Abstract

The unusual structure and chemical composition of the mycobacterial cell wall, the tedious duration of therapy, and resistance developed by the microorganism have made the recurrence of the disease multidrug resistance and extensive or extreme drug resistance. The prevalence of tuberculosis in synergy with HIV/AIDS epidemic augments the risk of developing the disease by 100-fold. The need to synthesize new drugs that will shorten the total duration of effective treatment and/or significantly reduce the dosage taken under DOTS supervision, improve on the treatment of multidrug-resistant tuberculosis which defies the treatment with isoniazid and rifampicin, and provide effective treatment for latent TB infections which is essential for eliminating tuberculosis prompted this review. In this review, we considered the synthesis and structure activity relationship study of carboxamide derivatives with antitubercular potential.

Highlights

  • Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis, which most commonly affects the lungs

  • Delamanid marketed as Deltyba is indicated for use as part of an appropriate combination regimen for pulmonary Multidrug resistance tuberculosis (MDR-TB) in adult patients when an effective treatment regimen cannot otherwise be composed for reasons of resistance or tolerability. It must be administered as directly observed therapy (DOT) because of its adverse effect and it lasts for 24 weeks

  • Pyrazine carboxamide is an important component in the intensive phase of short-course treatment of TB owing to its sterilizing effect, ability to act in acidic environments, and excellent synergy with rifampicin

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Summary

Introduction

Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis, which most commonly affects the lungs. Bedaquiline is marketed as SIRTURO and chemically known as (1R,2S)-1-(6-bromo2-methoxy-3-quinolinyl)-4-(dimethylamino)-2-(1-naphthalenyl)-1-phenyl-2-butanol Though this drug has good antitubercular activity, it needs 24 weeks of treatment thereby encouraging the development of resistance specie arising from noncompliance to prescription and it has been shown to cause adverse effects like hemoptysis and anorexia [23]. Delamanid marketed as Deltyba is indicated for use as part of an appropriate combination regimen for pulmonary MDR-TB in adult patients when an effective treatment regimen cannot otherwise be composed for reasons of resistance or tolerability It must be administered as directly observed therapy (DOT) because of its adverse effect and it lasts for 24 weeks. In an effort to discover new and effective chemotherapeutic agent for the treatment of TB, the antimycobacterial activities of various phthalazin-4-yl acetamides [25], thiazolylthiosemicarbazones [26], chromeno[3,2-c]pyridine-3-yl derivatives [27], [1,4]-thiazines [28], thieno-[2,3-b]thiophene [29], spirocyclohexanones derivatives [30], thieno[3,2b]indoles [31], furan-2-yl derivatives [32], thiadiazoles derivatives [33], imidazole derivatives [34, 35], acyclic deoxy monosaccharide derivatives [36], benzoic acid hydrazine class [37], calanolide A, a naturally occurring coumarin derivatives [38, 39], purine derivatives [40, 41], pyrrole derivatives [42, 43], benzoxazine derivatives [44], diterpenoids derived from plants [45, 46], and quinoline and quinoxaline derivatives [47] have been reported

Synthesis of Pyrazine Derived Carboxamides
Synthesis of Novel Thiadiazolyl Pyrrolidine Carboxamides
Synthesis of Aryl Thiazolidine Carboxamides
Synthesis of Phenothiazine Derived Thiazolidinone Carboxamides
Synthesis of Tetrahydropyrazolopyrimidine Carboxamides
NCONH2 Cl
Findings
10. Conclusion
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