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1.
Eur J Med Chem ; 194: 112245, 2020 May 15.
Article in English | MEDLINE | ID: mdl-32220687

ABSTRACT

Antibacterial-resistance speaks to an overall alarm, particularly in regards to the flare-up of methicillin-resistance Staphylococcus aureus (MRSA), a classic reason for genuine skin and flimsy tissues diseases. Clinically noteworthy antibacterial-resistance is probably the best challenge of the 21st century. Notwithstanding, new-fangled antibiotics are right now being created at a much more slow pace than our developing requirement for such drugs. The intriguing atomic structure of indole ring makes them appropriate possibility for the drug advancement. In this scaled down survey we abridge novel indole-based derivatives potency against diverse bacterial strains. Specifically, we plot the connection between the different structures of altered indole derivatives along with its antibacterial movement against multidrug-resistance MRSA could be discussed. This prepared information may fill in as a target for the adjustment of accessible molecules to plan new powerful antibacterial agents with lesser side effects.


Subject(s)
Anti-Bacterial Agents/pharmacology , Indoles/pharmacology , Methicillin-Resistant Staphylococcus aureus/drug effects , Anti-Bacterial Agents/chemistry , Dose-Response Relationship, Drug , Drug Resistance, Bacterial/drug effects , Indoles/chemistry , Microbial Sensitivity Tests , Molecular Structure , Structure-Activity Relationship
2.
Eur J Med Chem ; 173: 117-153, 2019 Jul 01.
Article in English | MEDLINE | ID: mdl-30995567

ABSTRACT

At present more than 250 FDA approved chlorine containing drugs were available in the market and many pharmaceutically important drug candidates in pre-clinical trials. Thus, it is quite obvious to expect that in coming decades there will be an even greater number of new chlorine-containing pharmaceuticals in market. Chlorinated compounds represent the family of compounds promising for use in medicinal chemistry. This review describes the recent advances in the synthesis of chlorine containing heterocyclic compounds as diverse biological agents and drugs in the pharmaceutical industries for the inspiration of the discovery and development of more potent and effective chlorinated drugs against numerous death-causing diseases.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antimalarials/pharmacology , Antineoplastic Agents/pharmacology , Drug Discovery , Glycoside Hydrolase Inhibitors/pharmacology , Hydrocarbons, Chlorinated/pharmacology , Animals , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Antimalarials/chemical synthesis , Antimalarials/chemistry , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Glycoside Hydrolase Inhibitors/chemical synthesis , Glycoside Hydrolase Inhibitors/chemistry , Humans , Hydrocarbons, Chlorinated/chemical synthesis , Hydrocarbons, Chlorinated/chemistry , Molecular Structure
3.
Bioorg Chem ; 76: 113-129, 2018 02.
Article in English | MEDLINE | ID: mdl-29169078

ABSTRACT

Amino acids/peptide conjugated heterocycles represent an important class of therapeutical agents. Biologically active heterocycles are conjugated with amino acids or peptides to increase the drug resistance. Furthermore, the amino acid/peptide based drugs have low toxicity, ample bioavailability and permeability, modest potency and good metabolic and pharmacokinetic properties. Synthetic amino acid/peptides based heterocyclic conjugates constitute a promising choice for the development of new, less toxic and safer conventional pharmaceutical drugs in the near future. In this review, we discuss and highlight the recent findings of the structural features that encourage biological applications of amino acid/peptides based conjugates.


Subject(s)
Amino Acids/pharmacology , Peptides/pharmacology , Amino Acids/chemistry , Animals , Anti-Infective Agents/chemistry , Antineoplastic Agents/chemistry , Humans , Peptides/chemistry
4.
Anticancer Agents Med Chem ; 18(4): 488-505, 2018.
Article in English | MEDLINE | ID: mdl-29110622

ABSTRACT

Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer drugs and diverse new natural or synthetic compounds are developed continuously by scientists. Presently, a large number of drugs in clinical practice have showed pervasive side effect and multidrug resistance. Sulfonyl or sulfonamide hybrids became one of the most attractive subjects due to their broad spectrum of pharmacological activities. Sulfonyl hybrids were broadly explored for their anticancer activities and it was found that they possess minimum side effect along with multi-drug resistance activity. This review describes the most recent applications of sulfonyl hybrid analogues in anticancer drug discovery and further discusses the mechanistic insights, structure-activity relationships and molecular docking studies for the potent derivatives.


Subject(s)
Antineoplastic Agents/pharmacology , Drug Discovery , Neoplasms/drug therapy , Sulfonamides/pharmacology , Sulfonylurea Compounds/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Neoplasms/pathology , Structure-Activity Relationship , Sulfonamides/chemical synthesis , Sulfonamides/chemistry , Sulfonylurea Compounds/chemical synthesis , Sulfonylurea Compounds/chemistry
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