Recent Advances in Biological Active Sulfonamide based Hybrid Compounds Part A: Two-Component Sulfonamide Hybrids

Abstract

Sulfonamides constitute an important class of drugs, with many types of pharmacological agents possessing antibacterial, anti-carbonic anhydrase, anti-obesity, diuretic, hypoglycemic, antithyroid, antitumor, and anti-neuropathic pain activities. The sulfonamides have the general formula R-SO2NHR', in which the functional group is bound to an aromatic, heterocycle, aliphatic, and so on. The nature of the R and R' moiety is variable, starting with hydrogen and ranging to a variety of moieties incorporating organic compounds such as coumarin, isoxazole, tetrazole, pyrazole, pyrrole, and so many other pharmaceutical active scaffolds that lead to a considerable range of hybrids named as sulfonamide hybrids. Part A of this review presents the most recent advances in designing and developing two-component sulfonamide hybrids containing coumarin, indole, quinoline, isoquinoline, chalcone, pyrazole/pyrazoline, quinazoline, pyrimidine, thiazole, benzothiazole, and pyridine between 2015 and 2020. Specifically, the authors review the scientific reports on the synthesis and biological activity of this kind of hybrid agent.

Synthesis, Characterization, Antimicrobial and Time Killing Activities of New Sulfa-Derived Schiff Bases Coordinated with Cu(II)

“…When the IR spectrums of compounds are examined, the O-H stretching vibrations of the phenolic -OH group is broad at the range of 3434-3421 cm −1 , and the C=N stretching vibrations of the azomethine group are seen as sharply in the range of 1614-1609 cm −1 . These bands support the completion of the formation reaction of compounds L 1 H-L 3 H. These values agree with those found for similar compounds [14][15][16].…”

“…Since sulfonamides are structurally similar to paminobenzoic acid (PABA), a cofactor in folic acid synthesis by bacteria, they can compete with it efficiently to inhibit the synthesis of proteins and nucleic acids, resulting in the inhibition of various microorganisms. Also, it is a sulfonamide, versatile half for its various pharmacological activities, including antibacterial, antifungal, anti-inflammatory, anti-carbonic anhydrase, diuretic, hypoglycemic, antithyroid and antiproton activities, and enzyme inhibition [7][8][9][10][11][12][13][14][15][16]. Sulfonamides, which inhibit the growth of bacterial cells by blocking the synthesis of an important vitamin called folic acid, have also been the subject of many studies due to their significant antitumor activity both in vitro and in vivo [17][18][19][20][21].…”

2-(N-allylsulfamoyl)-N-propylbenzamide

“…Sulfonamides are a very interesting class of drugs because of their many pharmacological properties [1], including their ability to inhibit carbonic anhydrase "CA" and their diuretic [2,3], anticancer [4], hypoglycemic [5], antiviral [6], antibacterial [7], and metalloprotease inhibitory effects [8]. Although they were discovered in the 1930s as chemotherapeutic agents for their antibacterial properties, they have recently attracted increasing interest due to the discovery of new pharmacological properties [9].…”

Design, synthesis, docking, ADMET and anticancer evaluations of N-alkyl substituted iodoquinazoline derivatives as dual VEGFR-2 and EGFR inhibitors

“…The hybridization strategy aimed at combining the EGFR, VEGFR inhibition and anticancer activity of quinazolines with other privileged pharmacophores possessing antitumor potency could enhance the activity of the compounds. 2,42 In this work, we designed some new iodoquinazolinones as potential VEGFR-2 and EGFR inhibitors by keeping the acetamide linker attached to the N-3 of the iodoquinazoline ring and modication of the distal side chains to be aliphatic, aromatic and/or heterocyclic rings.…”