Chemical structure of phenothiazines and their biological activity.
نویسندگان
چکیده
Phenothiazines belong to the oldest, synthetic antipsychotic drugs, which do not have their precursor in the world of natural compounds. Apart from their fundamental neuroleptic action connected with the dopaminergic receptors blockade, phenothiazine derivatives also exert diverse biological activities, which account for their cancer chemopreventive-effect, as: calmodulin- and protein kinase C inhibitory-actions, anti-proliferative effect, inhibition of P-glycoprotein transport function and reversion of multidrug resistance. According to literature data on relations between chemical structure of phenothiazines and their biological effects, the main directions for further chemical modifications have been established. They are provided and discussed in this review paper.
منابع مشابه
Docking and Biological Screening of Bezo[A]phenothiazinones as Novel Inhibitors of Bacterial Peptidogloycan Transpeptidase
Rising cases of antibiotic-resistant bacteria is a public health concern. Many approved antibiotics target penicillin-binding proteins example peptidoglycan transpeptidase (PTPase). Due to wide pharmacological activity of phenothiazines, new styryl, aryl, alkynyl, and thiophenyl benzo[a]phenothiazines were synthesized and their inhibitory potency against PTPasein silico and Gram-po...
متن کاملApplication of Graph Theory: Relationship of Topological Indices with the Partition Coefficient (logP) of the Monocarboxylic Acids
It is well known that the chemical behavior of a compound is dependent upon the structure of itsmolecules. Quantitative structure – activity relationship (QSAR) studies and quantitative structure –property relationship (QSPR) studies are active areas of chemical research that focus on the nature ofthis dependency. Topological indices are the numerical value associated with chemical constitution...
متن کاملThe surface activity of phenothiazine derivatives at the air-solution interface.
The surface activity of triflupromazine, chlorpromazine, promazine, promethazine, and chlorpromazine sulfoxide has been determined at the air-solution interface by the drop-volume method to measure surface tension. Differences in the abilities of the various phenothiazines employed to affect surface pressure development seem correlated with their relative nonpolarities. Anionic buffer ingredien...
متن کاملMononuclear and Dinuclear Copper(II) Complexes Containing N, O and S Donor Ligands: Synthesis, Characterization, Crystal Structure Determination and Antimicrobial Activity of [Cu(phen)(tda)].2H2O and [(phen)2Cu(µ-tda)Cu(phen)](ClO4)2.1.5H2O
Copper complexes of [Cu(phen)(tda)].2H2O(1) and [(phen)2Cu(µ-tda) Cu(phen)](ClO4)2.1.5H2O (2) (where phen is 1,10-phenanthroline and tda2- is thiodiacetate) have been synthesized. Both complexes were characterized by elemental analysis, IR, UV–Vis spectroscopy and cyclic voltammetry. Their solid state struct...
متن کاملThe effect of halogen atoms at propanoate anion on thermo physical, vibrational spectroscopy, chemical reactivity, biological properties of morpholinium propionate Ionic Liquid
The morpholinium cation based ionic liquids are designed to evaluate the thermophysical, chemical reactivity, and biological activity. To estimate and design the bioactive ILs, propionate and trihalopropanoate were considered under theoretical study by Density Functional Theory (DFT). To make effect of halogens atom on anion, propionate, trifluro propionate, trichloro propionate, and tribromo p...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Pharmacological reports : PR
دوره 64 1 شماره
صفحات -
تاریخ انتشار 2012