ABSTRACT
Ideally a drug should be administered in a form that it exerts its pharmacological action at the target site using the lowest concentration possible and without undesirable effects. Drug targeting is the approach which is followed for the purpose. Among different approaches preparation of synthetic glycosides of target drug and administering them orally is one of the most recent approaches. The drug glycoside on reaching colonic region releases the active drug through enzymatic action. This approach has been detailed with different successful examples. Synthetic drug-glycosides, besides being used as drug targeting agents, have been shown to exhibit varied biological activities such as antineoplastic, antidiabetic, antiinfllamatory etc., which have been reviewed. Synthetic approaches to O-, C-, N-, S glycosides have been discussed.
Subject(s)
Antineoplastic Agents/chemistry , Drug Carriers/chemistry , Glycosides/chemistry , Prodrugs/chemistry , Anti-Inflammatory Agents/chemical synthesis , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/toxicity , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/toxicity , Antiviral Agents/chemical synthesis , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Cell Proliferation/drug effects , Colonic Diseases/drug therapy , Colonic Diseases/metabolism , Glycosides/therapeutic use , Glycosides/toxicity , Humans , Prodrugs/therapeutic use , Prodrugs/toxicity , Viruses/drug effectsABSTRACT
The significance of herbals and herbal products is gaining worldwide recognition. The concept of complementary or alternative medicine is becoming much more widely accepted, and there is an increasing belief in the efficacy of herbal remedies. Recently, the role of herbal drugs, herbal products and certain phytochemicals in the control of ageing has been documented using modern scientific approaches. This review pulls together such studies and critiques the efficacy and value of herbal medicines in the control of the ageing process.
Subject(s)
Aging/drug effects , Cellular Senescence/drug effects , Complementary Therapies , Plant Preparations/pharmacology , Animals , Humans , Molecular Structure , Plant Preparations/chemistry , Structure-Activity RelationshipABSTRACT
Although ageing is a natural wear and tear phenomenon, it can at least be postponed or prevented by certain approaches. Some chemicals that are present in the diet or in dietary supplements have been documented to have anti-ageing effects. Recently, a number of synthetic drugs used for other therapeutic indications have been shown to have anti-ageing potential.
Subject(s)
Aging/drug effects , Biological Products/pharmacology , Pharmaceutical Preparations/chemistry , Biological Products/chemistry , Diet , Dietary Supplements , Hormone Replacement Therapy , Humans , Molecular StructureABSTRACT
Several 1-aryl-2-phenyl-4-piperidino-4-thioalkyl-1,3-diazabuta-1,3-dienes were prepared by the treatment of N-arylimino isothiocyanate with piperidine followed by S-alkylation with alkyl iodides in the presence of dry acetone and potassium hydroxide. The constitution of the products was supported by IR, PMR and mass spectral study. The compounds synthesized were tested in in vitro against E. coli, S. aureus, P. aeruginosa, B. cereus and B. subtilis and fungal stains, Candida albicans and Aspergillus niger. Standard drugs were also tested under identical conditions for comparing the results.
Subject(s)
Amidines/chemical synthesis , Anti-Bacterial Agents/chemical synthesis , Antifungal Agents/chemical synthesis , Alkylation , Amidines/pharmacology , Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Butadienes/chemistry , Candida albicans/drug effects , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Isothiocyanates/chemistry , Molecular Structure , Piperidines/chemistryABSTRACT
A series of novel-2-phenyl-1-p-tolyl-4-thiomethyl-1,3-diazabuta-1,3-dienes compounds (5a-5e) possessing morpholino, diethyl amino, pyrrolidino, piperidino and 2-aminopyridino groups respectively at C-4 were prepared by reaction of alpha-aryliminobenzyl isothiocyanates with secondary amines and S-alklyation of the resultant thioureas with aqueous potassium hydroxide. The isothiocyanates were obtained from easily available starting materials. These 1,3-diazabuta-1,3-dienes were obtained in pure form after recrystallization and their structures were established by analytical and spectral data. The synthesized compounds were screened for their antibacterial activity and some of them were found to exhibit significant antibacterial activity.
