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Fertility Regulation in Male Rats by Implemented Tetraazamacrocyclic Compounds of Iron(II): Synthetic, Spectroscopic, and Applied Aspects With Toxicological Screening
Ashu Chaudhary
Bioinorganic Chemistry and Applications , 2006,
Abstract: Antifertility and histopathological investigations were carried out on reproductive organs of male albino rats induced by tetraazamacrocyclic complexes of iron(II). The complexes were synthesized by the template condensation of 1,2-diaminoethane, 1,3-diaminopropane with succinic acid and phthalic acid in 2:2 molar ratios which are abbreviated as [ Fe ( TAML n )OAc] ( n=1 or 2 and TAML n represents tetraazamacrocyclic ligand). The complexes have been characterized by elemental analysis, conductivity measurements, IR, and electronic spectra.
Macrocyclic Assembly: A Dive into the Pecking Order and Applied Aspects of Multitalented Metallomacrocycles
Ashu Chaudhary,Ekta Rawat
International Journal of Inorganic Chemistry , 2014, DOI: 10.1155/2014/509151
Abstract: To aid in knowledge of macrocyclic complexes and biomedical scientists, we are presenting here a review article with compilation of work done so far along in relation to macrocyclic ligands and their metal complexes. The metal ion chemistry of macrocyclic ligands has now become a major subdivision of coordination chemistry. This overview focuses on developments in design, synthesis, and self-assembly of metal-based architectures and ligands related to macrocyclic chemistry. 1. Introduction and Scope Macrocycles occupy a unique segment of chemical space. In the past decade, their chemical diversity expanded significantly, supported by advances in bioinformatics and synthetic methodology. As a consequence, this structural type has now been successfully tested on most biological target classes. The goal of this paper is to put into perspective the current applications and opportunities associated with macrocycles [1]. Macrocycles are defined herein as molecules containing at least one large ring composed of nine or more atoms. Macrocycles have several features that make them interesting in efforts to tackle “difficult” targets with extended binding sites [2]. Because of their size and complexity, they can engage targets through numerous and spatially distributed binding interactions, thereby increasing both binding affinity and selectivity. Furthermore, cyclization provides a degree of structural preorganization that may reduce the entropy cost of receptor binding compared to linear analogues [3, 4]. A significant number of macrocyclic drugs are currently on the market, predominantly of natural product origin with complex structures [5]. This paper is dedicated to explore the field of macrocycles and to highlight salient features of their versatile chemistry. Cyclization of a linear molecule into a macrocyclic ring constitutes a significant change in molecular shape. This transformation restricts the degrees of conformational freedom of the molecule and imposes structural organization which was absent in the linear precursor [6]. Since the birth of macrocycles as early as 1936 [7], the field only began to blossom in early 1960s with the pioneering work of Thompson and Busch [8]. In such a large subject, this paper can focus only on certain aspects of macrocyclic chemistry. Medicinal chemists have long used macrocyclization as a tool in drug discovery. A classic illustration of this technique was the discovery of potent cyclic peptide somatostatin mimics three decades ago [9, 10]. The method of cyclization since then developed into a general paradigm in
Fertility Regulation in Male Rats by Implemented Tetraazamacrocyclic Compounds of Iron(II): Synthetic, Spectroscopic, and Applied Aspects with Toxicological Screening
Ashu Chaudhary,Ran Vir Singh
Bioinorganic Chemistry and Applications , 2006, DOI: 10.1155/bca/2006/17316
Abstract: Antifertility and histopathological investigations were carried out on reproductive organs of male albino rats induced by tetraazamacrocyclic complexes of iron(II). The complexes were synthesized by the template condensation of 1,2-diaminoethane, 1,3-diaminopropane with succinic acid and phthalic acid in 2:2 molar ratios which are abbreviated as [Fe(TAMLn)OAc] (n=1 or 2 and TAMLn represents tetraazamacrocyclic ligand). The complexes have been characterized by elemental analysis, conductivity measurements, IR, and electronic spectra.
Txicological Aspects of Newly Designed Macrocyclic Complexes ofIron(II)
Ashu Chaudhary,R. V. Singh
Metal-Based Drugs , 2002, DOI: 10.1155/mbd.2002.315
Abstract:
Potentially Biodynamic Tetraaza Macrocycles and their Manganese Complexes : Antiandrogen, Antimicrobial and PDI Studies
Ashu Chaudhary,Anita Phor,R. V. Singh
Bioinorganic Chemistry and Applications , 2005, DOI: 10.1155/bca.2005.161
Abstract: Fourteen to eighteen membered tetraazamacrocyclic ligands N4TTD1–N4TTD4 have 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 studies viz., 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.
Tetraazamacrocyclic Complexes of Tin(II): Synthesis Spectroscopy and Biological screening
CHAUDHARY,ASHU; SWAROOP,RATAN; SINGH,R.;
Boletín de la Sociedad Chilena de Química , 2002, DOI: 10.4067/S0366-16442002000300002
Abstract: sixteen to eighteen membered tetraamide macrocyclic ligands n4l1 and n4l2 have been prepared by the condensation of 1,2-diaminoethane or 1,3-diaminopropane with phthalic acid in the presence of condensing reagents dicyclohexylcarbodiimide and 4- dimethylaminopyridine. on reduction, these macrocyclic ligands give new tetraazamacrocycles n4l3 and n4l4 which form complexes with tin(ii) chloride. the macrocyclic ligands and their complexes have been characterized by elemental analysis, molecular weight determinations, conductance, ir and 1h nmr spectral studies. the spectral data suggested hexacoordinated state for tin in these complexes. conductivity data suggested that they behave as non-electrolytes. an octahedral geometry for these complexes has been proposed as the binding sites are the nitrogen atoms of the macrocycles. the formulation of the complexes of the type [sn(n4ln)cl2] has been established on the basis of chemical composition. the ligands and their complexes have been screened in vitro against a number of pathogenic fungi and bacteria to assess their growth inhibiting potential
Fertility Inhibitors Macrocyclic Complexes of BivalentManganese: Synthetic, Spectroscopic and Medicinal Approach
R. V. Singh,Ashu Chaudhary,Anita Phor
Bioinorganic Chemistry and Applications , 2003, DOI: 10.1155/s1565363303000190
Abstract:
Tetraazamacrocyclic Complexes of Tin(II): Synthesis Spectroscopy and Biological screening
ASHU CHAUDHARY,RATAN SWAROOP,R. SINGH
Boletín de la Sociedad Chilena de Química , 2002,
Abstract: Sixteen to eighteen membered tetraamide macrocyclic ligands N4L1 and N4L2 have been prepared by the condensation of 1,2-diaminoethane or 1,3-diaminopropane with phthalic acid in the presence of condensing reagents dicyclohexylcarbodiimide and 4- dimethylaminopyridine. On reduction, these macrocyclic ligands give new tetraazamacrocycles N4L3 and N4L4 which form complexes with tin(II) chloride. The macrocyclic ligands and their complexes have been characterized by elemental analysis, molecular weight determinations, conductance, IR and 1H NMR spectral studies. The spectral data suggested hexacoordinated state for tin in these complexes. Conductivity data suggested that they behave as non-electrolytes. An octahedral geometry for these complexes has been proposed as the binding sites are the nitrogen atoms of the macrocycles. The formulation of the complexes of the type [Sn(N4Ln)Cl2] has been established on the basis of chemical composition. The ligands and their complexes have been screened in vitro against a number of pathogenic fungi and bacteria to assess their growth inhibiting potential Se han preparado ligandos tetraaza macrociclicos de entre 16 a 18 minbros, por condensación de 1,2-diaminoethane o 1,3-diaminopropano con acido ftalico in presencia de de los reactivos condensantes diciclohexilcarbodimida y 4-dimetilaminopiridina. Reducción de estos macrociclos dio nuevos tetraaza macrociclos N4L3 y N4L4 los cuales forman complejos con cloruro de Sn(II). Estos macrociclos y sus complejos han sido caracterizados por análisis elemental, determinaciones de pesois moleculares, conductividad y espectros IR y 1 H NMR. La data espectroscopica sugiere que una hexacoordinación para el esta o en estos complejos. Los datos de conductividad indican que ellos se comportan como no electrolitos. Se propone una geometría octahedrica ya que los sitios de coordinación son los nitrógenos de los macrociclos. La formulación de los complejos como [Sn(N4Ln)Cl2] se ha establecido a partir de los datos de la composición química. Los ligandos y sus complejos han sido usados, in vitro, para determinar su potencial inhibidor de crecimiento de hongos y bacterias
Antimicrobial, Antifertility and Antiinflammatory Approach toTetradentate Macrocyclic Complexes of Iron(II) and Manganese(II)
Ashu Chaudhary,D. P. Jaroli,R. V. Singh
Metal-Based Drugs , 2002, DOI: 10.1155/mbd.2002.347
Abstract:
Synthetic, Biochemical, Antifertility and Antiinflammatory Aspects of Manganese and Iron Complexes
Ashu Chaudhary,Anita Phor,Sanjay Sharma,Anita Gajraj
Metal-Based Drugs , 2002, DOI: 10.1155/mbd.2002.97
Abstract:
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