ABSTRACT
Liquid-phase combinatorial library synthesis is commonly developed into the viable alternatives or adjunct across the broad spectrum of polymer-supported organic chemistry. It includes the use of soluble polymer supports in the combinatorial synthesis of peptides and small-molecular library compounds which act as catalyst and reagent supports. It also includes high throughput biological screening with generation and evaluation of chemical leads for drug discovery development. In this review, liquid-phase combinatorial library synthesis is shown as the most efficient method of choice for the synthesis of most of the combinatorial library compounds with specific approaches from different groups that state potentials of solution-phase combinatorial synthesis.
Subject(s)
Combinatorial Chemistry Techniques/methods , Drug Discovery/methods , High-Throughput Screening Assays/methods , Combinatorial Chemistry Techniques/instrumentation , Drug Discovery/instrumentation , High-Throughput Screening Assays/instrumentation , Peptide Library , Peptides/chemical synthesis , Peptides/chemistry , Small Molecule Libraries/chemical synthesis , Small Molecule Libraries/chemistryABSTRACT
Benzopyran derivatives are the potassium channel openers (KCOs) having antihypertensive, cardio-protective, myocardial protectors, powerful peripheral vasodilators and anti-ischemic activity. Their usage as anti-ischemic including angina, hypertension and diabetes is thought to be due to the stimulation of KATP channels which are contemplated to produce vasorelaxation and myocardial protection. It is observed that potassium channels are involved in mediating the cardio-protective effects of pre-conditioning in animal models and man. KCOs protect heart from an ischemic insult without contribution from vasodilatation. This review provides an overview of the characteristics of KCOs and their actions on subtypes used widely for the treatments of various diseases including hypertension, cardiac ischemia, arrhythmia, smooth muscle relaxation, diabetes, cardio-protective and anti-angiogenic activities.
Subject(s)
Benzopyrans/chemistry , KATP Channels/metabolism , Animals , Anti-Arrhythmia Agents/chemistry , Anti-Arrhythmia Agents/pharmacology , Anti-Arrhythmia Agents/therapeutic use , Antihypertensive Agents/chemical synthesis , Antihypertensive Agents/chemistry , Antihypertensive Agents/pharmacology , Arrhythmias, Cardiac/drug therapy , Benzopyrans/chemical synthesis , Benzopyrans/therapeutic use , Blood Pressure/drug effects , Cardiotonic Agents/chemical synthesis , Cardiotonic Agents/chemistry , Cardiotonic Agents/pharmacology , Heart/drug effects , Humans , Ischemia/drug therapy , KATP Channels/chemistry , Muscle Relaxation/drug effects , Vasodilator Agents/chemistry , Vasodilator Agents/pharmacology , Vasodilator Agents/therapeutic useABSTRACT
Benzimidazole plays an important role in the medicinal chemistry and drug discovery with many pharmacological activities which have made an indispensable anchor for discovery of novel therapeutic agents. Substitution of benzimidazole nucleus is an important synthetic strategy in the drug discovery process. Therapeutic properties of the benzimidazole related drugs have encouraged the medicinal chemists to synthesize novel therapeutic agents. Therefore, it is required to couple the latest information with the earliest information to understand the current status of benzimidazole nucleus in drug discovery. In the present review, benzimidazole derivatives with different pharmacological activities are described on the basis of substitution pattern around the nucleus with an aim to help medicinal chemists for the development of SAR on benzimidazoles for each activity. This article aims to review the work reported, chemistry and pharmacological activities of benzimidazole derivatives during past years.
ABSTRACT
Recent developments and novel research strategies are adopted widely to discover and develop the new drugs to treat tuberculosis. New antitubercular drugs are urgently needed because tuberculosis remains a global health problem as around nine million new cases are estimated each year with almost two million fatalities. It states the impact and outcomes that have made a significant effect in antitubercular drug development. We are presenting current status of tuberculosis, antitubercular drug development, novel molecular targets, novel agents in clinical and pre-clinical development and some efforts that are being made in the development of novel molecules based on different pharmacophores as lead compounds and recent strategies.
Subject(s)
Antitubercular Agents/chemistry , Antitubercular Agents/pharmacology , Antitubercular Agents/therapeutic use , Clinical Trials as Topic , Cytochrome P-450 Enzyme Inhibitors , Cytochrome P-450 Enzyme System/metabolism , Drug Evaluation, Preclinical , Drug Resistance, Multiple, Bacterial , Heterocyclic Compounds/chemistry , Heterocyclic Compounds/pharmacology , Heterocyclic Compounds/therapeutic use , Humans , Mycobacterium tuberculosis/drug effects , Structure-Activity Relationship , Tuberculosis/drug therapyABSTRACT
An urgent need for the discovery of novel anticancer agents is required for the long term therapy of cancer. Large number of novel bio-active and potential anticancer agents are being used in clinical and pre-clinical trials. Although many heterocyclic compounds are already available commercially as anticancer agents, great efforts have been put to identify novel anticancer targets. This review provides an insight of the novel anticancer targets and molecules of the first and final stage of clinical and pre-clinical trials.
Subject(s)
Antineoplastic Agents/pharmacology , Drug Discovery , Neoplasms/drug therapy , Antineoplastic Agents/therapeutic use , Clinical Trials as Topic , Drug Evaluation, Preclinical , HumansABSTRACT
Benzimidazole plays an important role in the medicinal chemistry and drug discovery with many pharmacological activities which have made an indispensable anchor for discovery of novel therapeutic agents. Substitution of benzimidazole nucleus is an important synthetic strategy in the drug discovery process. Therapeutic properties of the benzimidazole related drugs have encouraged the medicinal chemists to synthesize novel therapeutic agents. Therefore, it is required to couple the latest information with the earliest information to understand the current status of benzimidazole nucleus in drug discovery. In the present review, benzimidazole derivatives with different pharmacological activities are described on the basis of substitution pattern around the nucleus with an aim to help medicinal chemists for the development of SAR on benzimidazoles for each activity. This article aims to review the work reported, chemistry and pharmacological activities of benzimidazole derivatives during past years.
