Novel 1,4‐Substituted‐1,2,3‐Triazoles as Antitubercular Agents

Abstract

Tuberculosis (TB) remains a pressing unmet medical need, particularly with the emergence of multidrug-resistant and extensively drug-resistant tuberculosis. Here, a series of 1,4-substituted-1,2,3-triazoles have been synthesized and evaluated as potential antitubercular agents. These compounds were assembled via click chemistry in high crude purity and in moderate to high yield. Of the compounds tested, 12 compounds showed promising antitubercular activity with six possessing minimum inhibitory concentration (MIC) values <10 μg mL(-1) , and total selectivity for Mycobacterium tuberculosis (Mtb) growth inhibition. A second set of 21 compounds bearing variations on ring C were synthesized and evaluated. This second library gave an additional six compounds displaying MIC values ≤10 μg mL(-1) and total selectivity for Mtb growth inhibition. These compounds serve as an excellent starting point for further development of antitubercular therapies.

Anti malignant (HepG2, MOLT-3) Activity of One, Two, Three- Triazoles New Prepared Bearing Hetero Compounds in Baghdad

“…Is often toxicc to the normal tissue and leads to many side effects, which in turn, limits its treatment efficacyy (7)(8)(9) .…”

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In the current work, chemistry a group of related chemicals that are similar in structure or properties of new heterocyclic compounds were prepared from paraP.nitrobenzoic, acid. This work includes four parts: the first part Preparation of 5-(4-nitro phenyl)-1,33,4-thiaadiazol-2-amine by the reaction of p.pnitrobenzoic acid with thioseemicarbazide,the second part prepared 2-chloro-N-(5-(4-Nnitrophenyl)-1,3,4-thiadiazol-2-yl) Aacetamide by reaction Chloroacetyl chloride with compound and part three contain reaction compound(2) with urea/thiourea to get compounds cyclization by using urea (thiourea) finally step reaction these compounds with different aldehydes and ketones in glacial acetic acid (6)(7)(8)(9)(10) , as shown in Scheme 1The aim of present work is synthesis new derivatives of 1,2,3-Triazole having heterocyclic compounds on ring from the reaction of azine with a different reagent to give (1,2,3-Triazole) rings.The1,2,3-Triaazoles It has been derivatives A long time ago and has been Scout mainly for their potenitial in anti-tTumor chemotherapy the prepared of 11,2,3-Triazole financial products have good AAnti malignant (HepG2, MOLT-3) Activity. Many groupss have ccarried out focused research in this particularr

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Synthesis and anti–microbial activity of 1,2,3–triazole tethered nitroguiacol ethers

“…On the other hand, 1,2,3-triazoles attained great attention due to their broad spectrum of biological activities including antimicrobial [7,8], anti-inflammatory [9,10], analgesic [10], anticancer [7,[11][12][13][14][15][16], antitubercular [17][18][19], local anesthetic [9], immunomodulatory [20], antimalarial [8,21,22], anti-HIV [7,[23][24][25], antileishmanial [26], and antiviral [7] activities. It has become an adjuvant ligand in drug discovery, which has been conjugated to improve the biological properties of molecules.…”

Design, Synthesis and Anticancer Screening of Novel Benzothiazole-Piperazine-1,2,3-Triazole Hybrids

“…In particular, the synthesis of 1,2,3-triazoles has attracted considerable attention during the last years. Several potent pharmacological properties such as anti-bacterial [ 6 ], antimicrobial [ 7 ], antioxidant [ 8 ], anticancer [ 9 ], and antitubecular [ 10 ] of 1,2,3-triazole derivatives have been reported. Some clinically and commercially approved drugs including Carboxyamidotriazole [ 11 ], Tazobactam [ 12 ], and Cifatrizine [ 13 ] were found to possess the 1,2,3-triazole core in their structures.…”