Potentially Biodynamic Tetraaza Macrocycles and their Manganese Complexes: Antiandrogen, Antimicrobial and PDI Studies

Fourteen to eighteen membered tetraazamacrocyclic ligands N4TTD1–N4TTD4have been synthesized by the condensation of aliphatic diamines. H2N–(CH2)y–NH2(y = 2 or 3) and dicarboxylic acids, HOOC- (CH2)x–COOH (x = 1 or 2) in the presence of condensing reagents dicyclohexylcarbodiimide (DCHC) and 4- dimethylaminopyridine (DMAP). On reduction these macrocyclic ligands give N4TTD5-N4TTD8, which form complexes with manganese(II) acetate. The new products with octahedral geometry have been characterized by elemental analyses, molecular weight determinations, magnetic moment and spectral studiesviz., infrared, electronic, mass and X-ray. On the basis of the spectral studies the binding sites are proposed as the nitrogen atom of the macrocycles. The formulation of the complexes as [Mn(CH3COO)2(N4TTDn)] (where n = 1 - 8) has been established on the basis of chemical composition. To assess the growth inhibiting potential of the ligands and their manganese (II) complexes biological screening have been undertaken. The testicular morphology, testicular sperm density, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trials and biochemical parameters of reproductive organs with ligands and their corresponding complexes, in vivo have also been described in the this communication.

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Antimicrobial, Antifertility and Antiinflammatory Approach to Tetradentate Macrocyclic Complexes of Iron(II) and Manganese(II)

Metal-Based Drugs ◽

10.1155/mbd.2002.347 ◽

2002 ◽

Vol 8 (6) ◽

pp. 347-353 ◽

Cited By ~ 9

Author(s):

Ashu Chaudhary ◽

D. P. Jaroli ◽

R. V. Singh

Keyword(s):

Molecular Weight ◽

Reproductive Organs ◽

Spectral Studies ◽

Central Metal Atom ◽

Central Metal ◽

Testicular Sperm ◽

Mass Spectral ◽

Sperm Density ◽

Elemental Analyses

Some antifertility inhibitors of 18 to 24-membered tetraazamacrocyclic complexes of iron(II) and manganese(II) have been synthesised by the template condensation using 1,3-phenylenediamine with malonic acid, succinic acid, glutaric acid and adipic acid. The reaction proceed smoothly to completion. The complexes were characterized by elemental analyses, molecular weight determinations, infrared, electronic, magnetic moment, mössbaur and mass spectral studies. The elemental analyses are consistent with the formation of the complexes [M(N4Ln)Cl2] (M = Fe(lI) or Mn(II)). All these complexes are stable and monomeric in nature as indicated by the molecular weight determinations. The spectral studies confirm the octahedral geometry around the central metal atom. The complexes have been screened in vitro against a number of fungi and bacteria to assess their growth inhibiting potential. The testicular sperm density and testicular sperm morphology, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trials and biochemical parameters of reproductive organs have been examined and discussed.

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Fertility Inhibitor Heterobimetallic Complexes of Platinum(II) and Palladium(II): Synthetic, Spectroscopic and Antimicrobial Aspects

Metal-Based Drugs ◽

10.1155/mbd.2000.105 ◽

2000 ◽

Vol 7 (2) ◽

pp. 105-113 ◽

Cited By ~ 15

Author(s):

Kripa Sharma ◽

S. C. Joshi ◽

R. V. Singh

Keyword(s):

Sperm Morphology ◽

Pathogenic Fungi ◽

Reproductive Organs ◽

Spectral Studies ◽

Planar Geometry ◽

Testicular Sperm ◽

Heterobimetallic Complexes ◽

Sperm Density ◽

Square Planar ◽

Elemental Analyses

Synthetic, spectroscopic and antimicrobial aspects of some fertility inhibitor heterobimetallic complexes have been carried out. These heterobimetallic chelates [M(C5H5N3)2M2'(R)4]Cl2 (M = Pd or Pt and M' = Si, Sn, Ti and Zr) have been successfully synthesinzed via the reaction of M(C5H7N3)2Cl2 with group four or fourteen dichlorides in 1:2 stoichiometric proportions. The products were characterized by elemental analyses, molecular weight determinations, magnetic susceptibility measurements, conductance, and IR multinuclear NMR and electronic spectral studies. A square planar geometry has been suggested for all the complexes with the help of spectral data. Conductivity data strongly suggest that chlorine atoms are ionic in nature due to which complexes behave as electrolytes. All the complexes have been evaluated for their antmicrobial effects on different species of pathogenic fungi and bacteria. The testicular sperm density, testicular sperm morphology, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trails and biochemical parameters of reproductive organs have been examined and discussed.

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Synthesis and Characterization of Some Group 12 Metal Complexes with Tellurium Containing 10-Membered Tetraazamacrocyclic Ligands

E-Journal of Chemistry ◽

10.1155/2011/768192 ◽

2011 ◽

Vol 8 (3) ◽

pp. 1158-1163

Author(s):

Nitu ◽

K. K. Verma

Keyword(s):

Metal Complexes ◽

Spectral Studies ◽

Conductivity Measurements ◽

Metal Chlorides ◽

Group 12 ◽

Elemental Analyses ◽

Physicochemical Studies ◽

Tetraazamacrocyclic Ligands ◽

Pmr Spectra

A new series of 10-membered tellurium containing tetraazamacrocyclic complexes, [ML1Cl2], [ML2Cl2] and [ML3Cl2], where [M=Zn(II), Cd(II), Hg(II); L1, L2and L3=10-membered tellurium containing tetraazamacrocyclic ligands] have been prepared via the template condensation of ethylenediamine and diaryltellurium dichlorides, R2TeCl2, (R=p-hydroxyphenyl, 3-methyl-4-hydroxyphenyl,p-methoxyphenyl) in the presence of metal chlorides. These complexes have been characterized by elemental analyses, conductivity measurements, infrared, electronic absorption and proton magnetic resonance spectral studies. IR and PMR spectra confirm the formation of 10-membered tetraazamacrocycle skeleton and their tetradentate nature. An octahedral geometry has been assigned to all the metal complexes on the basis of various physicochemical studies.

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Txicological Aspects of Newly Designed Macrocyclic Complexes of Iron(II)

Metal-Based Drugs ◽

10.1155/mbd.2002.315 ◽

2002 ◽

Vol 8 (6) ◽

pp. 315-321 ◽

Cited By ~ 6

Author(s):

Ashu Chaudhary ◽

R. V. Singh

Keyword(s):

Binding Sites ◽

Brine Shrimp ◽

Condensation Reaction ◽

Octahedral Geometry ◽

Macrocyclic Complexes ◽

Spectral Studies ◽

X Ray ◽

Mass Spectral ◽

Molar Ratios ◽

Elemental Analyses

Brine shrimp lethality of a new series of 16 to 26-membered macrocycles of iron(II) containing tetraaza groups and prepared by the template condensation reaction of diacarboxylic acids (malonic, succinic, glutaric or adipic) with 2,6-diaminopyridine and diethylenetriamine in 1:2:2 molar ratios have been studied. Structures and bonding of the macrocyclic complexes have been proposed based on elemental analyses, IR, electronic, X-ray and mass spectral studies. An octahedral geometry for these complexes has been proposed as the binding sites are the nitrogen atoms of the macrocycles. The formation of the complexes as [Fe(Ln)Cl2] has been established on the basis of the chemical composition. The complexes have also been screened against several microbes.

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Design, Synthesis and Biological Evaluation of 5-amino-3-aryl-1-(6'-chloropyridazin-3'-yl)pyrazoles and their Derivatives as Analgesic Agents

Drug Research ◽

10.1055/a-1202-9959 ◽

2020 ◽

Vol 70 (11) ◽

pp. 493-502

Author(s):

Ranjana Aggarwal ◽

Pawan Kaushik ◽

Ajay Kumar ◽

Deepika Saini ◽

Keyword(s):

Biological Evaluation ◽

Spectral Studies ◽

Design Synthesis ◽

Standard Drug ◽

Docking Simulations ◽

Mass Spectral ◽

Elemental Analyses ◽

Analgesic Agents ◽

Docking Interaction

AbstractAn efficient and environmental benign solvent-free synthesis of 5-amino-3-aryl-1-(6'-chloropyridazin-3'-yl)pyrazoles (4a-e) was accomplished by grinding 3-chloro-6-hydrazinopyridazine (2) and β-ketonitriles (3a-e) in the presence of p-toulenesulfonic acid as a catalyst. Subsequently, 6'-chloro group in 4a-e was replaced with cyclic 2° amine derivatives viz. pyrrolidine 5a, piperidine 5b and morpholine 5c to obtain 6a-e, 7a-e, 8a-e respectively. The newly synthesized compounds were characterized by using IR, NMR (1H and 13C), mass spectral studies, elemental analyses. All the synthesized compounds were studied for their docking interaction with target protein 6COX and screened for their in vivo analgesic mode of action against swiss albino mice (animal model) using acetic-acid induced writhing test. Consequently, docking simulations data justifies the potential of synthesized series as an analgesic and very well correlated with in vivo study. Preliminary results revealed that most of the synthesized compounds exhibited moderate to good analgesic activity as compared to reference/standard drug (s) sodium diclofenac and candidates 4d and 7c protrude out as a promising lead for further investigation.

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Synthesis, Characterization, In Vitro and In Vivo Screening of Unsymmetrical Borole Complexes of 2-Hydroxy-N-Phenylbenzamide and its Derivatives

Metal-Based Drugs ◽

10.1155/mbd.2000.7 ◽

2000 ◽

Vol 7 (1) ◽

pp. 7-16 ◽

Cited By ~ 8

Author(s):

Taruna Pandey ◽

R. V. Singh

Keyword(s):

Pathogenic Fungi ◽

Reproductive Organs ◽

Molar Ratio ◽

Testicular Sperm ◽

Sperm Density ◽

Bactericidal Properties ◽

Boron Complexes

Biochemical aspects, synthesis and characterization of some boron complexes of 2-hydroxy-N-phenylbenzamide (HOPhBenz) and its semicarbazone (HOPhBenz.SCZH) and thiosemicarbazone (HOPhBenz.TSCZH) are described. These derivatives were prepared by the reactions of 2-isopropoxy-4-methyl-1,3,2-dioxaborolane, and 2-isopropoxy-4-methyl-1,3,2-dioxaborinane with 2-hydroxy-N-phenylbenzamide, 1-[(2-hydroxyphenyl)-1-N-phenylamino]hydrazinecarboxamide (HOPhBenz.SCZH), and 1-[(2-hydroxyphenyl)-1-N-phenylamino]hydrazinecarbothioamide(HOPhBenz.TSCZH) in a 1:1 molar ratio. In order to assess the increase of the inhibitor potency, (HOPhBenz), (HOPhBenz.SCZH), (HOPhBenz.TSCZH) and their boron complexes have been tested in vitro against a number of pathogenic fungi and bacteria at different concentrations and were found to possess remarkable fungicidal and bactericidal properties. The testicular sperm density, testicular sperm morphology, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trials and biochemical parameters of reproductive organs are discussed.

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Synthetic, structural and biochemical approach of the macro cyclic complexes of manganese (II) and tin (II)

Research Journal of Chemistry and Environment ◽

10.25303/257rjce16121 ◽

2021 ◽

Vol 25 (7) ◽

pp. 161-166

Author(s):

Nidhi Bansal ◽

Saurabh Dave ◽

Ruchi Seth

Keyword(s):

Metal Ion ◽

Biological Properties ◽

Molar Ratio ◽

High Yield ◽

Spectral Studies ◽

X Ray Diffraction ◽

X Ray ◽

Elemental Analyses ◽

Biochemical Approach ◽

Formation Of Complexes

This study presents a brief account of the synthesis, spectroscopic and biochemical aspects of tetraazamacrocyclic complexes of managenese (II) and tin (II). The complexes of manganese (II) and tin (II) were prepared by the template condensation of metal salts with phthalic acid and diamines (1,3-diaminobutane and 1,4- diaminobutane) in 1:2:2 molar ratio. All the complexes are soluble in polar solvent. The structures were investigated using elemental analyses, molecular weight determinations, conductivity measurements, electronic, infrared and X-Ray diffraction spectral studies. The elemental analyses are consistent with the formation of complexes of the type [M(Macn)Cl2] (where, n=1-2, M=Mn(II), Sn (II)). An octahedral geometry around the metal ion is suggested for these complexes. All the complexes were screened against several fungi and bacteria to assess its biological properties and results are discussed.The importance of this method includes shorter reaction time and high yield.

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Preparation of cultured astrocytes for x-ray microanalysis

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100156924 ◽

1989 ◽

Vol 47 ◽

pp. 988-989

Author(s):

N.K.R. Smith ◽

K.E. Hunter ◽

P. Mobley ◽

L.P. Felpel

Keyword(s):

Cultured Cells ◽

Elemental Content ◽

Elemental Distribution ◽

Sprague Dawley ◽

X Ray ◽

Cultured Astrocytes ◽

Freeze Dried ◽

Ultimate Objective

Electron probe energy dispersive x-ray microanalysis (XRMA) offers a powerful tool for the determination of intracellular elemental content of biological tissue. However, preparation of the tissue specimen , particularly excitable central nervous system (CNS) tissue , for XRMA is rather difficult, as dissection of a sample from the intact organism frequently results in artefacts in elemental distribution. To circumvent the problems inherent in the in vivo preparation, we turned to an in vitro preparation of astrocytes grown in tissue culture. However, preparations of in vitro samples offer a new and unique set of problems. Generally, cultured cells, growing in monolayer, must be harvested by either mechanical or enzymatic procedures, resulting in variable degrees of damage to the cells and compromised intracel1ular elemental distribution. The ultimate objective is to process and analyze unperturbed cells. With the objective of sparing others from some of the same efforts, we are reporting the considerable difficulties we have encountered in attempting to prepare astrocytes for XRMA.Tissue cultures of astrocytes from newborn C57 mice or Sprague Dawley rats were prepared and cultured by standard techniques, usually in T25 flasks, except as noted differently on Cytodex beads or on gelatin. After different preparative procedures, all samples were frozen on brass pins in liquid propane, stored in liquid nitrogen, cryosectioned (0.1 μm), freeze dried, and microanalyzed as previously reported.

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Features hormonal hemostasis in patients with benign hyper-plastic processes of breasts

HEALTH OF WOMAN ◽

10.15574/hw.2016.115.72 ◽

2016 ◽

pp. 72-74 ◽

Cited By ~ 2

Author(s):

M. Makarenko ◽

◽

D. Govsieiev ◽

O. Gromova ◽

L. Martynova ◽

...

Keyword(s):

Luteal Phase ◽

Reproductive Organs ◽

Breast Diseases ◽

Hormonal Changes ◽

Morphological Investigation ◽

Fibrocystic Disease ◽

X Ray ◽

Pelvic Organs ◽

Hormone Research ◽

Gynecological Diseases

The objective: to study the incidence of gynecological diseases, clinical and hormonal parameters of the menstrual cycle in patients with benign hyper-plastic processes of breasts. Patients and methods. 65 women with various forms of mastitis were investigated. The following investigations were conducted: mammologistic and gynecological investigation, mommologistic X-ray investigation, ultrasound of breasts and of the pelvic organs, endometrial aspiration biopsy that was followed by cytology; when it was necessary the diagnostic laparoscopy, colposcopy, hysteroscope with curettage and morphological investigation of the endometrium, hormone research and rectal temperature measurements were conducted. Results. The frequency of the benign breast diseases was set: fibrocystic disease of breast – 32 women (49.2±6.20%), fibrous of breast – 16 women (24.6±5.34%), nodular of breasts – 8 women (12.3±4.07%), fibroadenoma – 6 women (9.2±3.59%), nodular disease of breasts on the background of fibroid changes – 3 women (4.6±2.60%). All in all, 96.9±2.14% of the patients had any gynecological diseases. Thus, the average age of the ‘debut’ of mastitis was 31.4±1.09 years; the hyper-plastic processes in the uterus was 35.2±1.17 years. Anovulation was detected in 17 (47.2±8.3%) patients, the lack of the luteal phase (NLF) was detected in 11 (30.6±7.6) patients. Conclusions. Identified hormonal changes are typical for patients with the hyper-plastic processes of the reproductive organs with different localization (breasts, uterus, ovaries). Due to the commonality of the hormone changes in most cases mastitis is combined with the various gynecological diseases (96.9±2.14%). Key words: gynecological pathology, hormonal changes, breast, factors of risk.

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Tele-Substitution Reactions in the Synthesis of a Promising Class of Antimalarials

10.26434/chemrxiv.12212927 ◽

2020 ◽

Author(s):

Marat Korsik ◽

Edwin Tse ◽

David Smith ◽

William Lewis ◽

Peter J. Rutledge ◽

...

Keyword(s):

Heterocyclic Ring ◽

Ring System ◽

Substitution Reactions ◽

Laboratory Notebook ◽

Polar Solvents ◽

X Ray ◽

X Ray Crystallography ◽

The Core ◽

Nmr Data

We have discovered and studied a telesubstitution reaction in a biologically important heterocyclic ring system. Conditions that favour the tele-substitution pathway were identified: the use of increased equivalents of the nucleophile or decreased equivalents of base, or the use of softer nucleophiles, less polar solvents and larger halogens on the electrophile. Using results from X-ray crystallography and isotope labelling experiments a mechanism for this unusual transformation is proposed. We focused on this triazolopyrazine as it is the core structure of the in vivo active anti-plasmodium compounds of Series 4 of the Open Source Malaria consortium. Archive of the electronic laboratory notebook with the description of all conducted experiments and raw NMR data could be accessed via following link <a href="https://ses.library.usyd.edu.au/handle/2123/21890">https://ses.library.usyd.edu.au/handle/2123/21890</a> . For navigation between entries of laboratory notebook please use file "Strings for compounds in the article.pdf" that works as a reference between article codes and notebook codes, also this file contain SMILES for these compounds.

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