-ray diffraction was used to determine the crystal structures of dinitriles. The studied phthalocyanines revealed two typical absorption bands—the Soret band and the Q band. The most intense fluorescence was observed for octasubstituted magnesium(II) phthalocyanine in DMF (ΦFL = 0.022). The best singlet oxygen generators were octasubstituted magnesium(II) and zinc(II) phthalocyanines (Φ∆ 0.56 and 0.81, respectively). The studied compounds presented quantum yields of photodegradation at the level between 10−5 and 10−6. Due to their low solubility in a water environment, the liposomal formulations were prepared. Within the studied group, octasubstituted zinc(II) phthalocyanine at the concentration of 100 µM activated with red light showed the highest antibacterial activity against S. aureus equal to a 5.68 log reduction of bacterial growth.

show abstract

Metronidazole aryloxy, carboxy and azole derivatives: Synthesis, anti-tumor activity, QSAR, molecular docking and dynamics studies

Cited by 9 publications

References 23 publications

The Clinical Effects of Metronidazole Vaginal Effervescent Tablets Combined with Kushen Suppository in the Treatment of Trichomonas Vaginitis

The Clinical Effects of Metronidazole Vaginal Effervescent Tablets Combined with Kushen Suppository in the Treatment of Trichomonas Vaginitis

Synthesis, biological evaluation andin silicostudies of 1,2,3-triazolyl-metronidazole derivatives againstLeishmania major

New Metallophthalocyanines Bearing 2-Methylimidazole Moieties—Potential Photosensitizers against Staphylococcus aureus

Contact Info

Product

Resources

About