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2. In vitro PAI-1 inhibitory activity of oxalamide derivatives☆

Author

Soma Srivastava, Ajay Sharma, Hiteshkumar Soni, Mehul Raviya, Bhavesh Parmar, Ganes Chakrabarti, Mukul R. Jain, Vrajesh Pandya, Pankaj R. Patel, and Shankar Jayram Shetty

Subjects
Pharmacology, chemistry.chemical_classification, Oxamic Acid, Serine Proteinase Inhibitors, biology, T-plasminogen activator, Chromogenic, Stereochemistry, Organic Chemistry, Biological activity, General Medicine, Inhibitory postsynaptic potential, Amides, Chemical synthesis, In vitro, Inhibitory Concentration 50, Enzyme, chemistry, Biochemistry, Enzyme inhibitor, Tissue Plasminogen Activator, Plasminogen Activator Inhibitor 1, Drug Discovery, biology.protein, Humans
Abstract

A number of oxalamide derivatives have been synthesized and evaluated for PAI-1 inhibitory activity. In vitro PAI-1 inhibitory activities of oxalamide derivatives are evaluated by chromogenic assay. Few compounds have shown significant PAI-1 inhibitory activity.

Published
2008
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3. Discovery of inhibitors of plasminogen activator inhibitor-1: structure-activity study of 5-nitro-2-phenoxybenzoic acid derivatives

Author

Akshyaya Rath, Vrajesh Pandya, Mukul R. Jain, Hiteshkumar Soni, Ganes Chakrabarti, Mehul Raviya, Bhavesh Parmar, Pankaj R. Patel, Mubeen Shaikh, Jigar S. Patel, Balaji Chaugule, Nirav Joshi, Harilal Patel, Kalapatapu V.V.M. Sairam, and Jignesh K. Joshi

Subjects
Male, Stereochemistry, Clinical Biochemistry, Drug Evaluation, Preclinical, Pharmaceutical Science, Administration, Oral, Biological Availability, Biochemistry, Tissue plasminogen activator, Tiplaxtinin, Benzoates, Piperazines, chemistry.chemical_compound, Structure-Activity Relationship, Drug Discovery, Plasminogen Activator Inhibitor 1, medicine, Structure–activity relationship, Animals, Rats, Wistar, Molecular Biology, Piperazine, Indoleacetic Acids, Molecular Structure, Drug discovery, Phenyl Ethers, Organic Chemistry, Thrombosis, Bioavailability, Rats, Disease Models, Animal, chemistry, Plasminogen activator inhibitor-1, Drug Design, Nitro, Molecular Medicine, medicine.drug
Abstract

Two novel series of 5-nitro-2-phenoxybenzoic acid derivatives are designed as potent PAI-1 inhibitors using hybridization and conformational restriction strategy in the tiplaxtinin and piperazine chemo types. The lead compounds 5a, 6c, and 6e exhibited potent PAI-1 inhibitory activity and favorable oral bioavailability in the rodents.

Published
2011

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