nan Zabiulla

Piperazine and morpholine:Synthetic preview and pharmaceutical applications

This review summarizes the in vitro and in vivo medicinal chemistry investigations for piperazine and morpholine analogues. Piperazine and morpholine nucleus show a broad spectrum of pharmaceutical applications, thus, in recent years scientists has developed various new methods for the synthesis of their derivatives. This review shows current tendency in the piperazine and morpholine analogues synthesis and reveals their potent pharmacophoric activities.

Design and synthesis of diamide-coupled benzophenones as potential anticancer agents

A series of diamide-coupled benzophenone, 2-(4-benzoyl-phenoxy)-N-{2-[2-(4-benzoyl-phenoxy)-acetylamino]-phenyl}-acetamide analogues (9a-l) were synthesized by multistep reactions and all compounds were well characterized. Among the series (9a-l), compound 9k with three methyl groups at ortho position in rings A, B, and D and bromo group at the para position in ring E was selected as a lead compound by screening through multiple cancer cell types by in-vitro cytotoxic and antiproliferative assay systems. Also, the cytotoxic nature of the compound 9k resulted the regression of the tumor growth in-vivo, which could be due to decreased vascularisation in the peritoneum lining of the mice which regress the tumor growth. The results were reconfirmed in-vivo chorioallantoic membrane model which indicates a scope of developing 9k into potent anticancer drug in near future.

The anti-invasive role of novel synthesized pyridazine hydrazide appended phenoxy acetic acid against neoplastic development targeting matrix metallo proteases

Neoplastic metastasis is a major process where tumor cells migrate from the primary tumor and colonize at other parts of our body to form secondary tumor. Cancer incidences are rising and novel anti-neoplastic compounds with new mechanism of actions are essential for preventing cancer related deaths. In the current examination, a novel series of pyridazine analogues 6a-l was synthesized and evaluated against metastatic neoplastic cells. Experimental data postulated compound 6j has potential cytotoxic efficacy with prolonged activity against various cancer cells, including A549, HepG2, A498, CaSki and SiHa cells. Moreover, compound 6j arrests the A549 migration and invasions markedly by counteracting matrix metalloproteinase (MMP)-2 and MMP-9 expressions. Also, compound 6j proved its potentiality against Daltons solid lymphoma progression in-vivo by abridging MVD and MMP expressions. Compound 6j interacts with MMP-2 and MMP-9 by H- bond in-silico, thereby down regulates the MMPs action in tumourigenesis. Altogether, we concluded that compound 6j down regulates MMP-2 and MMP-9 and thereby impairs metastatic cancer cell migration and invasions which can be translated into a potent anti-neoplastic agent.

Statistical Analysis of Antimicrobial Data of 2-[2-(Aroyl)aroyloxy]methyl-1,3,4 Oxadiazoles analogues Using ANOVA

Heterocyclic chemistry has become one of the most important fields of research in pharmaceutical industry due to their many fold applications. Amongst all, heterocyclic molecules containing nitrogen and oxygen (like oxadiazole ring system) have shown most potent biological activities. Microorganisms are strictly attendant with the fitness and well-being of human beings. The present treatments of bacterial and fungal infections are a bit unsatisfactory, owing to rapidly developing drug resistance and side effects. The improved of antibacterial and antifungal agents results in resistant to drugs. A series of substituted Oxadiazoles analogues 4a-jwere synthesized and screened for their antibacterial and antifungal activities to evaluate zone of inhibition. The significant effect ofin-vitroantimicrobial and antifungal activities of compounds 4a-jwere studied using one way ANOVA. It was shown that the variables 4a-j series weresignificant. Further pairwise comparison of significant differences between the variables were analyzed using Tukey HSD. The data revels that compound 4a with 2-methyl and 3chloro group in phenyl and benzoyl ring respectively, have shown excellent activity and more potent among the 4a-j series.

Design and synthesis of conjugated azo-hydrazone analogues using nano BF3·SiO2 targeting ROS homeostasis in oncogenic and vascular progression

Disrupted redox balance is implicated in multiple pathologies including malignant progression and tumor angiogenesis. In this investigation, we report the design and development of novel and effective ROS detoxifying azo-hydrazone molecules targeting malignant pathologies and neoangiogenesis. A series of azo-derivatives conjugated to hydrazones moieties (9a-j) were synthesized using Nano BF3·SiO2. The compounds (9a-j) were screened for in-vitro antioxidant and lipid peroxidation inhibitory activity. Among the series 9a-j, compound 9f potently quenched biologically relevant radicals such as superoxide and hydrogen peroxide which emerged as the lead ROS detoxifying molecules. Compound 9f potently inhibited the proliferative capability of Daltons Lymphoma Ascites (DLA) tumor cells in-vivo in dose dependent manner. Regressed tumor progression was correlated with pronounced endogenous antioxidant enzyme superoxide dismutase and catalase in-vivo. Also, ROS levels were severely suppressed in 9f treated mice as assessed by lapsed lipid peroxidation. Altered enzymic and ROS levels in-vivo by 9f were implicated in suppressed VEGF secretion leading to regressed tumor neovasculature and tumor growth. Considering together, it is evident that the synthetic azo-hydrazone analogue 9f with potent ROS scavenging efficacy inhibits tumor progression and neo-angiogenesis.

Structural studies of a novel bioactive benzophenone derivative: (4-Chloro-2-hydroxy-phenyl)-phenyl-methanone

ABSTRACT The title compound (4-Chloro-2-hydroxy-phenyl)-phenyl-methanone was synthesized and the product obtained was characterized by spectroscopic techniques, and finally the structure was confirmed by X-ray diffraction studies. The compound crystallizes in the orthorhombic crystal system with the space group Pbca with unit cell parameters, a = 14.0359(5) Å, b = 6.8084(3) Å, c = 23.1097(8) Å, and Z = 4. The structure exhibits an intramolecular hydrogen bond which closes an S(6) ring. No directional interactions beyond the van der Waals packing contacts were identified in the crystal structure.

5-(4-Meth­oxy­phen­yl)-1,3,4-oxa­diazol-2-amine

In the title compound, C9H9N3O2, the dihedral angle between the aromatic rings is 8.64 (10)°. The crystal structure features inversion-related dimers linked by pairs of N—H⋯N hydrogen bonds, generating R22(8) loops. A further N—H⋯N hydrogen bond links the dimers into (100) sheets.